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Vitrakvi (LAROTRECTINIB)

Bayer · FDA-approved approved Small molecule Quality 55/100

Vitrakvi works by blocking the activity of a specific protein called the nerve growth factor receptor.

Vitrakvi (larotrectinib) is a small molecule kinase inhibitor developed by LOXO Oncology Inc and currently owned by Bayer Healthcare. It targets the high affinity nerve growth factor receptor, specifically inhibiting NTRK fusion gene-positive advanced or recurrent solid tumors. Vitrakvi was FDA-approved in 2018 for its approved indications and is a patented medication with no generic manufacturers. Key safety considerations include its short half-life of 2.9 hours. As a targeted therapy, Vitrakvi is designed to selectively inhibit the growth of cancer cells with NTRK fusion genes.

At a glance

Generic nameLAROTRECTINIB
SponsorBayer
Drug classKinase Inhibitor [EPC]
TargetHigh affinity nerve growth factor receptor
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved
First approval2018

Mechanism of action

Larotrectinib is an inhibitor of the tropomyosin receptor kinases (TRK), TRKA, TRKB, and TRKC. In 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 are encoded by the genes NTRK1, NTRK2, and NTRK3. Chromosomal rearrangements involving in-frame fusions of these 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 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, incl

Approved indications

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Patents

PatentExpiryType

Primary sources

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SourceUsed for
FDA labelMechanism, indications, dosing, boxed warnings, drug interactions
ClinicalTrials.govTrial enrolment, design, endpoints, results
FDA Orange BookPatents + exclusivity

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