{"id":4594,"date":"2025-04-11T01:02:07","date_gmt":"2025-04-11T06:02:07","guid":{"rendered":"https:\/\/www.bocsci.com\/blog\/?p=4594"},"modified":"2025-04-11T01:32:58","modified_gmt":"2025-04-11T06:32:58","slug":"summary-of-globally-marketed-adc-drugs-with-lysine-conjugation","status":"publish","type":"post","link":"https:\/\/www.bocsci.com\/blog\/summary-of-globally-marketed-adc-drugs-with-lysine-conjugation\/","title":{"rendered":"Summary of Globally Marketed ADC Drugs with Lysine Conjugation"},"content":{"rendered":"

As of now, a total of 17 ADC drugs have been approved and marketed globally, among which 5 are conjugated via lysine residues.<\/p>\n

\n\n\n\n\n\n\n\n\n
\n Product Name <\/strong><\/td>\nCompany <\/strong><\/td>\nTarget <\/strong><\/td>\nDAR <\/strong><\/td>\nToxin <\/strong><\/td>\nLinker <\/strong><\/td>\nAntibody Type <\/strong><\/td>\nPayload Type <\/strong><\/td>\n<\/tr>\n
Mylotarg<\/td>\nPfizer<\/td>\nCD33<\/td>\n2~3<\/td>\nCalicheamicin<\/td>\nDisulfide
\nAcid-cleavable<\/td>\n		IgG4<\/td>\nDNA damaging agent<\/td>\n<\/tr>\n
Kadcyla<\/td>\nRoche<\/td>\nHer2<\/a><\/td>\n3.5<\/td>\nDM1<\/td>\nSMCC
\nNon-cleavable<\/td>\n		IgG1<\/td>\nMicrotubule inhibitor<\/td>\n<\/tr>\n
Besponsa<\/td>\nPfizer<\/td>\nCD22<\/td>\n5~7<\/td>\nCalicheamicin<\/td>\nDisulfide
\nAcid-cleavable<\/td>\n		IgG4<\/td>\nDNA damaging agent<\/td>\n<\/tr>\n
Akalux<\/td>\nRakuten<\/td>\nEGFR<\/a><\/td>\nNA<\/td>\nIRDye700DX<\/td>\nDirect conjugation \/ photo-cleavable linker
\nNon-cleavable<\/td>\n		IgG1<\/td>\nPhototoxic agent<\/td>\n<\/tr>\n
ELAHERE<\/td>\nImmunoGen<\/td>\nFR\u03b1<\/td>\n3.4<\/td>\nDM4<\/td>\nSulfo-SPDB
\nReducible<\/td>\n		IgG1<\/td>\nMicrotubule inhibitor<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<\/figure>\n

What is ado-trastuzumab emtansine? <\/strong><\/h2>\n

Ado-trastuzumab emtansine is an antibody-drug conjugate (ADC)<\/u><\/a> composed of trastuzumab<\/u><\/a> (an anti-HER2 IgG1 antibody) and the microtubule inhibitor DM1 (a maytansine derivative), linked via a thioether linker. The drug binds to the HER2 receptor through its antibody component, blocking activation of the HER2 signaling pathway and thereby inhibiting tumor cell proliferation. After internalization by tumor cells, DM1 is released in the intracellular environment, where it binds to tubulin, disrupts the microtubule network, and induces cell cycle arrest and apoptotic cell death. Ado-trastuzumab emtansine is primarily used for the treatment of HER2-positive breast cancer, including early-stage and metastatic breast cancer.<\/p>\n

\n\n\n\n\n\n\n\n\n\n\n\n\n\n
Item <\/strong><\/td>\nInformation <\/strong><\/td>\n<\/tr>\n
Product Name<\/td>\nKadcyla<\/td>\n<\/tr>\n
Generic Name<\/td>\nAdo-trastuzumab emtansine<\/td>\n<\/tr>\n
Manufacturer<\/td>\nRoche<\/td>\n<\/tr>\n
Indication<\/td>\nHER2-positive breast cancer (for treatment of patients with previously treated HER2-positive metastatic breast cancer)<\/td>\n<\/tr>\n
Target<\/td>\nHER2<\/td>\n<\/tr>\n
Dosage Form<\/td>\nLyophilized powder<\/td>\n<\/tr>\n
Strength<\/td>\n100 mg, 160 mg\/vial \u2013 20 mg\/mL<\/td>\n<\/tr>\n
Reconstitution Solution Type<\/td>\nBuffer: 10 mM succinic acid<\/td>\n<\/tr>\n
Stabilizer: 60 mg\/mL sucrose<\/td>\n<\/tr>\n
Surfactant: 0.2 mg\/mL polysorbate 20, pH 5.0<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<\/figure>\n

