Sorafenib
- Atc Codes:L01XE05
- CAS Codes:284461-73-0#475207-59-1
- PHARMGKB ID:284461-73-0#475207-59-1
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Nexavar; Belgium: Nexavar; Bulgaria: Nexavar; Czech Republic: Nexavar; Denmark: Nexavar; Estonia: Nexavar; Finland: Nexavar; France: Nexavar; Germany: Nexavar; Greece: Nexavar; Hungary: Nexavar; Ireland: Nexavar; Italy: Nexavar; Latvia: Nexavar; Lithuania: Nexavar; Malta: Nexavar; Netherlands: Nexavar; Poland: Nexavar; Portugal: Nexavar; Romania: Nexavar; Slovakia: Nexavar; Slovenia: Nexavar; Sweden: Nexavar; UK: Nexavar.
North America
Canada: Nevaxar; USA: Nexavar.
Latin America
Argentina: Nexavar; Mexico: Nexavar.
Asia
Japan: Nexavar.
Drug combinations
Chemistry
Sorafenib: C~21~H~16~ClF~3~N~4~O~3~. Mw: 464.82. (1) 2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-trifluoromethyl)phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-; (2) 4-(4-{3-[4-Chloro-3-(trifluoromethyl)phenyl]ureido}phenoxy)-N2-methylpyridine-2-carboxamide. CAS-284461-73-0 (2006).
Sorafenib Tosylate: C~21~H~16~ClF~3~N~4~O~3~.C~7~H~8~O3S. Mw: 637.00. 1-[4-Chloro-3-(trifluoromethyl)phenyl]-3-[4-[[2-(methylcarbamoyl)pyridin-4-yl]oxy]phenyl]urea mono(4-methylbenzenesulfonate). CAS-475207-59-1 (2006).
Pharmacologic Category
Other Antineoplastic Agents; Protein Kinase Inhibitors. Tyrosine Kinase Inhibitor. Vascular Endothelial Growth Factor (VEGF) Inhibitor. (ATC-Code: L01XE05).
Mechanism of action
Multikinase inhibitor. Inhibits tumor growth and angiogenesis by inhibiting intracellular Raf kinases (CRAF, BRAF, and mutant BRAF), and cell surface kinase receptors (VEGFR-2, VEGFR-3, PDGFR-β, cKIT, and FLT-3).
Therapeutic use
Advanced renal cell cancer, unresectable hepatocellular cancer.
Pregnancy and lactiation implications
Teratogenicity and fetal loss shown in animals. There are no adequate studies in humans. As sorafenib inhibits angiogenesis, adverse effects on pregnancy would be expected. Excretion in breast milk unknown (not recommended in nursing women).
Unlabeled use
Advanced thyroid cancer.
Contraindications
Hypersensitivity to sorafenib or any component of the formulation.
Warnings and precautions
Increased risk of bleeding may occur. May cause cardiac ischemia or infarction (use with caution in cardiovascular disease). Hand-foot skin reaction and rash are most common adverse events. GI perforation reported. May cause hypertension, especially in first 6 weeks of treatment (caution if underlying or poorly-controlled hypertension). May complicate wound healing. Avoid concurrent use (if possible) with strong CYP3A4 inducers. Use caution when administering sorafenib with compounds metabolized predominantly via UGT1A1.