Partner:  

Mechanism of Action: small molecule inhibitors against several targets including the KRAS oncogene

Indication: Oncology

Collaborative program: In January 2020 Astex Pharmaceuticals announced that it had entered into an exclusive worldwide research collaboration and license agreement with Merck, known as MSD outside the United States and Canada, and Taiho Pharmaceutical Co, Ltd., to develop small molecule inhibitors against several drug targets, including the KRAS oncogene, which are currently being investigated for the treatment of cancer.

Under the collaboration, Merck, Taiho and Astex will combine preclinical candidates and their data with knowledge and expertise from their respective research programs. Merck will fund research and development and will be responsible for commercialization of products globally. Taiho has retained co-commercialization rights in Japan and an option to promote in specific areas of South East Asia. In April 2024, Merck announced that it had initiated a Phase 3 clinical trial of MK-1084, an investigational oral KRAS G12C inhibitor, in combination with KEYTRUDA^® (pembrolizumab) for first-line treatment of certain patients with metastatic non-small cell lung cancer.

Mutations in KRAS are among the most prevalent mutations found in cancer, occurring with high frequency in non-small cell lung cancer, pancreatic, urogenital and colorectal cancers.

Prescribing and safety information for Keytruda^® is available at https://www.keytruda.com/.

Clinical status
MK-1084, an investigational oral KRAS G12C inhibitor, is currently being evaluated by Merck in Phase III trials.