Partner:  

Mechanism of Action: small molecule inhibitors targetting SHP2

Indication: Oncology

Discovery: In January 2021 Astex and Taiho announced that they had extended their strategic oncology collaboration with Merck & Co., Inc., known as MSD outside the United States and Canada, by granting an exclusive license to Astex and Taiho’s joint small-molecule drug discovery program targeting SHP2.

An option for MSD to acquire the exclusive license to the Astex-Taiho SHP2 program was included as part of the strategic oncology collaboration between MSD, Astex and Taiho, announced in January 2020. The collaboration focuses on the discovery and development of small molecule inhibitors against several drug targets, including the KRAS oncogene, which are currently being investigated for the treatment of cancer.

SHP2, a dephosphorylating enzyme, is a signaling molecule which regulates various cellular processes including cell proliferation and differentiation, and acts as a regulator in the activation of the RAS signaling pathway such as KRAS.

In exchange for providing MSD with an exclusive global license to their small molecule SHP2 inhibitor candidates, Taiho and Astex will receive an option-exercise fee payment and will be eligible to receive further undisclosed payments contingent upon the achievement of clinical, regulatory and sales milestones for SHP2 products, as well as tiered royalties on sales. MSD will be solely responsible for funding all further research and development and will be responsible for commercialization of SHP2 products globally. Taiho has retained co-commercialization rights in Japan and an option to promote SHP2 products in specific areas of Southeast Asia.

MK-0472 is currently being evaluated in a Phase 1 study (NCT05853367) to assess the efficacy, safety, and tolerability of MK-0472 administered as monotherapy and in combination with pembrolizumab (MK-3475) or MK-1084 in participants with histologically or cytologically confirmed diagnosis of advanced/metastatic solid tumors. (Study Details | Study of MK-0472 in Participants With Advanced/Metastatic Solid Tumors (MK-0472-001) | ClinicalTrials.gov).