Preferred Label : Selitrectinib;
NCIt synonyms : (13E,14E,22R,6R)-35-fluoro-6-methyl-7-aza-1(5,3)-pyrazolo[1,5-a]pyrimidina-3(3,2)-pyridina-2(1,2)-pyrrolidinacyclooctaphan-8-one;
NCIt related terms : TRK Inhibitor LOXO-195;
NCIt definition : An orally bioavailable, selective tropomyosin-related-kinase (tyrosine receptor kinase;
TRK) inhibitor, with potential antineoplastic activity. Upon oral administration,
LOXO-195 specifically targets and binds to TRK, including the fusion proteins containing
sequences from neurotrophic tyrosine receptor kinase (NTRK) types 1 (NTRK1), 2 (NTRK2),
and 3 (NTRK3). This prevents neurotrophin-TRK interaction and TRK activation, which
results in both the induction of cellular apoptosis and the inhibition of cell growth
in tumors that overexpress TRK and/or express NTRK fusion proteins. LOXO-195 targets
specific point mutations that occur after treatment with and result in acquired resistance
to another TRK inhibitor; therefore, LOXO-195 is able to overcome acquired resistance
to other TRK inhibitors. 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 and plays an important role in tumor cell growth and survival.;
UNII : 0J45910S3X;
InChIKey : OEBIHOVSAMBXIB-SJKOYZFVSA-N;
CAS number : 2097002-61-2;
Molecule name : LOXO 195; LOXO-195; BAY 2731954;
NCI Metathesaurus CUI : CL525677;
Origin ID : C138160;
UMLS CUI : C5139762;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
