Pan-KRAS Inhibitor AMG 410

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable, macrocyclic, non-covalent inhibitor of both the active, guanosine triphosphate (GTP)-bound (ON) form and the inactive, guanosine diphosphate (GDP)-bound (OFF) form of multiple oncogenic KRAS substitution mutations, including KRAS G12D, G12V, G12C, and G13D, as well as wild-type (WT) KRAS, with potential antineoplastic activity. Upon oral administration, pan-KRAS inhibitor AMG 410 selectively targets and reversibly binds to KRAS, thereby inhibiting KRAS-dependent signaling. This inhibits the growth and survival of KRAS-overexpressing and mutated tumor cells. KRAS, a member of the RAS family of oncogenes, plays an important role in cell signaling, division and differentiation. Mutations of KRAS may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.

**Synonyms:** - AMG 410 - AMG-410 - AMG410 - GTP-/GDP-bound State KRAS Inhibitor AMG 410 - KRAS Inhibitor AMG 410 - Pan-KRAS Dual-state Inhibitor AMG 410 - Pan-KRAS ON/OFF Inhibitor AMG 410