1. Respiratory system
1.1. Lung cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Gefitinib | lressa | 184475-35-2 | EGFR | Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines including NR6, NR6M and NR6W cell lines. | FDA; NMPA |
| Icotinib | Conmana | 610798-31-7 | EGFR | Icotinib Hydrochloride (BPI-2009H), or Icotinib, is a highly selective, first generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). | NMPA |
| Erlotinib | Tarceva | 183321-74-6 | EGFR | Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. | FDA; NMPA |
| Afatinib | Gilotrif | 439081-18-2 | EGFR; HER2; HER4 | Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2. | FDA; NMPA |
| Dacomitinib | Vizimpro | 1110813-31-4 | EGFR | Dacomitinib is an orally bioavailable, highly selective, second-generation small-molecule inhibitor of the pan-epidermal growth factor receptor (EGFR) family of tyrosine kinases (ErbB family) with potential antineoplastic activity. | FDA; NMPA |
| Osimertinib | Tagrisso | 1421373-65-0 | EGFR | Osimertinib is a third-generation, orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. | FDA; NMPA |
| Almonertinib | Ameile | 1899921-05-1 | EGFR | Almonertinib is a third-generation EGFR tyrosine kinase inhibitor targeting EGFR-sensitizing and T790M resistance mutations. | NMPA |
| Furmonertinib | Ivesa | 1869057-83-9 | EGFR T790M | Furmonertinib is an orally available selective inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. | NMPA |
| Crizotinib | Xalkori | 877399-52-5 | ALK; MET; ROS1 | Crizotinib is an anti-cancer drug acting as an ALK (anaplastic lymphoma kinase) and ROS1 (c-ros oncogene 1) inhibitor. | FDA; NMPA |
| Alectinib | Alecensa | 1256580-46-7 | ALK | Alectinib is an oral drug that blocks the activity of anaplastic lymphoma kinase (ALK) and is used to treat non-small-cell lung cancer (NSCLC). | FDA; NMPA |
| Ceritinib | Zykadia | 1032900-25-6 | ALK; ROS1 | An anaplastic lymphoma kinase (ALK)-positive inhibitor used for the treatment of non-small cell lung cancer (NSCLC). | FDA; NMPA |
| Brigatinib | Alunbrig | 1197953-54-0 | ALK | Brigatinib is an orally active, potent and selective dual ALK/EGFR inhibitor. AP26113 is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK; IC50 < 100 nM in Ba/F3 cells). | FDA |
| Lorlatinib | Lorbrena | 1454846-35-5 | ALK; ROS1 | Lorlatinib is an ATP-competitive ROS1/ALK inhibitor with potential antitumor activity. | FDA |
| Ensartinib | Bemena | 1370651-20-9 | ALK | Ensartinib is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. | NMPA |
| Entrectinib | Rozlytrek | 1108743-60-7 | NRTK1/2/3; ALK; ROS1 | Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. | FDA; MHLW |
| Dabrafenib | Tafinlar | 1195765-45-7 | BRAF V600E | Dabrafenib is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively. | FDA |
| Trametinib | Mekinist | 1187431-43-1 | MEK1/2; BRAF V600E | Trametinib is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2. | FDA |
| Vemurafenib | Zelboraf | 918504-65-1 | BRAF V60OE | Vemurafenib is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM. | Not Approved |
| Vandetanib | Caprelsa | 443913-73-3 | RET; EGFR; VEGFR | Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM. | Not Approved |
| Cabozantinib | Cabometyx | 849217-68-1 | RET; MET; VEGFR-1,2,3; C-Kit | Cabozantinib is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively. | Not Approved |
| Ado-trastuzumab emtansine | Kadcyla | HER2 | Ado-trastuzumab emtansine is an Anti-HER2 monoclonal antibody combined with a microtubular inhibitor. | Not Approved | |
| Fam-trastuzumab deruxtecan-nxki | Enhertu | HER2 | Fam-trastuzumab deruxtecan-nxki is composed of an anti-human epidermal growth factor receptor 2 (HER2) antibody and topoisomerase I inhibitor (DXd), which causes DNA damage and apoptotic cell death. | Not Approved | |
| Pyrotinib | Ai Rui Ni | 1269662-73-8 | HER2 | Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively. | Not Approved |
| Tepotinib | TEPMETKO | 1100598-32-0 | MET | Tepotinib is an inhibitor of MET tyrosine kinase with potential antineoplastic activity. | FDA; MHLW |
| Capmatinib | Tabrecta | 1029712-80-8 | MET | Capmatinib, also known as INCB28060 and INC280, is an orally bioavailable inhibitor of the proto-oncogene c-Met (hepatocyte growth factor receptor [HGFR]) with potential antineoplastic activity. | FDA |
| Savolitinib | ORPATHYS | 1313725-88-0 | MET | Savolitinib is a tyrosine kinase inhibitor with potential anticancer activity. | NMPA |
| Selpercatinib | Retevmo | 2152628-33-4 | RET | Selpercatinib is a selective RET inhibitor with antineoplastic activity. | FDA |
| Pralsetinib | Gavreto | 2097132-94-8 | RET | Pralsetinib is a highly effective and selective RET inhibitor. | FDA; NMPA |
| Sotorasib | Lumakras | 2252403-56-6 | KRAS G12C | Sotorasib is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. | FDA |
| Amivantamab | Rybrevant | EGFR 20ins | Amivantamab is an EGFR-MET bispecific antibody with immune cell-directing activity. | FDA | |
| Mobocertinib | Exkivity | 1847461-43-1 | EGFR 20ins | Mobocertinib is an effective and orally active inhibitor of EGFR and HER2 oncogenic mutants. Anti-tumor activity. | FDA |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA; NMPA | |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA; NMPA | |
| lpilimumab | Yervoy | CTLA-4 | Ipilimumab is a human cytotoxic T-lymphocyte antigen 4 (CTLA-4) blocking antibody used to treat metastatic or unresectable melanoma. | FDA | |
| Atezolizumab | Tecentriq | PD-L1 | Atezolizumab is a humanized IgG1 monoclonal anti-programmed death-ligand 1 (PD-L1) antibody that can be used as a single agent or in combination with other chemotherapeutic agents. | FDA; NMPA | |
| Durvalumab | lmfinzi | PD-L1 | Durvalumab is a human immunoglobulin G1 kappa monoclonal antibody that blocks the interaction of programmed cell death ligand 1 with the PD-1. | FDA; NMPA | |
| Cemiplimab | Libtayo | PD-1 | A drug that binds to the protein PD-1 to help immune cells kill cancer cells better and is used to treat different types of cancer | FDA | |
| Camrelizumab | AiRuiKa | PD-1 | Camrelizumab is a humanised IgG4-kappa antiprogrammed cell death 1 (PD-1) monoclonal antibody used in cancer immunotherapy. | NMPA | |
| Tislelizumab | Baize’an | PD-1 | Tislelizumab (BGB-A317) is a humanized IgG4 anti-PD-1 monoclonal antibody specifically designed to minimize binding to FcγR on macrophages. | NMPA | |
| Sintilimab | TYVYT | PD-1 | Sintilimab is a recombinant, fully human IgG4 anti-PD-1 monoclonal antibody. | NMPA | |
| Sugemalimab | Cejemly | PD-L1 | Sugemalimab is an anti-PD-1/PD-L1 monoclonal antibody for patients with stage III and IV NSCLC. | NMPA | |
| Bevacizumab | Avastin | VEGF | Bevacizumab is a humanized monoclonal IgG antibody, and inhibits angiogenesis by binding and neutralizing VEGF-A. | FDA; NMPA | |
| Nintedanib | Ofev | 656247-17-5 | VEGFR-1,2,3; FGFR-1,2,3 | Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM. | EMA |
