Trade names Erivedge Routes of
administration By mouth (capsules) Molar mass 421.3 g/mol Formula C19H14Cl2N2O3S ATC code L01XX43 (WHO) | AHFS/Drugs.com Monograph Protein binding >99% Bioavailability 31.8% Pronunciation VIS-moe-DEG-ib | |
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Pregnancy
category AU: X (High risk)
US: D (Evidence of risk) Legal status AU: S4 (Prescription only)
CA: ℞-only
UK: POM (Prescription only)
US: ℞-only License data EU EMA: Erivedge; US FDA: Vismodegib | ||
Vismodegib shrinks tumors in metastatic basal cell carcinoma patients
Vismodegib (trade name Erivedge EH-rih-vej) is a drug 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, which is headquartered at South San Francisco, California, USA.
Contents
Indication
Vismodegib is indicated for patients 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 adverse effects included gastrointestinal disorders (nausea, vomiting, diarrhoea, constipation), muscle spasms, fatigue, hair loss, and dysgeusia (distortion of the sense of taste). The effects were mostly mild to moderate.