ACE-16229210

ACE-16229210 is a highly potent and selective small molecule inhibitor of fibroblast growth factor receptor 2 (FGFR2), currently being developed by Acerand Therapeutics for the treatment of solid tumors. It is designed to selectively target FGFR2-driven oncogenic alterations, such as fusions, amplifications, and mutations, while sparing other FGFR isoforms (FGFR1, FGFR3, and FGFR4) to minimize off-target toxicities like hyperphosphatemia and diarrhea. Preclinical studies have demonstrated that ACE-16229210 maintains activity against a broad spectrum of FGFR2 alterations, including gatekeeper and molecular brake mutations, and has shown significant antitumor efficacy in models of gastric, breast, ovarian, and endometrial cancers. The drug candidate is currently in the IND-enabling stage of development.

Other names

Acerand Therapeutics FGFR2 inhibitorSelective FGFR2 Inhibitor