On September 24, 2026 Astellas Pharma Inc. (TSE: 4503, President and CEO: Naoki Okamura, "Astellas") reported that the first patient has been dosed in a Phase 3 study evaluating setidegrasib, a novel, investigational KRAS G12D-targeted protein degrader, versus docetaxel in people with KRAS G12D-mutated locally advanced (unresectable) or metastatic non-small cell lung cancer (NSCLC) whose disease has progressed on or after initial platinum-based chemotherapy and checkpoint inhibitor therapy (CPI).1

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Lung cancer is the most commonly diagnosed cancer and the leading cause of cancer-related death worldwide, with NSCLC accounting for approximately 80% of cases.2,3 Around 5% of people with NSCLC have a KRAS G12D mutation.4 Despite advances in targeted treatment for other molecularly defined forms of NSCLC, there are currently no therapies approved specifically for people with KRAS G12D-mutated NSCLC.3,5 Patients whose disease progresses on or after initial treatment currently rely on standard systemic options, such as chemotherapy.5

Setidegrasib is an investigational targeted protein degrader designed to degrade and eliminate the disease-driving KRAS G12D protein. By removing this protein, setidegrasib may help disrupt cancer cell signaling and destroy cancer cells.4 This Phase 3 study in previously treated NSCLC builds on early clinical evidence published in The New England Journal of Medicine in March 2026, which demonstrated antitumor activity and a manageable safety profile in patients with KRAS G12D-mutated solid tumors, supporting the proposed mechanism of action of setidegrasib.4

Hidenori Kitai, M.D., Ph.D., Department of Respiratory Medicine, Faculty of Medicine, Hokkaido University, Japan:
"For too long, patients with KRAS G12D-mutated non-small cell lung cancer have had limited treatment options after standard therapies. This Phase 3 study represents an important step forward for the field, helping to build the evidence needed to understand whether setidegrasib could offer a potential new approach for this molecularly defined patient population."

Tadaaki Taniguchi, M.D., Ph.D., Chief Research and Development Officer, Astellas:
"The initiation of this Phase 3 study in NSCLC, our second Phase 3 study of setidegrasib within six months, reflects continued progress in its clinical development. This study will help us understand how setidegrasib’s novel approach to degrading disease-driving KRAS G12D may help address unmet needs for patients with this type of NSCLC. We are grateful to the patients, investigators and study teams making this research possible."

Setidegrasib is Astellas’ lead investigational targeted protein degrader. Initiation of the Phase 3 study in previously treated patients with NSCLC supports Astellas’ Corporate Strategic Plan, with an ambition to initiate five or more Phase 3 or pivotal studies by fiscal year 2027. It follows the initiation of a Phase 3 study of setidegrasib in front-line pancreatic ductal adenocarcinoma (PDAC) in April 2026.6

To further inform the scientific understanding of setidegrasib and KRAS G12D-driven disease biology, Astellas will also present translational analyses from the Phase 1 study of setidegrasib in patients with KRAS G12D-mutated PDAC at the upcoming AACR (Free AACR Whitepaper) Conference on Pancreatic Cancer, September 25–28, 2026.7,8 The analyses will provide further insight into mechanisms of response, resistance and potential rational combination approaches in pancreatic cancer. The findings will be featured in both a proffered oral presentation and a poster presentation.*

(Press release, Astellas, SEP 24, 2026, View Source [SID1234671023])