| Ramucirumab | Cyramza | VEGFR-2 | Ramucirumab is a fully human monoclonal antibody developed for the treatment of solid tumors. | FDA | |
| Anlotinib | FOCUS V | 1058156-90-3 | VEGFR-1,2,3; PDGFR-β | Anlotibib is a multi-targetes kinase inhibitor of receptor tyrosine and could effectively resist the formation of new angiogenesis. | NMPA |
| Necitumumab | Portraza | EGFR | Necitumumab is a monoclonal antibody used to treat metastatic squamous non-small cell lung cancer. | FDA |
1.1.1. Non-small cell lung cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Atezolizumab | Tecentriq | PD-L1 | Atezolizumab is a humanized IgG1 monoclonal anti-programmed death-ligand 1 (PD-L1) antibody that can be used as a single agent or in combination with other chemotherapeutic agents. | FDA; NMPA | |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA | |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA withdraws indication | |
| Durvalumab | lmfinzi | PD-L1 | Durvalumab is a human immunoglobulin G1 kappa monoclonal antibody that blocks the interaction of programmed cell death ligand 1 with the PD-1. | FDA; NMPA | |
| Anlotinib | FOCUS V | 1058156-90-3 | VEGFR-1,2,3; PDGFR-β | Anlotibib is a multi-targetes kinase inhibitor of receptor tyrosine and could effectively resist the formation of new angiogenesis. | NMPA |
1.1.2. Small cell lung cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Cetuximab | Erbitux | EGFR | Cetuximab is used to treat a certain type of cancer of the colon (large intestine) or rectum. | FDA; NMPA | |
| Panitumumab | Vectibix | EGFR | Panitumumab is a type of targeted cancer drug called a monoclonal antibody. | FDA | |
| Encorafenib | Braftovi | 1269440-17-6 | BRAF V60OE | Encorafenib, also known as LGX-818, is an orally available Raf kinase inhibitor with potential antineoplastic activity. | FDA |
| Vemurafenib | Zelboraf | 918504-65-1 | BRAF V60OE | Vemurafenib is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM. | Not Approved |
| Dabrafenib | Tafinlar | 1195765-45-7 | BRAF V600E | Dabrafenib is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively. | Not Approved |
| Trametinib | Mekinist | 871700-17-3 | MEK1/2; BRAF V600E | Trametinib is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2. | Not Approved |
| Trastuzumab | Herceptin | HER2 | Trastuzumab is used to treat HER2-positive breast cancer and gastric cancer. | Not Approved | |
| Pertuzumab | Perjeta | HER2 | Pertuzumab is an antineoplastic agent used in the treatment of HER2-positive metastatic breast cancer in combination with other antineoplastic agents. | Not Approved | |
| Lapatinib | Tykerb | 388082-78-8 | HER2 | Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. | Not Approved |
| Bevacizumab | Avastin | VEGF | Bevacizumab is a humanized monoclonal IgG antibody, and inhibits angiogenesis by binding and neutralizing VEGF-A. | FDA; NMPA | |
| Regorafenib | Stivarga | 755037-03-7 | RET; c-Kit; VEGFR-1/2/3 | Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. | FDA; NMPA |
| Ziv-aflibercept | Zaltrap | VEGFA/B | Ziv-aflibercept (also known as VEGF-trap) works by interfering with the process of angiogenesis by targeting human vascular endothelial growth factor (VEGF). | FDA | |
| Ramucirumab | Cyramza | VEGFR-2 | Ramucirumab is a fully human monoclonal antibody developed for the treatment of solid tumors. | FDA | |
| Fruquintinib | Elunate | 1194506-26-7 | VEGFR-1/2/3 | Fruquintinib is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities. | NMPA |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA; NMPA | |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA | |
| lpilimumab | Yervoy | CTLA-4 | Ipilimumab is a human cytotoxic T-lymphocyte antigen 4 (CTLA-4) blocking antibody used to treat metastatic or unresectable melanoma. | FDA |
2. Digestive system
2.1. Colorectal cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Cetuximab | Erbitux | EGFR | Cetuximab is used to treat a certain type of cancer of the colon (large intestine) or rectum. | FDA; NMPA | |
| Panitumumab | Vectibix | EGFR | Panitumumab is a type of targeted cancer drug called a monoclonal antibody. | FDA | |
| Encorafenib | Braftovi | 1269440-17-6 | BRAF V60OE | Encorafenib, also known as LGX-818, is an orally available Raf kinase inhibitor with potential antineoplastic activity. | FDA |
| Vemurafenib | Zelboraf | 918504-65-1 | BRAF V60OE | Vemurafenib is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM. | Not Approved |
| Dabrafenib | Tafinlar | 1195765-45-7 | BRAF V600E | Dabrafenib is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively. | Not Approved |
| Trametinib | Mekinist | 871700-17-3 | MEK1/2; BRAF V600E | Trametinib is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2. | Not Approved |
| Trastuzumab | Herceptin | HER2 | Trastuzumab is used to treat HER2-positive breast cancer and gastric cancer. | Not Approved | |
| Pertuzumab | Perjeta | HER2 | Pertuzumab is an antineoplastic agent used in the treatment of HER2-positive metastatic breast cancer in combination with other antineoplastic agents. | Not Approved | |
| Lapatinib | Tykerb | 388082-78-8 | HER2 | Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. | Not Approved |
| Bevacizumab | Avastin | VEGF | Bevacizumab is a humanized monoclonal IgG antibody, and inhibits angiogenesis by binding and neutralizing VEGF-A. | FDA; NMPA | |
| Regorafenib | Stivarga | 755037-03-7 | RET; c-Kit; VEGFR-1/2/3 | Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. | FDA; NMPA |
| Ziv-aflibercept | Zaltrap | VEGFA/B | Ziv-aflibercept (also known as VEGF-trap) works by interfering with the process of angiogenesis by targeting human vascular endothelial growth factor (VEGF). | FDA | |
| Ramucirumab | Cyramza | VEGFR-2 | Ramucirumab is a fully human monoclonal antibody developed for the treatment of solid tumors. | FDA | |
| Fruquintinib | Elunate | 1194506-26-7 | VEGFR-1/2/3 | Fruquintinib is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities. | NMPA |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA; NMPA | |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA | |
| lpilimumab | Yervoy | CTLA-4 | Ipilimumab is a human cytotoxic T-lymphocyte antigen 4 (CTLA-4) blocking antibody used to treat metastatic or unresectable melanoma. | FDA |
2.2. Gastric cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Ramucirumab | Cyramza | VEGFR-2 | Ramucirumab is a fully human monoclonal antibody developed for the treatment of solid tumors. | FDA | |
| Apatinib | Aitan | 1218779-75-9 | VEGFR-2 | Apatinib mesylate is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. | NMPA |
| Trastuzumab | Herceptin | HER2 | Trastuzumab is used to treat HER2-positive breast cancer and gastric cancer. | FDA; NMPA | |
