Preferred Label : Zanzalintinib Fumarate;
NCIt definition : The fumarate salt form of zanzalintinib, an orally bioavailable inhibitor of the receptor
tyrosine kinases (RTKs) hepatocyte growth factor receptor (c-Met; HGFR), vascular
endothelial growth factor receptor type 2 (VEGFR2), AXL and MER, with potential anti-angiogenesis
and antineoplastic activities. Upon oral administration, zanzalintinib targets and
binds to c-Met, VEGFR2, AXL and MER, and prevents their RTK activity. This blocks
c-Met/VEGFR2/AXL/MER-mediated signal transduction pathways, and inhibits the proliferation
and migration of c-Met-, VEGFR2-, AXL- and MER-overexpressing tumor cells. c-Met,
overexpressed in many tumor cell types, plays a critical role in tumor formation,
proliferation, invasion and metastasis, and contributes to tumor resistance. VEGFR2,
overexpressed in certain tumor types, plays an essential role in angiogenesis and
the proliferation, survival, migration and differentiation of endothelial cells. AXL
and MER, both members of the TAM (Tyro3, Axl and Mer) family of RTKs, are overexpressed
by many tumor cell types. They play key roles in tumor cell proliferation, survival,
invasion, angiogenesis and metastasis, and their expression is associated with enhanced
immunosuppression, drug resistance and poor prognosis.;
UNII : I793JC4077;
CAS number : 2444285-59-8;
NCI Metathesaurus CUI : CL1922247;
Origin ID : C203118;
UMLS CUI : C5909002;
Semantic type(s)
- concept_is_in_subset
- has_free_acid_or_base_form
- is_salt_form_of
