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LOXO-101

LOXO-101 structure

CAS No:
1223403-58-4
Formula:
C21H22F2N6O2
Chemical Name:
LOXO-101
Synonyms:
LOXO-101;CS-2322;LOXO101;LOXO 101;LOXO-101 Larotrectinib;LOXO-101 (ARRY-470,Larotrectinib);LOXO-101,LAROTRECTINIB,ARRY-470;ARRY 470;(S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Larotrectinib (VITRAKVIR) is an orally administered, small molecule, highly-selective, tropomyosin receptor kinase (TRK) inhibitor that was developed by Loxo Oncology in collaboration with Bayer AG as a treatment for adult and paediatric patients whose cancers harbour neurotrophic receptor tyrosine kinase (NTRK) gene fusions.Larotrectinib is a highly selective, potent inhibitor of TRKA, TRKB and TRKC (in vitro 50% inhibitory constant 5–11 nmol/L), with minimal or no activity against other kinase and non-kinase targets [1, 2]. Inhibition of TRKs prevents TRK activation, resulting in both the induction of cellular apoptosis and the inhibition of cell growth in tumours that overexpress TRKs.

LOXO-101 is an inhibitor of the tropomyosin-related kinases TrkA, TrkB, and TrkC (IC50s = 2-20 nM). It is selective for TrkA, -B, and -C over a panel of 226 kinases at 1 μM. LOXO-101 inhibits the growth of CUTO-3.29, KM12, and MO-91 patient-derived cancer cell lines (IC50s = <100, <10, and <10 nM, respectively).In vivo, LOXO-101 (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.

Larotrectinib, also known as LOXO-101 and ARRY-470, is a small molecule that was designed to block the ATP-binding site of the TRKA, TRKB, and TRKC, serving as a highly specific and potent inhibitor of all of the three tropomyosin kinase receptors.

Class: receptor tyrosine kinase; Treatment: NTRK-altered solid tumors; Other name: ARRY-407, LOXO-101; Oral bioavailability = 25%; Elimination half-life = 2.9 h; Protein binding = 70%

LOXO-101 Basic Attributes

Molecular Weight：

428.44

Exact Mass：

428.44

Color/Form：

Yellow

Characteristics

PSA：

XLogP3：

3.0234

Appearance：

White to yellow solid

Density：

1.55±0.1 g/cm3(Predicted)

PKA：

8.41±0.40(Predicted)

Critical Temperature & Pressure：

LOXO-101 Use and Manufacturing

LOXO-101 is a drug used to treat adults and children with certain types of solid tumors that have spread or cannot be removed by surgery and have the NTRK gene fusion. It is also being studied in the treatment of other types of cancer.

Larotrectinib is a TRK Inhibitor (Tyrosine kinase inhibitor).

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