| Fam-trastuzumab deruxtecan-nxki | Enhertu | HER2 | Fam-trastuzumab deruxtecan-nxki is composed of an anti-human epidermal growth factor receptor 2 (HER2) antibody and topoisomerase I inhibitor (DXd), which causes DNA damage and apoptotic cell death. | FDA | |
| Disitamab Vedotin | Aidixi | HER2 | Disitamab vedotin is a novel ADC that selectively delivers the anti-cancer agent monomethyl auristatin E (MMAE) into HER2-expressing tumor cells. | NMPA | |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA | |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA; NMPA |
2.3. Esophageal cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Trastuzumab | Herceptin | HER2 | Trastuzumab is used to treat HER2-positive breast cancer and gastric cancer. | FDA; NMPA | |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA; NMPA | |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA; NMPA | |
| Camrelizumab | AiRuiKa | PD-1 | Camrelizumab is a humanised IgG4-kappa antiprogrammed cell death 1 (PD-1) monoclonal antibody used in cancer immunotherapy. | NMPA | |
| Anlotinib | FOCUS V | 1058156-90-3 | VEGFR-1,2,3; PDGFR-β | Anlotibib is a multi-targetes kinase inhibitor of receptor tyrosine and could effectively resist the formation of new angiogenesis. | Not Approved |
| Apatinib | Aitan | 1218779-75-9 | VEGFR-2 | Apatinib mesylate is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. | Not Approved |
| Ramucirumab | Cyramza | VEGFR-2 | Ramucirumab is a fully human monoclonal antibody developed for the treatment of solid tumors. | Not Approved |
2.4. Hepatocellular carcinoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Lenvatinib | Lenvima | 417716-92-8 | VEGFR-1,2,3; C-Kit; RET | Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM. | FDA; NMPA |
| Sorafenib | Nexavar | 284461-73-0 | VEGFR-1,2,3; RET/PTC; BRAF | Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. | FDA; NMPA |
| Regorafenib | Stivarga | 755037-03-7 | RET; c-Kit; VEGFR-1/2/3 | Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. | FDA; NMPA |
| Cabozantinib | Cabometyx | 849217-68-1 | RET; MET; VEGFR-1,2,3; C-Kit | Cabozantinib is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively. | FDA |
| Apatinib | Aitan | 1218779-75-9 | VEGFR-2 | Apatinib mesylate is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. | NMPA |
| Donafenib | Zepsun | 1130115-44-4 | VEGFR; PDGFR | Donafenib is an orally available multikinase inhibitor that targets Raf kinase and various receptor tyrosine kinases (RTKs), with potential antineoplastic activity. | NMPA |
| Ramucirumab | Cyramza | VEGFR-2 | Ramucirumab is a fully human monoclonal antibody developed for the treatment of solid tumors. | FDA | |
| Bevacizumab | Avastin | VEGF | Bevacizumab is a humanized monoclonal IgG antibody, and inhibits angiogenesis by binding and neutralizing VEGF-A. | FDA; NMPA | |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA | |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA | |
| lpilimumab | Yervoy | CTLA-4 | Ipilimumab is a human cytotoxic T-lymphocyte antigen 4 (CTLA-4) blocking antibody used to treat metastatic or unresectable melanoma. | FDA | |
| Atezolizumab | Tecentriq | PD-L1 | Atezolizumab is a humanized IgG1 monoclonal anti-programmed death-ligand 1 (PD-L1) antibody that can be used as a single agent or in combination with other chemotherapeutic agents. | FDA; NMPA | |
| Camrelizumab | AiRuiKa | PD-1 | Camrelizumab is a humanised IgG4-kappa antiprogrammed cell death 1 (PD-1) monoclonal antibody used in cancer immunotherapy. | NMPA | |
| Tislelizumab | Baize’an | PD-1 | Tislelizumab (BGB-A317) is a humanized IgG4 anti-PD-1 monoclonal antibody specifically designed to minimize binding to FcγR on macrophages. | NMPA | |
| Sintilimab | TYVYT | PD-1 | Sintilimab is a recombinant, fully human IgG4 anti-PD-1 monoclonal antibody. | NMPA |
2.5. Pancreatic cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Erlotinib | Tarceva | 183321-74-6 | EGFR | Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. | FDA |
| Nimotuzumab | BIOMAb-EGFR | EGFR | Nimotuzumab is a humanized therapeutic monoclonal antibody against epidermal growth factor receptor (EGFR). | Not Approved | |
| Olaparib | Lynparza | 763113-22-0 | PARP-1,2,3 | Olaparib is a small-molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential chemosensitizing, radiosensitizing, and antineoplastic activities. | FDA |
2.6. Biliary tract tumors
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Pemigatinib | PEMAZYRE | 1513857-77-6 | FGFR2 | Pemigatinib is an inhibitor of fibroblast growth factor receptor types 1, 2, and 3 (FGFR1/2/3). | FDA |
| Infigratinib | Truseltiq | 872511-34-7 | FGFR2 | Infigratinib is a pan FGFR kinase inhibitor, and is an orally bioavailable pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities. | FDA |
| Ivosidenib | Tibsovo | 1448347-49-6 | IDH1 | Ivosidenib is an oral inhibitor that specifically inhibits a mutated form of IDH1 in the cytoplasm, which blocks the proliferation of tumor cells expressing IDH1. | FDA |
| Dabrafenib | Tafinlar | 1195765-45-7 | BRAF V600E | Dabrafenib is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively. | Not Approved |
| Trametinib | Mekinist | 1187431-43-1 | MEK1/2; BRAF V600E | Trametinib is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2. | Not Approved |
| Regorafenib | Stivarga | 755037-03-7 | RET; c-Kit; VEGFR-1/2/3 | Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. | Not Approved |
| Lenvatinib | Lenvima | 417716-92-8 | VEGFR-1,2,3; C-Kit; RET | Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM. | Not Approved |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | Not Approved | |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | Not Approved | |
| Camrelizumab | AiRuiKa | PD-1 | Camrelizumab is a humanised IgG4-kappa antiprogrammed cell death 1 (PD-1) monoclonal antibody used in cancer immunotherapy. | Not Approved |
3. Gynecological oncology
3.1. Ovarian cancer, fallopian tube cancer, peritoneal cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Bevacizumab | Avastin | VEGF | Bevacizumab is a humanized monoclonal IgG antibody, and inhibits angiogenesis by binding and neutralizing VEGF-A. | FDA; NMPA | |
| Pazopanib | Votrient | 444731-52-6 | VEGFR-1,2,3; PDGFR-α,B; c-Kit | Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively. | Not Approved |
| Sorafenib | Nexavar | 284461-73-0 | VEGFR-1,2,3; RET/PTC; BRAF | Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. | Not Approved |
| Olaparib | Lynparza | 763113-22-0 | PARP-1,2,3 | Olaparib is a small-molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential chemosensitizing, radiosensitizing, and antineoplastic activities. | FDA; NMPA |
| Rucaparib | Rubraca | 283173-50-2 | PARP-1,2,3 | Rucaparib, also named as AG-014699 or PF-01367338, is a poly (ADP ribose) polymerase (PARP) inhibitor. | FDA |
| Niraparib | Zejula | 1038915-60-4 | PARP-1,2 | Niraparib is an inhibitor of PARP, which was approved by FDA for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy. | FDA; NMPA |
