Inhibitor

Lilly’s RET inhibitor LOXO-292 receives FDA priority review

Lilly’s RET inhibitor LOXO-292 receives FDA priority review

Lilly recently announced that its RET inhibitor, selpercatinib (loxo-292), has been granted priority review status by the U.S. FDA and is expected to accelerate its approval for the treatment of […]

PROTAC technology: Small molecule drug research and development mass murderer is coming! (Ⅱ)

PROTAC technology: Small molecule drug research and development mass murderer is coming! (Ⅱ)

Protein degradation targeted chimera (PROTAC) PROTAC technology began in 2001 that uses the ubiquitin-proteasome system (UPS), the intracellular “cleaner” for cleaning up denatured, mutated, or harmful proteins in cells. PROTAC, which uses […]

PROTAC technology: Small molecule drug research and development mass murderer is coming! (Ⅰ)

PROTAC technology: Small molecule drug research and development mass murderer is coming! (Ⅰ)

Preface Judging from the global drug sales trend in recent years, biological drugs have begun to become popular, while sales of small molecular drugs are declining. Innovations in research and […]

“Opportunities and Challenges” in the development of the HDACs drugs for cancers

“Opportunities and Challenges” in the development of the HDACs drugs for cancers

Despite the popularity in the development of histone deacelytase (HDAC) inhibitors, the indications of the five already approved HDAC inhibitor drugs on the market are limited to peripheral T-cell lymphoma […]

Osimertinib was approved for first-line treatment

Osimertinib was approved for first-line treatment

The third-generation EGFR inhibitor, Osimertinib (Tagrisso, AZD9291), was approved by the Chinese Food and Drug Administration (NMPA) recently for first-line treatment of patients with EGFR mutation-positive advanced or metastatic non-small cell lung […]

The first listed BTK inhibitor – Imbruvica

The first listed BTK inhibitor – Imbruvica

The sales of 2018 global small molecule drug apixaban replaced lenalidomide with a slight advantage, ranking first, and immediately after the two, it is the Imbruvica, the first listed BTK […]

Apixaban

Apixaban

In the past 2018, the global drug sales champion was still the macromolecular monoclonal antibody Humira (just short of $20 billion). The Top2 variety is a small molecular drug, but […]

Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors

Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors

The ADP-ribosyltranferase diphtheria toxin-like (ARTD) or poly-ADP-ribose polymerase (PARP) protein superfamily comprises 17 proteins that contain a common catalytic domain. Those that are catalytically active use β-NAD+ as an essential […]

Tyrosine Kinase Inhibitor Can Induced a Continuous Improving Effect on Idiopathic Pulmonary Fibrosis

Tyrosine Kinase Inhibitor Can Induced a Continuous Improving Effect on Idiopathic Pulmonary Fibrosis

The continuous effect of tyrosine kinase inhibitor on idiopathic pulmonary was newly found and the effect can last about two years to slow the progression of idiopathic pulmonary (IPF), which […]

Gerilizumab IL-6 is Put into Human Trial for Rheumatoid Arthritis

Gerilizumab IL-6 is Put into Human Trial for Rheumatoid Arthritis

Recently, a biotechnology company announced that gerilizumab IL-6 as a drug for rheumatoid arthritis was under trial in healthy people. Once the safety is proved in human trial, gerilizumab will […]