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Genentech
Vismodegib
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    Vismodegib

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    Vismodegib
    Vismodegib2DACS.svg
    Clinical data
    Pronunciation /ˌvɪsmoʊˈdɛɡɪb/
    VIS-moh-DEG-ib
    Trade names Erivedge
    Other names GDC-0449, RG-3616
    AHFS/Drugs.com Monograph
    License data
    Pregnancy
    category
    • AU: X (High risk)
    Routes of
    administration    		 By mouth
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Bioavailability 31.8%
    Protein binding >99%
    Metabolism <2% metabolised by CYP2C9, CYP3A4, CYP3A5
    Elimination half-life 4 days (continuous use),
    12 days (single dose)
    Excretion Fecal (82%), Urinary (4.4%)
    Identifiers
    • 2-Chloro-N-(4-chloro-3-pyridin-2-ylphenyl)-4-methylsulfonylbenzamide
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard 100.234.019
    Chemical and physical data
    Formula C19H14Cl2N2O3S
    Molar mass 421.29 g·mol−1
    3D model (JSmol)
    • CS(=O)(=O)C1=CC(=C(C=C1)C(=O)NC2=CC(=C(C=C2)Cl)C3=CC=CC=N3)Cl
    • InChI=1S/C19H14Cl2N2O3S/c1-27(25,26)13-6-7-14(17(21)11-13)19(24)23-12-5-8-16(20)15(10-12)18-4-2-3-9-22-18/h2-11H,1H3,(H,23,24)
    • Key:BPQMGSKTAYIVFO-UHFFFAOYSA-N

    Vismodegib, sold under the brand name Erivedge, is a medication used for the treatment of basal-cell carcinoma (BCC). The approval of vismodegib on January 30, 2012, represents the first Hedgehog signaling pathway targeting agent to gain U.S. Food and Drug Administration (FDA) approval. The drug is also undergoing clinical trials for metastatic colorectal cancer, small-cell lung cancer, advanced stomach cancer, pancreatic cancer, medulloblastoma and chondrosarcoma as of June 2011. The drug was developed by the biotechnology/pharmaceutical company Genentech.

    Indication

    Vismodegib is indicated for people with basal-cell carcinoma (BCC) which has metastasized to other parts of the body, relapsed after surgery, or cannot be treated with surgery or radiation.

    Mechanism of action

    The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the Hedgehog signaling pathway. SMO inhibition causes the transcription factors GLI1 and GLI2 to remain inactive, which prevents the expression of tumor mediating genes within the hedgehog pathway. This pathway is pathogenetically relevant in more than 90% of basal-cell carcinomas.

    Side effects

    In clinical trials, common side effects included gastrointestinal disorders (nausea, vomiting, diarrhoea, constipation), muscle spasms, fatigue, hair loss, and dysgeusia (distortion of the sense of taste).

    Development

    Vismodegib has undergone several promising phase I and phase II clinical trials for its use in treating medulloblastoma.

    Further reading

    External links

    • "Vismodegib". Drug Information Portal. U.S. National Library of Medicine.

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