Mechanism of ActionLarotrectinib is an inhibitor of the tropomyosin receptor kinases (TRK), TRKA, TRKB, and TRKC. In a broad panel of purified enzyme assays, larotrectinib inhibited TRKA, TRKB, and TRKC with IC50 values between 5-11 nM. One other kinase TNK2 was inhibited at approximately 100-fold higher concentration. TRKA, B, and C are encoded by the genes NTRK1, NTRK2, and NTRK3.Chromosomal rearrangements involving in-frame fusions of these Reference ID: 4354324 genes with various partners can result in constitutively-activated chimeric TRK fusion proteins that can act as an oncogenic driver, promoting cell proliferation and survival in tumor cell lines. In in vitro and in vivo tumor models, larotrectinib demonstrated anti-tumor activity in cells with constitutive activation of TRK proteins resulting from gene fusions, deletion of a protein regulatory domain, or in cells with TRK protein overexpression. Larotrectinib had minimal activity in cell lines with point mutations in the TRKA kinase domain, including the clinically identified acquired resistance mutation, G595R. Point mutations in the TRKC kinase domain with clinically identified acquired resistance to larotrectinib include G623R, G696A, and F617L.
IndicationVITRAKVI is a kinase inhibitor indicated for the treatment of adult and pediatric patients with solid tumors that: • have a neurotrophic receptor tyrosine kinase (NTRK) gene fusion without a known acquired resistance mutation, • are metastatic or where surgical resection is likely to result in severe morbidity, and • have no satisfactory alternative treatments or that have progressed following treatment.
Dr. Reddy's Expertise
Headquartered in Hyderabad, India, Dr. Reddy's Laboratories is one of the leading Active Pharmaceutical Ingredients (API) manufacturers and suppliers globally for Larotrectinib API. Dr. Reddy's API business is a preferred partner to pharma companies across the US, Europe, Brazil, Latin America, Japan, China, Korea, Middle East and other emerging markets.
Dr. Reddy's API business thrives on the deep technical strengths established over the last 30+ years in the development and manufacture of complex APIs such as steroids, peptides, complex long chain molecules and highly potent APIs (HPAPIs / oncology drugs). This expertise is complemented by our prowess in intellectual property and regulatory affairs which helps us consistently meet and exceed regulatory standards. Dr. Reddy's Larotrectinib API is the outcome of the extensive expertise in R&D, IP, and Regulatory.
A key component in helping our customers be first to market is a responsive supply chain. We achieve this by making sure that all our facilities are operating efficiently and to the latest standards of quality, safety, and productivity. A strong interconnect between business and factories allows for a quick reaction to dynamic market changes, so that we can avert shortages and meet sudden surges in demand.
Please fill in the following form and we'll get back to you shortly
Products protected by valid patents are not offered for sale in countries where the sale of such products constitutes patent infringement. Availability may be restricted to certain markets or countries. Please Contact Us for more information on availability and product suitability.
All product information, including that with regard to active pharmaceutical ingredients (API), the indication, and possible mechanism(s) of action, is based on publicly available product label.