What is gemtuzumab ozogamicin? <\/strong><\/h2>\n

Gemtuzumab ozogamicin<\/u><\/a> is an antibody-drug conjugate (ADC) targeting CD33, composed of a humanized monoclonal antibody against CD33 (IgG4 \u03ba antibody hP67.6) covalently linked to the cytotoxic antitumor antibiotic calicheamicin (N-acetyl-\u03b3-calicheamicin) via a bifunctional linker. The drug binds to CD33-positive leukemia cells through its antibody component and is subsequently internalized into the cells. Inside the cell, the linker is cleaved by lysosomal enzymes, releasing calicheamicin, which induces DNA double-strand breaks, leading to cell cycle arrest and apoptosis. Gemtuzumab ozogamicin is used for the treatment of CD33-positive acute myeloid leukemia (AML), including both newly diagnosed and relapsed or refractory patients.<\/p>\n

\n\n\n\n\n\n\n\n\n\n\n\n\n\n
\n Item <\/strong><\/td>\nInformation <\/strong><\/td>\n<\/tr>\n
Product Name<\/td>\nMylotarg<\/td>\n<\/tr>\n
Generic Name<\/td>\nGemtuzumab ozogamicin<\/td>\n<\/tr>\n
Manufacturer<\/td>\nPfizer (USA)<\/td>\n<\/tr>\n
Indication<\/td>\nCD33-positive acute myeloid leukemia<\/td>\n<\/tr>\n
Target<\/td>\nCD33<\/td>\n<\/tr>\n
Dosage Form<\/td>\nLyophilized powder<\/td>\n<\/tr>\n
Strength<\/td>\n4.5 mg\/vial \u2013 1 mg\/mL<\/td>\n<\/tr>\n
Reconstitution Solution Type<\/td>\nBuffer: 5 mM sodium succinate<\/td>\n<\/tr>\n
Stabilizer: 14 mg\/mL sucrose, 8 mg\/mL polysorbate 40<\/td>\n<\/tr>\n
Surfactant: None, pH 7.4<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<\/figure>\n

What is inotuzumab ozogamicin? <\/strong><\/h2>\n

Inotuzumab ozogamicin<\/u><\/a> is a CD22-targeted ADC composed of a humanized monoclonal antibody (IgG4 \u03ba) against CD22, linked to the cytotoxic agent ozogamicin (N-acetyl-\u03b3-calicheamicin dimethyl hydrazide) via an AcBut linker. The drug binds to CD22-positive cells and is internalized. Within the lysosome, the linker is cleaved to release ozogamicin, which causes DNA damage leading to cell death. Inotuzumab ozogamicin is used to treat relapsed or refractory CD22-positive B-cell acute lymphoblastic leukemia (ALL).<\/p>\n

\n\n\n\n\n\n\n\n\n\n\n\n\n\n
Item <\/strong><\/td>\nDescription <\/strong><\/td>\n<\/tr>\n
Brand Name<\/td>\nBesponsa (Inotuzumab Ozogamicin)<\/td>\n<\/tr>\n
Generic Name<\/td>\nInotuzumab Ozogamicin<\/td>\n<\/tr>\n
Manufacturer<\/td>\nPfizer Inc. (Wyeth Pharma, a Pfizer subsidiary)<\/td>\n<\/tr>\n
Indication<\/td>\nBesponsa is indicated for the treatment of adult patients with relapsed or refractory B-cell precursor acute lymphoblastic leukemia (ALL).<\/td>\n<\/tr>\n
Target<\/td>\nCD22<\/td>\n<\/tr>\n
Form<\/td>\nLyophilized Powder<\/td>\n<\/tr>\n
Specification<\/td>\n1 mg\/vial, 0.25 mg\/mL<\/td>\n<\/tr>\n
Reconstitution Solution Type<\/td>\nBuffer: 18 mM tris(hydroxymethyl)aminomethane<\/td>\n<\/tr>\n
Stabilizer: 45 mg\/mL sucrose, 5 mg\/mL sodium chloride<\/td>\n<\/tr>\n
Surfactant: 0.1 mg\/mL polysorbate 80, pH 8.0<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<\/figure>\n

