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Substance Name: Larotrectinib [USAN:INN]
RN: 1223403-58-4
UNII: PF9462I9HX
InChIKey: NYNZQNWKBKUAII-KBXCAEBGSA-N

Note

  • A TRK kinase inhibitor.

    NCI: Trk inhibitor LOXO-101 An orally available, tropomyosin receptor kinase (Trk) inhibitor, with potential antineoplastic activity. Upon administration, LOXO-101 binds to Trk, thereby preventing 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. Trk, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival. (NCI Thesaurus)

Molecular Formula

  • C21-H22-F2-N6-O2

Molecular Weight

  • 428.4408
 

Classification Code

  • Treatment of TRK Positive Tumors
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Names and Synonyms

Name of Substance

  • Larotrectinib [USAN:INN]

Synonyms

  • 1-Pyrrolidinecarboxamide, N-(5-((2R)-2-(2,5-difluorophenyl)-1-pyrrolidinyl)pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxy-, (3S)-
  • ARRY 470
  • Larotrectinib
  • LOXO 101
  • LOXO-101
  • UNII-PF9462I9HX

Systematic Name

  • (3S)-N-(5-((2R)-2-(2,5-Difluorophenyl)pyrrolidin-1-yl)pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine- 1-carboxamide

Registry Numbers

CAS Registry Number

  • 1223403-58-4

FDA UNII

  • PF9462I9HX

System Generated Number

  • 1223403584

Structure Descriptors

InChI

1S/C21H22F2N6O2/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31)/t14-,18+/m0/s1

InChIKey

NYNZQNWKBKUAII-KBXCAEBGSA-N

Smiles

O[C@H]1CCN(C1)C(=O)Nc2cnn3ccc(nc23)N4CCC[C@@H]4c5cc(F)ccc5F