| Fluzoparib | AiRuiYi | 1358715-18-0 | PARP | Fuzuloparib is an orally available inhibitor of poly (ADP-ribose) polymerase (PARP) types 1 and 2, with potential antineoplastic activity. | NMPA |
| Pamiparib | BGB-290 | 1446261-44-4 | PARP | Pamiparib is a potent and selective inhibitor of PARP1/PARP2 displaying anticancer activity. | NMPA |
3.2. Cervical cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Bevacizumab | Avastin | VEGF | Bevacizumab is a humanized monoclonal IgG antibody, and inhibits angiogenesis by binding and neutralizing VEGF-A. | FDA; NMPA | |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA | |
| Tisotumab vedotin | Tivdak | TF | Tisotumab vedotin is designed to target tissue factor (TF) using our proprietary antibody-drug conjugate (ADC) technology. | FDA |
3.3. Endometrial cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Trastuzumab | Herceptin | HER2 | Trastuzumab is used to treat HER2-positive breast cancer and gastric cancer. | Not Approved | |
| Everolimus | Afinitor | 159351-69-6 | mTOR | Everolimus is an inhibitor of mammalian target of rapamycin (mTOR) with an immunosuppressive activity which is comparable to that of rapamycin. | Not Approved |
| Bevacizumab | Avastin | VEGF | Bevacizumab is a humanized monoclonal IgG antibody, and inhibits angiogenesis by binding and neutralizing VEGF-A. | Not Approved | |
| Lenvatinib | Lenvima | 417716-92-8 | VEGFR-1,2,3; C-Kit; RET | Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM. | FDA |
| Pazopanib | Votrient | 444731-52-6 | VEGFR-1,2,3; PDGFR-α,B; c-Kit | Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively. | Not Approved |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA | |
| Dostarlimab | Jemperli | PD-1 | Dostarlimab is a monoclonal antibody used as a medication for the treatment of endometrial cancer. | FDA |
4. Urogenital system
4.1. Kidney cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Sorafenib | Nexavar | 284461-73-0 | VEGFR-1,2,3; RET/PTC; BRAF | Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. | FDA; NMPA |
| Cabozantinib | Cabometyx | 849217-68-1 | RET; MET; VEGFR-1,2,3; C-Kit | Cabozantinib is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively. | FDA |
| Sunitinib | SUTENT | 557795-19-4 | VEGFR-1,2,3 | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. | FDA; NMPA |
| Lenvatinib | Lenvima | 417716-92-8 | VEGFR-1,2,3; C-Kit; RET | Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM. | FDA |
| Pazopanib | Votrient | 444731-52-6 | VEGFR-1,2,3; PDGFR-α,B; c-Kit | Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively. | FDA; NMPA |
| Bevacizumab | Avastin | VEGF | Bevacizumab is a humanized monoclonal IgG antibody, and inhibits angiogenesis by binding and neutralizing VEGF-A. | FDA | |
| Axitinib | lnlyta | 319460-85-0 | VEGFR-1,2,3 | Axitinib is a tyrosine kinase inhibitor that blocks the activation of VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ (IC50 = 1.2, 0.25, 0.29, 1.7, and 1.6 nM, respectively). | FDA; NMPA |
| Tivozanib | Fotivda | 475108-18-0 | VEGFR-1,2,3 | Tivozanib is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities. | FDA |
| Everolimus | Afinitor | 159351-69-6 | mTOR | Everolimus is an inhibitor of mammalian target of rapamycin (mTOR) with an immunosuppressive activity which is comparable to that of rapamycin. | FDA; NMPA |
| Temsirolimus | Torisel | 162635-04-3 | mTOR | Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM. | FDA |
| Erlotinib | Tarceva | 183321-74-6 | EGFR | Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. | Not Approved |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA | |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA | |
| lpilimumab | Yervoy | CTLA-4 | Ipilimumab is a human cytotoxic T-lymphocyte antigen 4 (CTLA-4) blocking antibody used to treat metastatic or unresectable melanoma. | FDA | |
| Avelumab | Bavencio | PD-L1 | Avelumab is a fully human monoclonal antibody medication for the treatment of Merkel cell carcinoma, urothelial carcinoma, and renal cell carcinoma. | FDA | |
| Camrelizumab | AiRuiKa | PD-1 | Camrelizumab is a humanised IgG4-kappa antiprogrammed cell death 1 (PD-1) monoclonal antibody used in cancer immunotherapy. | NMPA |
4.2. Bladder cancer (including urothelial cancer)
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Erdafitinib | Balversa | 1346242-81-6 | FGFR-1,2,3,4; PDGFR-α,β | Erdafitinib, also known as JNJ-42756493, is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. | FDA |
| Atezolizumab | Tecentriq | PD-L1 | Atezolizumab is a humanized IgG1 monoclonal anti-programmed death-ligand 1 (PD-L1) antibody that can be used as a single agent or in combination with other chemotherapeutic agents. | FDA | |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA | |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA | |
| Avelumab | Bavencio | PD-L1 | Avelumab is a fully human monoclonal antibody medication for the treatment of Merkel cell carcinoma, urothelial carcinoma, and renal cell carcinoma. | FDA | |
| Durvalumab | lmfinzi | PD-L1 | Durvalumab is a human immunoglobulin G1 kappa monoclonal antibody that blocks the interaction of programmed cell death ligand 1 with the PD-1. | FDA | |
| Tislelizumab | Baize’an | PD-1 | Tislelizumab (BGB-A317) is a humanized IgG4 anti-PD-1 monoclonal antibody specifically designed to minimize binding to FcγR on macrophages. | NMPA | |
| Toripalimab | Tuoyi | PD-1 | Toripalimab is a selective, recombinant, humanized monoclonal antibody against programmed death protein 1 (PD-1) | NMPA | |
| Enfortumab vedotin-ejfv | Padcev | Nectin-4 | Enfortumab vedotin-ejfv has been approved for people with advanced bladder cancer. | FDA | |
| Sacituzumab govitecan-hziy | Trodelvy | Trop-2 | Sacituzumab govitecan-hziy is an antibody-drug conjugate that combines a humanized monoclonal antibody. | FDA |
4.3. Prostate cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | Not Approved | |
| Rucaparib | Rubraca | 283173-50-2 | PARP-1,2,3 | Rucaparib, also named as AG-014699 or PF-01367338, is a poly (ADP ribose) polymerase (PARP) inhibitor. | FDA |
| Olaparib | Lynparza | 763113-22-0 | PARP-1,2,3 | Olaparib is a small-molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential chemosensitizing, radiosensitizing, and antineoplastic activities. | FDA; NMPA |
5. Breast cancer and surface tumors
5.1. Breast cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Trastuzumab | Herceptin | HER2 | Trastuzumab is used to treat HER2-positive breast cancer and gastric cancer. | FDA; NMPA | |
| Ado-trastuzumab emtansine | Kadcyla | HER2 | Ado-trastuzumab emtansine is an Anti-HER2 monoclonal antibody combined with a microtubular inhibitor. | FDA; NMPA | |
| Pertuzumab | Perjeta | HER2 | Pertuzumab is an antineoplastic agent used in the treatment of HER2-positive metastatic breast cancer in combination with other antineoplastic agents. | FDA; NMPA | |
