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    Larotrectinib

    From Mdwiki - Reading time: 9 min
    Larotrectinib
    Names
    Trade namesVitrakvi
    Other namesLOXO-101, ARRY-470
    • (3S)-N-{5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl}-3-hydroxypyrrolidine-1-carboxamide
    Clinical data
    Drug classTyrosine kinase inhibitor[1]
    Main usesCancer[2]
    Side effectsLiver problems, low red blood cells, muscle pain, tiredness, low white blood cells, diarrhea, nausea, fever[3]
    Pregnancy
    category
    • AU: D
    Routes of
    use    		By mouth
    Typical dose100 mg BID[4]
    External links
    AHFS/Drugs.comMonograph
    MedlinePlusa619006
    Legal
    License data
    Legal status
    • AU: S4 (Prescription only)
    • US: ℞-only
    • EU: Rx-only
    Chemical and physical data
    FormulaC21H22F2N6O2
    Molar mass428.444 g·mol−1
    3D model (JSmol)
    • O[C@H]1CCN(C1)C(=O)Nc2cnn3ccc(nc23)N4CCC[C@@H]4c5cc(F)ccc5F
    • 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, sold under the brand name Vitrakvi, is a medication used to treat cancer.[2][3] Specifically it is used for cases that have a neurotrophic receptor tyrosine kinase (NTRK) gene fusion.[3] It is taken by mouth.[1]

    Common side effects include liver problems, low red blood cells, muscle pain, tiredness, low white blood cells, diarrhea, nausea, and fever.[3] Other side effects may include numbness, tremor, and delirium.[1] Use in pregnancy may harm the baby.[3] It is a tyrosine kinase inhibitor of TrkA, TrkB, and TrkC.[1]

    Larotrectinib was approved for medical use in the United States in 2018, Europe in 2019, and Australia in 2020.[1][5][2] In the United Kingdom it costs the NHS about £15,000 a month as of 2021.[4] In the United States this amount is about 34,000 USD.[6]

    Medical uses[edit | edit source]

    In two thirds of people it decreased the size of their cancer to less than half.[5]

    Dosage[edit | edit source]

    It is generally taken at a dose of 100 mg twice per day.[4]

    History[edit | edit source]

    It was discovered by Array BioPharma and licensed to Loxo Oncology in 2013. Larotrectinib was initially 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.[7] Some clinical trial results were announced in 2017.[8]

    Larotrectinib was the first drug to be specifically developed and approved to treat any cancer containing certain mutations, as opposed to cancers of specific tissues (i.e., the approval is "tissue agnostic"). Several earlier drugs, including pembrolizumab, were eventually approved by the FDA for treatment of specific mutations independent of the type of cancer, but those drugs had been initially developed for specific cancer types.[9] The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[10]

    References[edit | edit source]

    1. ↑ 1.0 1.1 1.2 1.3 1.4 "Larotrectinib Monograph for Professionals". Drugs.com. Archived from the original on 21 January 2021. Retrieved 21 November 2021.
    2. ↑ 2.0 2.1 2.2 "Vitrakvi". Therapeutic Goods Administration (TGA). 16 September 2020. Archived from the original on 19 September 2020. Retrieved 22 September 2020.
    3. ↑ 3.0 3.1 3.2 3.3 3.4 "Vitrakvi- larotrectinib capsule Vitrakvi- larotrectinib solution, concentrate". DailyMed. 26 July 2019. Archived from the original on 7 April 2021. Retrieved 22 September 2020.
    4. ↑ 4.0 4.1 4.2 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1031. ISBN 978-0857114105.
    5. ↑ 5.0 5.1 "Vitrakvi EPAR". European Medicines Agency (EMA). 23 July 2019. Archived from the original on 2 October 2020. Retrieved 22 September 2020.
    6. ↑ "Vitrakvi Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 21 April 2021. Retrieved 21 November 2021.
    7. ↑ "Larotrectinib". AdisInsight. Archived from the original on 12 March 2018. Retrieved 31 January 2017.
    8. ↑ "Novel Agent Shows Antitumor Activity in TRK-Fusion Cancers. June 2017". Archived from the original on 2021-01-24. Retrieved 2021-08-16.
    9. ↑ Dun L (27 November 2018). "FDA approves a new cancer drug targeted to genetic mutation, not cancer type". NBC. Archived from the original on 2 December 2018. Retrieved 3 Dec 2018.
    10. ↑ New Drug Therapy Approvals 2018 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2019. Archived from the original on 17 September 2020. Retrieved 16 September 2020.

    External links[edit | edit source]

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