First patient dosing completed for KRAS G12D inhibitor ABSK141 On the morning of March 4th, Heyu -B (02256) announced that its subsidiary, Shanghai Heyu Biopharmaceutical Technology Co., Ltd., has successfully completed the first patient dosing in a Phase I/II clinical trial of its oral, highly effective, and selective small molecule KRAS G12D inhibitor, ABSK141, for patients with advanced solid tumors harboring KRAS G12D mutations. This progress marks a significant milestone for Heyu Pharmaceuticals in the field of KRAS-targeted therapy, and is expected to provide a transformative potential treatment option for patients with KRAS G12D-mutated solid tumors. 　　According to the announcement, KRAS is one of the most common oncogenes in human cancers, with G12D being the major mutation subtype, widely found in various solid tumors such as pancreatic ductal adenocarcinoma, colorectal cancer, and non-small cell lung cancer. Because G12D mutations lead to specific conformational changes in the KRAS protein, it has long been considered an “untreatable” target, and currently, no targeted therapies against KRAS G12D mutations have been approved globally. 　　The announcement indicates that the first patient dose was administered in an open-label Phase I/II clinical trial, which is expected to receive approval for a new drug clinical trial from the U.S. Food and Drug Administration and the China National Medical Products Administration in December 2025. ABSK141 is a novel oral small-molecule KRAS G12D inhibitor independently designed and developed by Heyu Pharmaceuticals. It selectively binds to the KRAS G12D mutant protein, blocking downstream signaling pathways and inhibiting tumor cell proliferation. Preclinical studies have shown that ABSK141 exhibits potentially best-in-class oral bioavailability in various animal models and demonstrates significant antitumor activity in multiple human tumor cell line xenograft models, including pancreatic ductal adenocarcinoma and colorectal cancer. 　　The announcement stated that Heyu Pharmaceuticals, established in April 2016, is a biopharmaceutical company focused on the field of oncology, headquartered in Shanghai, and dedicated to the discovery and development of innovative drugs.The company aims to address unmet medical needs in China and globally. Its founders and management team are all seasoned drug development experts with extensive R&D and management experience from leading multinational pharmaceutical companies. Since its inception, Heyu Pharmaceuticals has built a rich pipeline of innovative products, focusing on precision oncology and immuno-oncology field. 网址：https

March 4, 2026  Source: drugdu 27