| Lapatinib | Tykerb | 388082-78-8 | HER2 | Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. | FDA; NMPA |
| Pyrotinib | Ai Rui Ni | 1269662-73-8 | HER2 | Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively. | NMPA |
| Neratinib | Nerlynx | 698387-09-6 | EGFR; HER2; HER4 | Neratinib, also known as HKI-272 or PB272, is an orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. | FDA; NMPA |
| Fam-trastuzumab deruxtecan-nxki | Enhertu | HER2 | Fam-trastuzumab deruxtecan-nxki is composed of an anti-human epidermal growth factor receptor 2 (HER2) antibody and topoisomerase I inhibitor (DXd), which causes DNA damage and apoptotic cell death. | FDA | |
| Tucatinib | Tukysa | 937263-43-9 | HER2 | Tucatinib is a small molecule inhibitor of HER2 for the treatment of HER2-positive breast cancer. | FDA |
| Inetetamab | Cipterbin | HER2 | Inetetamab is a monoclonal antibody binding to domain IV of HER2 receptor. | NMPA | |
| Margetuximab-cmkb | Margenza | HER2 | Margetuximab-cmkb (Margenza) medically necessary for treatment of HER2-positive recurrent unresectable or metastatic breast cancer. | FDA | |
| Olaparib | Lynparza | 763113-22-0 | PARP-1,2,3 | Olaparib is a small-molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential chemosensitizing, radiosensitizing, and antineoplastic activities. | FDA |
| Talazoparib | Talzenna | 1207456-01-6 | PARP-1,2 | Talazoparib is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity. | FDA |
| Alpelisib | Piqray | 1217486-61-7 | PIK3CA | Alpelisib is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. | FDA |
| Palbociclib | lbrance | 571190-30-2 | CDK4/6 | Palbociclib is an orally available cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. | FDA; NMPA |
| Abemaciclib | Verzeni | 1231929-97-7 | CDK4/6 | Abemaciclib is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. | FDA |
| Ribociclib | Kisqali | 1211441-98-3 | CDK4/6 | Ribociclib is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. | FDA |
| Dalpiciclib | AiRuiKang | 1637781-04-4 | CDK4/6 | Dalpiciclib is a cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. | NMPA |
| Everolimus | Afinitor | 159351-69-6 | mTOR | Everolimus is an inhibitor of mammalian target of rapamycin (mTOR) with an immunosuppressive activity which is comparable to that of rapamycin. | FDA |
| Sacituzumab govitecan-hziy | Trodelvy | Trop-2 | Sacituzumab govitecan-hziy is an antibody-drug conjugate that combines a humanized monoclonal antibody. | FDA | |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA |
5.2. Melanoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Vemurafenib | Zelboraf | 918504-65-1 | BRAF V60OE | Vemurafenib is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM. | FDA; NMPA |
| Cobimetinib | Cotellic | 934660-93-2 | MEK1/2; BRAF V600 | Cobimetinib is a potent, orally available and highly selective MEK1 inhibitor with IC50 of 4.2 nM. | FDA |
| Dabrafenib | Tafinlar | 1195765-45-7 | BRAF V600E | Dabrafenib is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively. | FDA; NMPA |
| Trametinib | Mekinist | 1187431-43-1 | MEK1/2; BRAF V600E | Trametinib is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2. | FDA; NMPA |
| Encorafenib | Braftovi | 1269440-17-6 | BRAF V60OE | Encorafenib, also known as LGX-818, is an orally available Raf kinase inhibitor with potential antineoplastic activity. | FDA |
| Binimetinib | Mektovi | 606143-89-9 | MEK1/2 | Binimetinib is an oral, highly selective MEK inhibitor. | FDA |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA | |
| lpilimumab | Yervoy | CTLA-4 | Ipilimumab is a human cytotoxic T-lymphocyte antigen 4 (CTLA-4) blocking antibody used to treat metastatic or unresectable melanoma. | FDA | |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA; NMPA | |
| Toripalimab | Tuoyi | PD-1 | Toripalimab is a selective, recombinant, humanized monoclonal antibody against programmed death protein 1 (PD-1) | NMPA | |
| Atezolizumab | Tecentriq | PD-L1 | Atezolizumab is a humanized IgG1 monoclonal anti-programmed death-ligand 1 (PD-L1) antibody that can be used as a single agent or in combination with other chemotherapeutic agents. | FDA | |
| Imatinib | Gleevec | 152459-95-5 | BCR-ABL; PDGFRA; c-Kit | Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM. | Not Approved |
5.3. Basal cell carcinoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Sonidegib | Odomzo | 956697-53-3 | SMO | Sonidegib is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. | FDA; NMPA |
| Vismodegib | Erivedge | 879085-55-9 | SMO | Vismodegib (GDC-0449) is a potent, novel and specific inhibitor of hedgehog with IC50 of 3 nM and also inhibitor of P-gp with IC50 of 3.0 μM. | FDA |
| Cemiplimab | Libtayo | PD-1 | A drug that binds to the protein PD-1 to help immune cells kill cancer cells better and is used to treat different types of cancer | FDA |
5.4. Merkel cell carcinoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | Not Approved | |
| Avelumab | Bavencio | PD-L1 | Avelumab is a fully human monoclonal antibody medication for the treatment of Merkel cell carcinoma, urothelial carcinoma, and renal cell carcinoma. | FDA | |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA |
6. Bone and soft tissue sarcomas
6.1. Soft tissue sarcomas
6.1.1. Gastrointestinal stromal tumors
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Imatinib | Gleevec | 152459-95-5 | BCR-ABL; PDGFRA; c-Kit | Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM. | FDA; NMPA |
| Sunitinib | SUTENT | 557795-19-4 | VEGFR-1,2,3 | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. | FDA; NMPA |
| Regorafenib | Stivarga | 755037-03-7 | RET; c-Kit; VEGFR-1/2/3 | Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. | FDA; NMPA |
| Ripretinib | Qinlock | 1442472-39-0 | c-Kit; PDGFRA | Ripretinib is an orally bioavailable KIT/PDGFR inhibitor with antitumor effect. | FDA; NMPA |
| Avapritinib | AYVAKIT | 1703793-34-3 | PDGFRA E18 | Avapritinib is a potent and selective inhibitor of exon 17 mutant KIT (IC50= 0.27 nM for KIT D816V). | FDA; NMPA |
| Dasatinib | Sprycel | 302962-49-8 | PDGFRA D842V | Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. | Not Approved |
| Cabozantinib | Cabometyx | 849217-68-1 | RET; MET; VEGFR-1,2,3; C-Kit | Cabozantinib is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively. | Not Approved |
| Sorafenib | Nexavar | 284461-73-0 | VEGFR-1,2,3; RET/PTC; BRAF | Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. | Not Approved |
| Nilotinib | Tasigna | 641571-10-0 | BCR-ABL; c-Kit | Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM. | Not Approved |
| Pazopanib | Votrient | 444731-52-6 | VEGFR-1,2,3; PDGFR-α,B; c-Kit | Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively. | Not Approved |
| Everolimus | Afinitor | 159351-69-6 | mTOR | Everolimus is an inhibitor of mammalian target of rapamycin (mTOR) with an immunosuppressive activity which is comparable to that of rapamycin. | Not Approved |
