Preferred Label : Enbezotinib;
NCIt synonyms : RET/SRC Tyrosine Kinase Inhibitor TPX-0046; (3aR,11S,20aS)-7-Fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-17,19-metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one; 17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one,
7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aR,11S,20aS)-; RET/SRC Inhibitor TPX-0046;
NCIt definition : An orally bioavailable selective dual inhibitor of fusions and mutations involving
the proto-oncogene receptor tyrosine kinase rearranged during transfection (ret) and
the src family tyrosine kinases, with potential antineoplastic activity. Upon oral
administration, enbezotinib specifically targets and binds to ret mutants and ret-containing
fusion products. This results in an inhibition of cell growth of tumor cells that
exhibit increased ret activity. By inhibiting src kinase-mediated signaling and reducing
the src-initiated recruitment of multiple receptor tyrosine kinases involved in bypass
resistance, enbezotinib may be able to overcome tumor resistance which may increase
its therapeutic effect. Ret overexpression, activating mutations, and fusions result
in the upregulation and/or overactivation of ret tyrosine kinase activity in various
cancer cell types; dysregulation of ret activity plays a key role in the development
and progression of these cancers. Src tyrosine kinases are upregulated in many tumor
cells and play important roles in tumor cell proliferation, survival, migration, invasion
and angiogenesis. Src upregulation is seen in tumors with acquired resistance to RET
inhibitors.;
UNII : F6EVK907XR;
CAS number : 2359649-81-1;
Molecule name : TPX 0046; TPX-0046;
NCI Metathesaurus CUI : CL972435;
Origin ID : C167210;
UMLS CUI : C5908071;
Semantic type(s)
- concept_is_in_subset
- has_target
