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Generic Name: Sorafenib
Brand Name(s): Nexavar®
IUPAC: 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino] phenoxy]-N-methyl-pyridine-2-carboxamide
FDA Approval: yes
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Usage: Approved in late 2005 for use in advanced renal cell (kidney) cancer. Approved in November 2007 for treatment of inoperable liver cancer. The use of sorafenib in other cancer types is actively being investigated. Sorafenib is administered as an oral capsule.
Mechanism: Sorafenib (Nexavar®) is one of the first of a new class of drugs. This drug blocks multiple kinases involved in cell division. Sorafenib is known to block a variety of different targets. Sorafenib inhibits many
growth factor receptors such as receptor tyrosine kinases.These include PDGFR-beta, VEGFR-2, VEGFR-3, KIT, and FLT-3. These receptors act to receive signals that directly or indirectly stimulate tumor growth. Blocking of the activity of these receptors can cause cancer cell death and/or a reduction in
angiogenesis, the process that brings new blood vessels to a growing tumor. Sorafenib also inhibits other signal transduction proteins, enzymes (serine/threonine kinases) that help to stimulate cell division. Targets include CRAF, BRAF and mutated forms of BRAF.
Side Effects: Possible side effects include nausea, diarrhea, hair loss, fatigue, hypertension (high blood pressure), effects on bone marrow resulting in leukopenia (low white blood cell counts) and lymphopenia (low
lymphocyte counts).
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