Vismodegib, sold under the brand name Erivedge, is a medication used for the treatment of basal-cell carcinoma (BCC).
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
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
