Vemurafenib
Other name
-
International/Other brands
Zelboraf
Groups
Approved
Structure
Prescription products
| Name | Dosage | Strength | Route | Labeller |
|---|---|---|---|---|
| Zelboraf | Tablet | 240 mg | Oral | Hoffmann La Roche |
| Zelboraf | Tablet, film coated | 240 mg/1 | Oral | Genentech, Inc. |
| Zelboraf | Tablet, film coated | 240 mg | Oral | Roche Registration Limited |
Target
Description
Vemurafenib is a competitive kinase inhibitor with activity against BRAF kinase with mutations like V600E. It exerts its function by binding to the ATP-binding domain of the mutant BRAF.Vemurafenib was co-developed by Roche and Plexxikon and it obtained its FDA approval on August 17, 2011, under the company Hoffmann La Roche. After approval, Roche in collaboration with Genentech launched a broad development program.
Indications
Metastatic Melanoma; Unresectable Melanoma; Refractory Erdheim-Chester disease; Refractory Non-small cell lung cancer
Other indications
-
Mechaism of action
-
Absorption
Vemurafenib is well absorbed after oral administration. Peak concentrations are reached in 3 hours when an oral dose of 960 mg twice daily for 15 days has been given to patients. In the same conditions, Vemurafenib presents a Cmax of 62 mcg/ml and AUC of 601 mcg h/ml.[FDA Label] It is unknown how food affects the absorption of vemurafenib. It presents an accumulation ratio of 7.36 after repeating doses of 960 mg
Metabolism
Vemurafenib is metabolized by CYP3A4 and the metabolites make up 5% of the components in plasma. The parent compound makes up for the remaining 95%.
Toxicity
In the few toxicity reports, it has been shown an increased in the development of cutaneous squamous cell carcinomas or acceleration in pre-existant tumor growth.