Astellas Doses First Patient in Phase 3 Study of setidegrasib (ASP3082) for KRAS G12D-mutated Metastatic Pancreatic Ductal Adenocarcinoma
Astellas Pharma Inc. (TSE: 4503, President and CEO: Naoki Okamura, “Astellas”) today announced that the first patient has been successfully dosed in the Phase 3 registrational study evaluating setidegrasib (ASP3082) in combination with mFOLFIRINOX or NALIRIFOX as first-line treatment for patients with KRAS G12D-mutated metastatic pancreatic ductal adenocarcinoma (PDAC).
KRAS G12D mutations occur in approximately 40% of people with PDAC and remain associated with poor outcomes.1 There are currently no approved therapies that specifically target the KRAS G12D mutation.
Setidegrasib is an investigational KRAS G12D-targeted protein degrader, discovered through Astellas’ in-house research and development capabilities.2 It is designed to selectively bind mutant KRAS G12D proteins and an E3 ligase to trigger degradation of the disease-driving protein.3 Phase 1 data demonstrated KRAS G12D target degradation consistent with the proposed mechanism of action.4 Results from the open-label, two-part Phase 1 study have been published in The New England Journal of Medicine and can be accessed here.5
Tadaaki Taniguchi, M.D., Ph.D., Chief Research and Development Officer, Astellas:
“KRAS has been recognized for decades as a challenging oncogenic driver, with KRAS G12D representing an area of significant unmet need across multiple cancers. Successfully advancing a KRAS G12D-directed protein degrader into a Phase 3 study is an important milestone for Astellas, underscoring the value of strategic investment in our in-house expertise and capabilities to discover and develop our targeted protein degradation platform.”
The Phase 3, randomized, double-blind, placebo-controlled study is designed to evaluate the efficacy and safety of setidegrasib in combination with mFOLFIRINOX or NALIRIFOX as first-line treatment in participants with confirmed KRAS G12D-mutated metastatic PDAC.6 The primary endpoint is overall survival in this biomarker-defined population, with key secondary endpoints including progression-free survival and safety.6 The study plans to enroll more than 600 participants across multiple countries.6
About setidegrasib
Setidegrasib (ASP3082) is a selective protein degrader discovered through Astellas’ in-house research and development capabilities that targets mutated KRAS G12D, which is one of the most common KRAS mutation subtypes across tumors.7 Setidegrasib has been evaluated in a first-in-human, open label Phase 1 study in patients with metastatic or locally advanced unresectable solid tumors harboring a KRAS G12D mutation, including advanced pancreatic and non-small cell lung cancers.4,8 For more information about the Phase 1 study, visit clinicaltrials.gov with identifier NCT05382559. For more information about the Phase 3 study in PDAC, visit clinicaltrials.gov with identifier NCT07409272.
The safety and efficacy of setidegrasib is not established for the uses being considered. There is no guarantee that setidegrasib will receive regulatory approval and become commercially available for the uses being investigated.
About Astellas
Astellas is a global life sciences company committed to turning innovative science into value for patients. We provide transformative therapies in disease areas that include oncology, ophthalmology, urology, immunology and women’s health. Through our research and development programs, we are pioneering new healthcare solutions for diseases with high unmet medical need.
Source Link:https://newsroom.astellas.com/
