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| Pronunciation | /ˌvɪsmoʊˈdɛɡɪb/ VIS-moh-DEG-ib |
| Trade names | Erivedge |
| Other names | GDC-0449, RG-3616 |
| AHFS/Drugs.com | Monograph |
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| Routes of administration | By mouth |
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| 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%) |
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| ECHA InfoCard | 100.234.019  |
| Chemical and physical data | |
| Formula | C19H14Cl2N2O3S |
| Molar mass | 421.29 g·mol−1 |
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Vismodegib, sold under the brand name Erivedge, is a medication used for the treatment of basal-cell carcinoma (BCC).[3] 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.[4] 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[update].[5] The drug was developed by the biotechnology/pharmaceutical company Genentech.[4]
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.[4][6]
The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the Hedgehog signaling pathway.[5] SMO inhibition causes the transcription factors GLI1 and GLI2 to remain inactive, which prevents the expression of tumor mediating genes within the hedgehog pathway.[7] This pathway is pathogenetically relevant in more than 90% of basal-cell carcinomas.[8]
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).[3]
Vismodegib has undergone several promising phase I and phase II clinical trials for its use in treating medulloblastoma.[9]
