|Pronunciation||Vismodegib // VIS-moh-DEG-ib|
Erivedge // ERR-i-vej
|Other names||GDC-0449, RG-3616|
|Drug class||Hedgehog pathway inhibitor|
|Main uses||Basal-cell cancer (BCC)|
|Side effects||Hair loss, tiredness, nausea, muscle spasms|
|Interactions||St John’s wort|
|By mouth (capsules)|
|Typical dose||150 mg once daily|
|Metabolism||<2% metabolised by CYP2C9, CYP3A4, CYP3A5|
|Elimination half-life||4 days (continuous use),|
12 days (single dose)
|Excretion||Fecal (82%), Urinary (4.4%)|
|Chemical and physical data|
|Molar mass||421.29 g·mol−1|
|3D model (JSmol)|
Vismodegib, sold under the brand name Erivedge, is a medication used to treat basal-cell cancer (BCC). Specifically it is used in those in who the cancer has spread or has recurred and cannot be treated by other methods. It is taken by mouth.
Common side effects include hair loss, tiredness, nausea, and muscle spasms. Use during pregnancy may harm the baby. Effective birth control is recommended for both men and women. It is a hedgehog pathway inhibitor.
Vismodegib was approved for medical use in the United States in 2012 and Europe in 2013. In the United States it costs about 12,300 USD per month as of 2021 and is only available through specialty pharmacies. In the United Kingdom this amount costs the NHS about £6,300.
It is taken at a dose of 150 mg once per day.
Common side 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.
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.
- Cyclopamine, a naturally occurring SMO antagonist
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- FDA Professional Drug Information
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- "Vismodegib (GDC-0449) Smoothened Inhibitor - BioOncology".
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