Vemurafenib

The drug is used to treat advanced or metastaticThe term for a cancer that has spread beyond its point of origin. Metastatic disease is responsible for the majority of cancer deaths. melanoma that can not be removed by surgery. It is only used in patients whose cancer cells have the BRAF V600E mutation. Vemurafenib is given as a pill, typically two pills at a time, twice daily.1
Vemurafenib (ZELBORAF®) works by blocking an enzymeA protein that speeds up the process of chemical reactions in the body without becoming altered in the process. Almost every biological process is driven by the activity of enzymes. Without enzyme catalysts, the complex reactions that build and break down cell parts would not happen at a rate compatible with life. Enzyme names usually describe the reaction that is being catalyzed and all of them end in -ase. encoded by the BRAF geneA stretch of DNA that leads to the production of an RNA. The RNA is produced during the process of transcription. This RNA can be used to guide the formation of a protein via translation or can be used directly in the cell.. The enzyme is a kinaseAn enzyme that adds phosphate groups to another molecule. Many key proteins controlling gene expression are kinase targets. Addition of a phosphate group to a protein can alter the activity of the protein and are often used as molecular on/off switches. For example, the retinoblastoma tumor suppressor gene is 'off' when phosphate groups are added to the protein at specific locations. Removal of the phosphate groups turns the protein 'on'. Enzymes that remove phosphate groups are known as phosphatases. Note that all enzymes, regardless of function, end in ASE and like all kinases, its job is to add phosphate groups onto targets. The addition (or removal) of phosphate groups from proteins frequently acts like an on-off switch. This drug blocks the activity of a specific mutated form of BRAF. The presence of the mutation in the cancer must be identified by a special (FDA-approved) test before the drug can be used on a patient. It should be noted that Vemurafenib does not inhibit wild-type BRAF or other Raf kinases.1
The diagram below shows the 3D molecular structure of Vemurafenib.
Vemurafenib can have some serious side effects, which include the development of cutaneous squamous cell cancers and keratoacanthomas as a result of treatment. Other, less severe toxicities include skin reactions, elevations in serum bilirubin and photosensitivity.1