Preferred Label : KRAS G12D Inhibitor RMC-9805;
NCIt synonyms : KRASG12D(ON) Inhibitor RMC-9805;
NCIt definition : An orally bioavailable covalent tri-complex inhibitor of the oncogenic KRAS substitution
mutation G12D, with potential antineoplastic activity. Upon oral administration, KRAS
G12D inhibitor RMC-9805 specifically targets and non-covalently binds to cyclophilin
A to form a non-covalent binary complex, which subsequently covalently and irreversibly
binds to the active GTP-bound form of KRAS G12D (KRASG12D(ON)). This prevents KRAS
G12D-mediated signaling and activation of downstream survival pathways. This causes
apoptosis in KRAS G12D-expressing tumor cells. In addition, inhibition of KRAS G12D
signaling by RMC-9805 abrogates the suppressive tumor microenvironment (TME) and enhances
an anti-tumor immune response which further leads to an inhibition of proliferation
of KRAS G12D-expressing tumor cells. KRAS, a member of the RAS family of oncogenes,
serves an important role in cell signaling, division and differentiation. Mutations
of KRAS may induce constitutive signal transduction leading to tumor cell proliferation,
invasion, and metastasis.;
Molecule name : RMC-9805; RMC 9805; RM-036; RM 036;
Origin ID : C201828;
concept_is_in_subset
- has_target
