Astellas Initiates Phase 3 Study of Setidegrasib for Lung Cancer

Tokyo – Astellas Pharma Inc. has announced the dosing of the first patient in a Phase 3 study assessing setidegrasib, an investigational KRAS G12D-targeted protein degrader. The study is for patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) whose disease has progressed after initial platinum-based chemotherapy and checkpoint inhibitor therapy.

Lung cancer is the most common cancer worldwide and the leading cause of cancer-related death. Approximately 5% of NSCLC cases have a KRAS G12D mutation, for which there are currently no approved therapies. Patients whose disease progresses after initial treatment typically rely on standard options such as chemotherapy.

Setidegrasib is designed to degrade and eliminate the disease-driving KRAS G12D protein. Early clinical evidence published in March 2026 demonstrated antitumor activity and a manageable safety profile in patients with KRAS G12D-mutated solid tumors, supporting the drug's proposed mechanism of action.

The initiation of this Phase 3 study aligns with Astellas' corporate strategy to launch five or more Phase 3 or pivotal studies by fiscal year 2027. This marks the second Phase 3 study for setidegrasib within six months, following a similar study initiated for pancreatic cancer in April 2026.

Astellas will also present translational analyses from the Phase 1 study of setidegrasib at the AACR Conference on Pancreatic Cancer in September 2026, aiming to provide insights into mechanisms of response, resistance, and potential combination approaches for pancreatic cancer.