6.1.2. Desmoid tumors
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Imatinib | Gleevec | 152459-95-5 | BCR-ABL; PDGFRA; c-Kit | Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM. | Not Approved |
| Sorafenib | Nexavar | 284461-73-0 | VEGFR-1,2,3; RET/PTC; BRAF | Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. | Not Approved |
6.1.3. Pigmented villonodular synovitis / Giant cell tumor of the tendon sheath
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Imatinib | Gleevec | 152459-95-5 | BCR-ABL; PDGFRA; c-Kit | Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM. | Not Approved |
| Pexidartinib | Turalio | 1029044-16-3 | CSF1R; c-Kit | Pexidartinib is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R with IC50 of 20 nM, Kit with IC50 of 10 nM, and Flt3 with IC50 160 nM. | FDA |
6.1.4. Angiosarcoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Sorafenib | Nexavar | 284461-73-0 | VEGFR-1,2,3; RET/PTC; BRAF | Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. | Not Approved |
| Sunitinib | SUTENT | 557795-19-4 | VEGFR-1,2,3 | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. | Not Approved |
| Bevacizumab | Avastin | VEGF | Bevacizumab is a humanized monoclonal IgG antibody, and inhibits angiogenesis by binding and neutralizing VEGF-A. | Not Approved |
6.1.5. Solitary fibroma / Hemangiopericytoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Bevacizumab | Avastin | VEGF | Bevacizumab is a humanized monoclonal IgG antibody, and inhibits angiogenesis by binding and neutralizing VEGF-A. | Not Approved | |
| Sorafenib | Nexavar | 284461-73-0 | VEGFR-1,2,3; RET/PTC; BRAF | Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. | Not Approved |
| Sunitinib | SUTENT | 557795-19-4 | VEGFR-1,2,3 | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. | Not Approved |
| Pazopanib | Votrient | 444731-52-6 | VEGFR-1,2,3; PDGFR-α,B; c-Kit | Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively. | Not Approved |
6.1.6. Acinar soft tissue sarcoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Sunitinib | SUTENT | 557795-19-4 | VEGFR-1,2,3 | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. | Not Approved |
| Pazopanib | Votrient | 444731-52-6 | VEGFR-1,2,3; PDGFR-α,B; c-Kit | Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively. | Not Approved |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | Not Approved | |
| Anlotinib | FOCUS V | 1058156-90-3 | VEGFR-1,2,3; PDGFR-β | Anlotibib is a multi-targetes kinase inhibitor of receptor tyrosine and could effectively resist the formation of new angiogenesis. | NMPA |
6.1.7. Inflammatory myofibroblastic tumor
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Crizotinib | Xalkori | 877399-52-5 | ALK; MET; ROS1 | Crizotinib is an anti-cancer drug acting as an ALK (anaplastic lymphoma kinase) and ROS1 (c-ros oncogene 1) inhibitor. | Not Approved |
| Ceritinib | Zykadia | 1032900-25-6 | ALK; ROS1 | An anaplastic lymphoma kinase (ALK)-positive inhibitor used for the treatment of non-small cell lung cancer (NSCLC). | Not Approved |
6.1.8. Undifferentiated pleomorphic sarcoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | Not Approved |
6.1.9. Retroperitoneal well-differentiated / Dedifferentiated liposarcoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Palbociclib | lbrance | 571190-30-2 | CDK4/6 | Palbociclib is an orally available cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. | Not Approved |
6.1.10. Perivascular epithelioid cell tumor / Recurrent angiomyolipoma / Lymphangioleiomyoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Everolimus | Afinitor | 159351-69-6 | mTOR | Everolimus is an inhibitor of mammalian target of rapamycin (mTOR) with an immunosuppressive activity which is comparable to that of rapamycin. | Not Approved |
| Sirolimus | Rapamune | 53123-88-9 | mTOR | Sirolimus is an mTOR inhibitor immunosuppressant and kinase inhibitor with both antifungal and antineoplastic properties. | FDA |
| nab-sirolimus | Fyarro | mTOR | nab-Sirolimus is active in patients with malignant PEComa. | FDA | |
| Temsirolimus | Torisel | 162635-04-3 | mTOR | Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM. | Not Approved |
6.2. Chordoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Imatinib | Gleevec | 152459-95-5 | BCR-ABL; PDGFRA; c-Kit | Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM. | Not Approved |
| Sirolimus | Rapamune | 53123-88-9 | mTOR | Sirolimus is an mTOR inhibitor immunosuppressant and kinase inhibitor with both antifungal and antineoplastic properties. | Not Approved |
| Erlotinib | Tarceva | 183321-74-6 | EGFR | Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. | Not Approved |
| Sunitinib | SUTENT | 557795-19-4 | VEGFR-1,2,3 | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. | Not Approved |
| Lapatinib | Tykerb | 388082-78-8 | HER2 | Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. | Not Approved |
| Sorafenib | Nexavar | 284461-73-0 | VEGFR-1,2,3; RET/PTC; BRAF | Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. | Not Approved |
| Dasatinib | Sprycel | 302962-49-8 | PDGFRA D842V | Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. | Not Approved |
6.3. Multiple myeloma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Daratumumab | Darzalex | CD38 | Daratumumab is an anti-cancer monoclonal antibody medication. | FDA; NMPA | |
| Elotuzumab | Empliciti | SLAMF7 | Elotuzumab is an antibody approved to treat multiple myeloma. | FDA | |
| Selinexor | Xpovio | 1393477-72-9 | XPO1 | Selinexor is a potent and selective inhibitor of chromosome region maintenance 1 protein/exportin 1 (CRM1/XPO1). | FDA; NMPA |
| Venetoclax | Venclexta | 1257044-40-8 | BCL-2 | Venetoclax is a small-molecule inhibitor that has high selectivity for Bcl-2 (Ki < 0.01 nM in cell-free assays) over Mcl-1. | FDA |
| Belantamab mafodotin-blmf | Blenrep | BCMA | Belantamab mafodotin is a medication for the treatment of relapsed and refractory multiple myeloma. | FDA | |
| Carfilzomib | Kyprolis | 868540-17-4 | Proteasome | Carfilzomib is a tetrapeptide epoxyketone and an analog of epoxomicin, acting as a selective proteasome inhibitor. | FDA |
7. Central nervous system tumors
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Bevacizumab | Avastin | VEGF | Bevacizumab is a humanized monoclonal IgG antibody, and inhibits angiogenesis by binding and neutralizing VEGF-A. | FDA | |
| Everolimus | Afinitor | 159351-69-6 | mTOR | Everolimus is an inhibitor of mammalian target of rapamycin (mTOR) with an immunosuppressive activity which is comparable to that of rapamycin. | FDA; NMPA |
| Lapatinib | Tykerb | 388082-78-8 | HER2 | Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. | Not Approved |
| Rituximab | Rituxan | CD20 | Rituximab is a monoclonal antibody medication used to treat certain autoimmune diseases and types of cancer. | Not Approved | |
