QTX3034

QTX3034 is a non-covalent, potent, orally bioavailable, and allosteric small molecule inhibitor that targets multiple forms of mutant GTPase KRas proteins, with a preference for the G12D variant. It binds to GDP-bound forms of both mutant and wild-type GTPase KRas with subnanomolar affinity, allosterically inhibiting their conversion to the active state. This inhibition blocks downstream GTPase KRas-dependent signaling pathways (such as MAPK), suppressing tumor cell proliferation and inducing apoptosis in cancers harboring GTPase KRas mutations. Preclinical studies have shown significant anti-tumor activity across various models—including pancreatic and colorectal cancer xenografts—and evidence of brain penetration. QTX3034 is being evaluated in Phase 1 clinical trials as monotherapy and in combination with EGFR inhibitors (e.g., cetuximab) for patients with advanced solid tumors carrying the KRAS G12D mutation[1][2][5][6][8].

Other names

KRAS mutant inhibitor QTX3034