Astellas Submits IND Application in China for ASP3082, the World’s First KRAS G12D Degrader

On May 22, the CDE website showed that Astellas' globally first-in-class new drug ASP3082 has applied for clinical trials in China.

RAS is a common family of mutated genes in cancer, among which KRAS mutations are the most prevalent, accounting for about 85%. ASP3082 is a highly efficient and selective KRAS G12D protein degrader (PROTAC) developed by Astellas. Preclinical data show that ASP3082 can effectively degrade KRAS G12D protein, significantly inhibit extracellular signal-regulated kinase phosphorylation and its downstream genes, and effectively induce the cleavage of caspase-3.

In multiple xenograft mouse models carrying the KRAS G12D mutation, ASP3082 also demonstrated broad anti-tumor activity, accompanied by a reduction in the levels of the KRAS G12D mutant protein.

ASP3082 is currently the only KRAS G12D degrader to have entered the clinical stage. It can be said that Astellas has gained a speed advantage in the race for KRAS G12D-targeted drugs. However, it is regrettable that ASP3082 still requires intravenous administration, while MRTX1133, a small-molecule drug targeting KRAS G12D developed by Mirati Therapeutics, can be administered orally, offering greater advantages in improving patient compliance. In addition, Hengrui Medicine has also developed an injectable KRAS G12D-targeted drug, HRS-4642, which has already entered clinical research (CTR20222279).

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