daraxonrasib

An orally bioavailable inhibitor of the active, guanosine triphosphate (GTP)-bound form of both wild type and mutant variants of the RAS isoforms, including HRAS, NRAS and KRAS, with potential antineoplastic activity. Upon oral administration, daraxonrasib binds to an intracellular chaperone protein, cyclophilin A (CypA). The resulting inhibitory binary complex binds to active, GTP-bound RAS to form a tri-complex. This tri-complex inhibits RAS-dependent signaling and inhibits the proliferation of tumor cells in which RAS is overexpressed and/or mutated. RAS plays an important role in cell signaling, division and differentiation. Mutations of RAS may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.