Vismodegib
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| Systematic (IUPAC) name | |
| 2-Chloro-N-(4-chloro-3-pyridin-2-ylphenyl)-4-methylsulfonylbenzamide | |
| Clinical data | |
| Trade names | Erivedge |
| Licence data | US FDA:link |
| Pregnancy cat. | D (US) |
| Legal status | ℞-only (US) |
| Routes | Oral |
| Identifiers | |
| ATC code | L01XX43 |
| PubChem | CID 24776445 |
| UNII | 25X868M3DS |
| ChEBI | CHEBI:66903  |
| Synonyms | GDC-0449, RG-3616 |
| Chemical data | |
| Formula | C19H14Cl2N2O3S |
| Mol. mass | 421.30 g/mol |
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Vismodegib (trade name Erivedge) 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.[1] 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].[2] The drug was developed by the biotechnology / pharmaceutical company Genentech, which is headquartered at South San Francisco, California, USA.
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Indication [edit]
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.[3]
Mechanism of action [edit]
The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway.[2] SMO inhibition causes the transcription factors GLI1 and GLI2 to remain inactive, which prevents the expression of tumor mediating genes within the hedgehog pathway.[4] This pathway is pathogenetically relevant in more than 90% of basal-cell carcinomas.[5]
See also [edit]
- Cyclopamine, a naturally occurring SMO antagonist
References [edit]
- ^ "Vismodegib, First Hedgehog Inhibitor, Approved for BCC Patients".
- ^ a b Molecule of the Month. June 2011.
- ^ "FDA approves Erivedge (vismodegib) capsule, the first medicine for adults with advanced basal cell carcinoma".
- ^ "Vismodegib (GDC-0449) Smoothened Inhibitor - BioOncology".
- ^ H. Spreitzer (4 July 2011). "Neue Wirkstoffe – Vismodegib". Österreichische Apothekerzeitung (in German) (14/2011): 10.
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