Larotrectinib

Larotrectinib
Identifiers
	IUPAC name (3S)-N-{5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl}-3-hydroxypyrrolidine-1-carboxamide;
CAS Number	1223403-58-4;
ChemSpider	44210503;
UNII	PF9462I9HX;
Chemical and physical data
3D model (JSmol)	Interactive image;
	SMILES O[C@H]1CCN(C1)C(=O)Nc2cnn3ccc(nc23)N4CCC[C@@H]4c5cc(F)ccc5F;
	InChI 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; Key:NYNZQNWKBKUAII-KBXCAEBGSA-N;

Larotrectinib (LOXO-101, ARRY-470) is an experimental drug for the treatment of cancer.^[1] It is an inhibitor of tropomyosin kinase receptors TrkA, TrkB, and TrkC. It was discovered by Array BioPharma and licensed to Loxo Oncology in 2013.

Larotrectinib was awarded orphan drug status in 2015 for soft tissue sarcoma and breakthrough therapy designation in 2016 for the treatment of metastatic solid tumors with NTRK fusion.^[2]

Phase II clinical trials evaluating the drug for efficacy and safety in treating several types of solid tumors are ongoing.^[3]

Some clinical trial results were announced in 2017.^[4]

References

↑ "STATEMENT ON A NONPROPRIETARY NAME ADOPTED BY THE USAN COUNCIL" (PDF). ama-assn.org. October 26, 2016.
↑ "Larotrectinib". AdisInsight. Retrieved 31 January 2017.
↑ Study of LOXO-101 (Larotrectinib) in Subjects With NTRK Fusion Positive Solid Tumors (NAVIGATE)
↑ Novel Agent Shows Antitumor Activity in TRK-Fusion Cancers. June 2017

External links

Larotrectinib - AdisInsight

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[1] "STATEMENT ON A NONPROPRIETARY NAME ADOPTED BY THE USAN COUNCIL" (PDF). ama-assn.org. October 26, 2016.

[adis-2] "Larotrectinib". AdisInsight. Retrieved 31 January 2017.

[3] Study of LOXO-101 (Larotrectinib) in Subjects With NTRK Fusion Positive Solid Tumors (NAVIGATE)

[4] Novel Agent Shows Antitumor Activity in TRK-Fusion Cancers. June 2017

Identifiers

IUPAC name (3S)-N-{5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl}-3-hydroxypyrrolidine-1-carboxamide
CAS Number	1223403-58-4
ChemSpider	44210503
UNII	PF9462I9HX
Chemical and physical data
3D model (JSmol)	Interactive image
SMILES O[C@H]1CCN(C1)C(=O)Nc2cnn3ccc(nc23)N4CCC[C@@H]4c5cc(F)ccc5F
InChI 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 Key:NYNZQNWKBKUAII-KBXCAEBGSA-N