Sorafenib: a clinical and pharmacologic review.

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Iyer R, Fetterly G, Lugade A, Thanavala Y

Sorafenib: a clinical and pharmacologic review.

Expert Opin Pharmacother. 2010 Aug;11(11):1943-55. doi: 10.1517/14656566.2010.496453.

PubMed ID

20586710 [ View in PubMed

]

Abstract

IMPORTANCE OF THE FIELD: Sorafenib is an oral receptor tyrosine kinase inhibitor that inhibits Raf serine/threonine kinases and receptor tyrosine kinases (vascular endothelial growth factor receptors 1, 2, 3 and platelet-derived growth factor-beta, Flt-3 and c-kit) that are implicated in tumorigenesis and tumor progression. Sorafenib is approved for the treatment of advanced inoperable hepatocellular cancer and advanced renal cell cancer. AREAS COVERED IN THIS REVIEW: The findings from the major Phase III studies that led to FDA approval of this drug for the above indications are reviewed. Key aspects of sorafenib pharmacology, dosing in the presence of organ dysfunction, toxicities and weaknesses of the research done so far are summarized. WHAT WILL THE READER GAIN: The reader will have the knowledge of the major studies that form the basis of the clinical use of sorafenib, information on the upcoming Phase III trials that could lead to changes in clinical practice and some insights on aspects of the drugs' mechanism of action and toxicity that still remain unclear. TAKE HOME MESSAGE: Sorafenib is a well-tolerated oral antiangiogenic agent approved for treatment of two angiogenesis-driven cancers. Studies to broaden the clinical indications and increase understanding of the clinical and laboratory biomarkers of response are needed.

DrugBank Data that Cites this Article

Drugs

Sorafenib

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Sorafenib	Mast/stem cell growth factor receptor Kit	Protein	Humans	Yes	Antagonist	Details
Sorafenib	Platelet-derived growth factor receptor beta	Protein	Humans	Yes	Inhibitor	Details
Sorafenib	RAF proto-oncogene serine/threonine-protein kinase	Protein	Humans	Yes	Inhibitor	Details
Sorafenib	Receptor-type tyrosine-protein kinase FLT3	Protein	Humans	Yes	Inhibitor	Details
Sorafenib	Serine/threonine-protein kinase B-raf	Protein	Humans	Yes	Inhibitor	Details
Sorafenib	Vascular endothelial growth factor receptor 1	Protein	Humans	Yes	Inhibitor	Details
Sorafenib	Vascular endothelial growth factor receptor 2	Protein	Humans	Yes	Inhibitor	Details
Sorafenib	Vascular endothelial growth factor receptor 3	Protein	Humans	Yes	Inhibitor	Details