| Ibrutinib | Imbruvica | BTK | Ibrutinib is a small molecule drug that inhibits B-cell proliferation and survival by irreversibly binding the protein Bruton’s tyrosine kinase. | Not Approved | |
| Dinutuximab | Unituxin | GD2 | Dinutuximab is a monoclonal antibody used as a second-line treatment for children with high-risk neuroblastoma. | FDA | |
| Dinutuximab beta | Qarziba | GD2 | Dinutuximab beta is a monoclonal antibody used as a second-line treatment for children with high-risk neuroblastoma. | NMPA |
8. Head and neck tumors
8.1. Thyroid cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Selpercatinib | Retevmo | 2152628-33-4 | RET | Selpercatinib is a selective RET inhibitor with antineoplastic activity. | FDA |
| Pralsetinib | Gavreto | 2097132-94-8 | RET | Pralsetinib is a highly effective and selective RET inhibitor. | FDA |
| Vandetanib | Caprelsa | 443913-73-3 | RET; EGFR; VEGFR | Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM. | FDA |
| Cabozantinib | Cabometyx | 849217-68-1 | RET; MET; VEGFR-1,2,3; C-Kit | Cabozantinib is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively. | FDA |
| Sorafenib | Nexavar | 284461-73-0 | VEGFR-1,2,3; RET/PTC; BRAF | Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. | FDA; NMPA |
| Lenvatinib | Lenvima | 417716-92-8 | VEGFR-1,2,3; C-Kit; RET | Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM. | FDA; NMPA |
| Sunitinib | SUTENT | 557795-19-4 | VEGFR-1,2,3 | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. | Not Approved |
| Pazopanib | Votrient | 444731-52-6 | VEGFR-1,2,3; PDGFR-α,B; c-Kit | Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively. | Not Approved |
| Anlotinib | FOCUS V | 1058156-90-3 | VEGFR-1,2,3; PDGFR-β | Anlotibib is a multi-targetes kinase inhibitor of receptor tyrosine and could effectively resist the formation of new angiogenesis. | NMPA |
| Dabrafenib | Tafinlar | 1195765-45-7 | BRAF V600E | Dabrafenib is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively. | FDA |
| Trametinib | Mekinist | 1187431-43-1 | MEK1/2; BRAF V600E | Trametinib is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2. | FDA |
| Vemurafenib | Zelboraf | 918504-65-1 | BRAF V60OE | Vemurafenib is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM. | Not Approved |
8.2. Head and neck cancer
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Cetuximab | Erbitux | EGFR | Cetuximab is used to treat a certain type of cancer of the colon (large intestine) or rectum. | FDA; NMPA | |
| Nimotuzumab | BIOMAb-EGFR | EGFR | Nimotuzumab is a humanized therapeutic monoclonal antibody against epidermal growth factor receptor (EGFR). | NMPA | |
| Afatinib | Gilotrif | 439081-18-2 | EGFR; HER2; HER4 | Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2. | Not Approved |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA; NMPA | |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA; NMPA | |
| Toripalimab | Tuoyi | PD-1 | Toripalimab is a selective, recombinant, humanized monoclonal antibody against programmed death protein 1 (PD-1) | NMPA | |
| Camrelizumab | AiRuiKa | PD-1 | Camrelizumab is a humanised IgG4-kappa antiprogrammed cell death 1 (PD-1) monoclonal antibody used in cancer immunotherapy. | NMPA |
9. Hematological tumors and lymphomas
9.1. Lymphoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Rituximab | Rituxan | CD20 | Rituximab is a monoclonal antibody medication used to treat certain autoimmune diseases and types of cancer. | FDA; NMPA | |
| Tositumomab | Bexxar | CD20 | Tositumomab is a murine monoclonal antibody which targets the CD20 antigen produced in mammalian cell. | FDA | |
| Obinutuzumab | Gazyva | CD20 | Obinutuzumab is a humanized anti-CD20 monoclonal antibody as a cancer treatment. | FDA; NMPA | |
| Ibritumomab | Zevalin | CD20 | Ibritumomab is a monoclonal antibody radioimmunotherapy treatment for non-Hodgkin’s lymphoma. | FDA | |
| Brentuximab | Adcetris | CD30 | Brentuximab is an antibody-drug conjugate medication used to treat relapsed or refractory Hodgkin lymphoma and systemic anaplastic large cell lymphoma. | FDA; NMPA | |
| Ibrutinib | Imbruvica | BTK | Ibrutinib is a small molecule drug that inhibits B-cell proliferation and survival by irreversibly binding the protein Bruton’s tyrosine kinase. | FDA; NMPA | |
| Zanubrutinib | RPIIKINSA | 1691249-45-2 | BTK | Zanubrutinib is a potent and irreversible BTK inhibitor. | FDA; NMPA |
| Orelabrutinib | InnoCare | 1655504-04-3 | BTK | Orelabrutinib is an orally administered, potent, irreversible and highly selective BTK inhibitor. | NMPA |
| Idelalisib | Zydelig | 870281-82-6 | Pl3K | Idelalisib is a kinase inhibitor. In combination with rituximab, it was used for the treatment of relapsed or refractory chronic lymphocytic leukemia (CLL). | FDA |
| Venetoclax | Venclexta | 1257044-40-8 | BCL-2 | Venetoclax is a small-molecule inhibitor that has high selectivity for Bcl-2 (Ki < 0.01 nM in cell-free assays) over Mcl-1. | FDA; NMPA |
| Siltuximab | Sylvant | IL6 | Siltuximab is a chimeric monoclonal antibody. It binds to interleukin-6. | FDA | |
| Polatuzumab Vedotin-piiq | POLIVY | CD79b | Polatuzumab vedotin-piiq is a first-in-class CD79b-directed antibody-drug conjugate with activity against dividing B cells. | FDA | |
| Tazemetostat | Tazverik | 1403254-99-8 | EZH2 | Tazemetostat is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. | FDA |
| Brexucabtagene Autoleucel | TECARTUS | CD19 | Brexucabtagene autoleucel is a cell-based gene therapy medication for the treatment of mantle cell lymphoma and acute lymphoblastic leukemia. | FDA | |
| Blinatumomab | Blincyto | CD19/CD3 | Blinatumomab is a biopharmaceutical medication used as a second-line treatment for Philadelphia chromosome-negative relapsed or refractory acute lymphoblastic leukemia. | NMPA | |
| Loncastuximab tesirine | Zynlonta | CD19 | Loncastuximab tesirine is a monoclonal antibody conjugate medication used to treat large B-cell lymphoma. | FDA | |
| Crizotinib | Xalkori | 877399-52-5 | ALK; MET; ROS1 | Crizotinib is an anti-cancer drug acting as an ALK (anaplastic lymphoma kinase) and ROS1 (c-ros oncogene 1) inhibitor. | FDA |
| Umbralisib | Ukoniq | 1532533-67-7 | PI3K6; CK1E | Umbralisib is an orally bioavailable and selective PI3K delta inhibitor that targets delta isoform with nanomolar potency. | FDA |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA | |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA | |
| Sintilimab | TYVYT | PD-1 | Sintilimab is a recombinant, fully human IgG4 anti-PD-1 monoclonal antibody. | NMPA | |
| Camrelizumab | AiRuiKa | PD-1 | Camrelizumab is a humanised IgG4-kappa antiprogrammed cell death 1 (PD-1) monoclonal antibody used in cancer immunotherapy. | NMPA | |
| Tislelizumab | Baize’an | PD-1 | Tislelizumab (BGB-A317) is a humanized IgG4 anti-PD-1 monoclonal antibody specifically designed to minimize binding to FcγR on macrophages. | NMPA | |
