Sorafenib

Diagram of the molecular structure of Sorafenib
Brand name: Nexavar®
IUPAC: 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino] phenoxy]-N-methyl-pyridine-2-carboxamide
FDA approval: Yes
Usage:

Approved in late 2005 for use in advanced renal cell (kidney) cancer. Approved in November 2007 for treatment of inoperable liver cancer. Sorafenib is also used in treatment of unresectable hepatocellular cancer (HCC). Sorafenib is administered as an oral capsule.1

Mechanism:

Sorafenib (Nexavar®) is characterized as a signal transduction inhibitor. This drug blocks multiple kinases involved in cell division and inhibits many growth factorA substance that stimulates cell division. Growth factors are usually small proteins or steroid hormones. They may be secreted by the same cells on which they act or by cells that reside in a different part of the body than the target cells. Some examples of growth factors include estrogen, a growth factor for breast cells, and VEGF, a growth factor that causes the development of blood vessels. Several different anti-cancer treatments are designed to inhibit the activity of growth factors. receptors such as receptor tyrosine kinases.These receptor tyrosine kinases include PDGFR-beta, VEGFR-2, VEGFR-3, KIT, and FLT-3, which 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 angiogenesisThe formation of blood vessels. This process is required for a tumor to grow past a small size since the blood delivers nutrients to the cells in the tumor mass., 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.1

The diagram below shows the 3D molecular structure for Sorafenib.

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 lymphocyteA immune cell that resides primarily in the lymphatic system. The lymphocytes include T-cells (cells involved in the control of immune responses and cellular cytotoxicity) and B-cells (cells that produce antibodies or immunoglobulins). counts). 1

  • 1.a. b. c. Chu, E., & DeVita, V. T. (2015). Physicians' cancer chemotherapy drug manual 2015. Burlington, MA: Jones & Bartlett Learning.