Preferred Label : Zoldonrasib;
NCIt synonyms : KRASG12D(ON) Inhibitor RMC-9805; KRAS G12D 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, zoldonrasib
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 zoldonrasib 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.;
UNII : XJ52BWK3XE;
CAS number : 3034802-05-3;
Molecule name : RMC-9805; RMC 9805; RM-036; RM 036;
NCI Metathesaurus CUI : CL1920701;
Origin ID : C201828;
UMLS CUI : C5907933;
Semantic type(s)
- concept_is_in_subset
- has_target