| Piamprilumab | Aniko | PD-1 | The drug is approved for classical Hodgkin’s lymphoma. | NMPA | |
| Sepalizumab | / | PD-1 | Sepalizumab (GLS-010) is a fully human anti-PD-1 monoclonal antibody that has been naturally selected by the transgenic rat platform. | NMPA |
9.2. Leukemia
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Imatinib | Gleevec | 152459-95-5 | BCR-ABL; PDGFRA; c-Kit | Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM. | FDA; NMPA |
| Dasatinib | Sprycel | 302962-49-8 | PDGFRA D842V | Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. | FDA; NMPA |
| Nilotinib | Tasigna | 641571-10-0 | BCR-ABL; c-Kit | Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM. | FDA; NMPA |
| Bosutinib | Bosulif | 380843-75-4 | BCR-ABL | Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM, respectively. | FDA |
| Ponatinib | Iclusig | 943319-70-8 | BCR-ABL | Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively. | FDA |
| Olverembatinib | GZD824 | 1257628-77-5 | BCR-ABL | Olverembatinib potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50) values of 0.2 and 0.13 nM, respectively. | NMPA |
| Idelalisib | Zydelig | 870281-82-6 | Pl3K | Idelalisib is a kinase inhibitor. In combination with rituximab, it was used for the treatment of relapsed or refractory chronic lymphocytic leukemia (CLL). | FDA |
| Ibrutinib | Imbruvica | BTK | Ibrutinib is a small molecule drug that inhibits B-cell proliferation and survival by irreversibly binding the protein Bruton’s tyrosine kinase. | FDA; NMPA | |
| Orelabrutinib | InnoCare | 1655504-04-3 | BTK | Orelabrutinib is an orally administered, potent, irreversible and highly selective BTK inhibitor. | NMPA |
| Zanubrutinib | RPIIKINSA | 1691249-45-2 | BTK | Zanubrutinib is a potent and irreversible BTK inhibitor. | FDA; NMPA |
| Flumatinib | Xinfu | 895519-90-1 | PTK | Flumatinib is a multi-kinase inhibitor of c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2 nM, 307.6 nM and 2662 nM respectively. | NMPA |
| Venetoclax | Venclexta | 1257044-40-8 | BCL-2 | Venetoclax is a small-molecule inhibitor that has high selectivity for Bcl-2 (Ki < 0.01 nM in cell-free assays) over Mcl-1. | FDA |
| Polatuzumab vedotin-piiq | Polivy | CD79b | Polatuzumab vedotin-piiq is a first-in-class CD79b-directed antibody-drug conjugate with activity against dividing B cells. | FDA | |
| Rituximab | Rituxan | CD20 | Rituximab is a monoclonal antibody medication used to treat certain autoimmune diseases and types of cancer. | FDA | |
| Ofatumumab | Arzerra | CD20 | Ofatumumab is a fully human monoclonal antibody to CD20, which appears to inhibit early-stage B lymphocyte activation. | FDA | |
| Obinutuzumab | Gazyva | CD20 | Obinutuzumab is a humanized anti-CD20 monoclonal antibody as a cancer treatment. | FDA | |
| Gilteritinib | Xospata | 1254053-43-4 | FLT3 | Gilteritinib, also known as (ASP2215, is a potent FLT3/AXL inhibitor. | FDA; NMPA |
| Inotuzumab Ozogamicin | Besponsa | CD22 | Inotuzumab ozogamicin is an antibody-drug conjugate medication used to treat relapsed or refractory B-cell precursor acute lymphoblastic leukemia. | FDA; NMPA | |
| Gemtuzumab | Mylotarg | CD33 | Gemtuzumab is a type of targeted therapy called an antibody-drug conjugate. | FDA | |
| Blinatumomab | Blincyto | CD19/CD3 | Blinatumomab is a biopharmaceutical medication used as a second-line treatment for Philadelphia chromosome-negative relapsed or refractory acute lymphoblastic leukemia. | FDA; NMPA | |
| Ivosidenib | Tibsovo | 1448347-49-6 | IDH1 | Ivosidenib is an oral inhibitor that specifically inhibits a mutated form of IDH1 in the cytoplasm, which blocks the proliferation of tumor cells expressing IDH1. | FDA |
| Enasidenib | Idhifa | 1446502-11-9 | IDH2 | Enasidenib, aslo known as AG-221 and CC-90007, is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2). | FDA |
10. Other tumors
10.1. Neuroendocrine tumors
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Everolimus | Afinitor | 159351-69-6 | mTOR | Everolimus is an inhibitor of mammalian target of rapamycin (mTOR) with an immunosuppressive activity which is comparable to that of rapamycin. | FDA; NMPA |
| Sunitinib | SUTENT | 557795-19-4 | VEGFR-1,2,3 | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. | FDA; NMPA |
| Surufatinib | SULANDA | 1308672-74-3 | VEGFR-1,2,3; FGFR; CSF-1R | Surufatinib, an oral drug candidate, is a small molecule inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, and the fibroblast growth factor receptor type 1 (FGFR1). | NMPA |
10.2. Thymoma/Carcinoma
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Nivolumab | Opdivo | PD-1 | Nivolumab is a type of cancer treatment drug called an immunotherapy. It is a treatment for a number of different types of cancer. | FDA; NMPA | |
| lpilimumab | Yervoy | CTLA-4 | Ipilimumab is a human cytotoxic T-lymphocyte antigen 4 (CTLA-4) blocking antibody used to treat metastatic or unresectable melanoma. | FDA; NMPA | |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | Not Approved | |
| Sunitinib | SUTENT | 557795-19-4 | VEGFR-1,2,3 | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. | Not Approved |
| Everolimus | Afinitor | 159351-69-6 | mTOR | Everolimus is an inhibitor of mammalian target of rapamycin (mTOR) with an immunosuppressive activity which is comparable to that of rapamycin. | Not Approved |
10.3. Pan-tumor targeting and immune drugs
| Drug Name | Trade name | CAS | Target | Description | Approved Status |
| Larotrectinib | Vitrakvi | 1223403-58-4 | NRTK1/2/3 | Larotrectinib, also known as ARRY-470, is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC. | FDA |
| Entrectinib | Rozlytrek | 1108743-60-7 | NRTK1/2/3; ALK; ROS1 | Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. | FDA; MHLW |
| Pembrolizumab | Keytruda | PD-1 | Pembrolizumab is a type of immunotherapy. It stimulates the body’s immune system to fight cancer cells. | FDA | |
| Dostarlimab | Jemperli | PD-1 | Dostarlimab is a monoclonal antibody used as a medication for the treatment of endometrial cancer. | FDA | |
| Envafolimab | KN035 | PD-L1 | Jun 23, 2021 — Envafolimab is a novel, single-domain PD-L1 antibody that is administered by subcutaneous injection without the need for an adjuvant. | NMPA |
Globally, the burden of cancer is projected to increase by 50% in 2040 compared to 2020 due to an aging population, when the number of new cancer cases will reach nearly 30 million. This is most pronounced in countries undergoing social and economic transition. Integrating cancer prevention and treatment interventions into health plans will help reduce the future burden of cancer while driving the development of innovative medicines against cancer. The combination of prevention and treatment can better reduce the burden of cancer and protect people’s health.
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