Preferred Label : Paltimatrectinib;
NCIt synonyms : Pan-TRK Inhibitor PBI-200;
NCIt definition : An orally bioavailable, brain-penetrant pan-tropomyosin-related-kinase (tyrosine receptor
kinase; TRK) inhibitor, with potential antineoplastic activity. Upon oral administration,
paltimatrectinib specifically targets and binds to TRKs, mutated TRKs and fusion proteins
containing sequences from neurotrophic tyrosine receptor kinase (NTRK) types 1 (NTRK1;
TrkA), 2 (NTRK2; TrkB), and 3 (NTRK3; TrkC). This inhibits neurotrophin-TRK interaction
and TRK activation, thereby preventing the activation of downstream signaling pathways
and resulting in both the induction of cellular apoptosis and the inhibition of cell
growth in tumors that overexpress TRK and/or express NTRK fusion proteins. TRK, a
family of receptor tyrosine kinases (RTKs) activated by neurotrophins, is encoded
by NTRK family genes. The expression of either mutated forms of, or fusion proteins
involving, NTRK family members results in uncontrolled TRK signaling, which plays
an important role in tumor cell growth, survival, invasion and treatment resistance.;
UNII : SP4MKH8Y5J;
CAS number : 2353522-15-1;
Molecule name : PBI-200; PBI 200;
NCI Metathesaurus CUI : CL1663452;
Origin ID : C180857;
UMLS CUI : C5556668;
Semantic type(s)
- concept_is_in_subset
- has_target