What is cetuximab sarotalocan? <\/strong><\/h2>\n

Cetuximab sarotalocan is an ADC composed of a monoclonal antibody (IgG1) targeting the epidermal growth factor receptor (EGFR), conjugated to the cytotoxic agent sarotalocan (a topoisomerase I inhibitor) via a cleavable linker. The drug binds to EGFR-positive tumor cells via the antibody portion and is subsequently internalized. Inside the cell, the linker is cleaved, releasing sarotalocan, which induces DNA damage and cell death by inhibiting topoisomerase I. Cetuximab sarotalocan is used to treat EGFR-positive solid tumors, including colorectal cancer and squamous cell carcinoma of the head and neck.<\/p>\n

\n\n\n\n\n\n\n\n\n\n\n\n\n\n
\n Item <\/strong><\/td>\nDescription <\/strong><\/td>\n<\/tr>\n
Brand Name<\/td>\nAkalux<\/td>\n<\/tr>\n
Generic Name<\/td>\nCetuximab Sarotalocan<\/td>\n<\/tr>\n
Manufacturer<\/td>\nRakuten<\/td>\n<\/tr>\n
Indication<\/td>\nColorectal Cancer, Head and Neck Cancer<\/td>\n<\/tr>\n
Target<\/td>\nEGFR<\/td>\n<\/tr>\n
Form<\/td>\nLyophilized Powder<\/td>\n<\/tr>\n
Specification<\/td>\n250 mg\/vial, 5 mg\/mL<\/td>\n<\/tr>\n
Reconstitution Solution Type<\/td>\nBuffer: 10 mM Phosphate<\/td>\n<\/tr>\n
Stabilizer: 90 mg\/mL Trehalose<\/td>\n<\/tr>\n
Surfactant: 0.2 mg\/mL Polysorbate 80, pH 7.1<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<\/figure>\n

What is mirvetuximab soravtansine-gynx? <\/strong><\/h2>\n

Mirvetuximab soravtansine-gynx is a folate receptor alpha (FR\u03b1)-targeted ADC composed of a monoclonal antibody against FR\u03b1, a cleavable linker, and the cytotoxic agent DM4, a microtubule inhibitor. The antibody is a chimeric IgG1, conjugated to DM4 via a cleavable linker. After binding to FR\u03b1, the ADC is internalized, and DM4 is released inside the cell through proteolytic cleavage. DM4 disrupts the microtubule network, leading to cell cycle arrest and apoptotic cell death. This drug is used to treat FR\u03b1-positive ovarian cancer, particularly in patients with platinum-resistant epithelial ovarian, fallopian tube, or primary peritoneal cancer.<\/p>\n

\n\n\n\n\n\n\n\n\n\n\n\n\n
Item <\/strong><\/td>\nDescription <\/strong><\/td>\n<\/tr>\n
Brand Name<\/td>\nElahere<\/td>\n<\/tr>\n
Generic Name<\/td>\nMirvetuximab Soravtansine-gynx<\/td>\n<\/tr>\n
Indication<\/td>\nEpithelial Ovarian Cancer, Fallopian Tube Cancer, or Primary Peritoneal Cancer<\/td>\n<\/tr>\n
Target<\/td>\nFolate Receptor\u03b1 (FR\u03b1)<\/td>\n<\/tr>\n
Form<\/td>\nInjection<\/td>\n<\/tr>\n
Specification<\/td>\n100 mg\/vial, 5 mg\/mL<\/td>\n<\/tr>\n
Reconstitution Solution Type<\/td>\nBuffer: 0.22 mg\/mL Glacial Acetic Acid, 0.53 mg\/mL Sodium Acetate<\/td>\n<\/tr>\n
Stabilizer: 90 mg\/mL Sucrose<\/td>\n<\/tr>\n
Surfactant: 0.1 mg\/mL Polysorbate 20, pH 5.0<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<\/figure>\n

ADCs Cytotoxin at BOC Sciences <\/strong><\/p>\n

\n
\n