RCZY-698

RCZY-698 is a novel, orally bioavailable, non-covalent tri-complex inhibitor specifically targeting the GTP-bound (ON) conformation of the KRASG12V mutant. Developed by Rongchang Pharmaceuticals, it functions by engaging cyclophilin A (CypA) to form a stable ternary complex with KRASG12V, thereby disrupting the interaction between the mutant protein and downstream effector proteins. This mechanism effectively suppresses key signaling cascades, such as the MAPK pathway, which are typically constitutively active in KRASG12V-driven cancers. In preclinical studies, RCZY-698 has demonstrated potent antiproliferative effects across various KRASG12V-mutant tumor cell lines and induced dose-dependent tumor regression in xenograft models of pancreatic, colorectal, and non-small cell lung cancers.