Sorafenib (Nexavar)

General information

Class/mechanism: Tyrosine kinase inhibitor that inhibits multiple kinases: RAF1, BRAF, KIT, FLT-3, RET, vascular endothelial growth factor receptors VEGFR-1, VEGFR-2, VEGFR-3, and platelet-derived growth factor receptor beta (PDGFR-B). Inhibition of these kinases disrupts angiogenesis, tumor cell signaling, and induces apoptosis.
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is established (work in progress)

• Hepatocellular carcinoma
• Renal cell carcinoma
  • Clear cell renal cell carcinoma
• Differentiated thyroid cancer

Diseases for which it is used

• Acute myeloid leukemia
• Gastrointestinal stromal tumor
• Non-small cell lung cancer, nonsquamous
• Osteosarcoma
• Soft tissue sarcoma
  • Desmoid tumors
• Thyroid cancer
  • Medullary thyroid cancer

Patient drug information

• Sorafenib (Nexavar) package insert
• Sorafenib (Nexavar) patient drug information (Chemocare)
• Sorafenib (Nexavar) patient drug information (UpToDate)

History of changes in FDA indication

• 2005-12-20: Approved for the treatment of patients with advanced renal cell carcinoma (RCC). (Based on TARGET_RCC)
• 2007-11-16: Approved for the treatment of patients with unresectable hepatocellular carcinoma (HCC). (Based on SHARP)
• 2013-11-22: Approved for the treatment of locally recurrent or metastatic, progressive, differentiated thyroid carcinoma (DTC) refractory to radioactive iodine treatment. (Based on DECISION)

History of changes in EMA indication

• 2006-07-19: Initial marketing authorization as Nexavar

History of changes in Health Canada indication

• 2006-07-28: Initial notice of compliance with conditions
• 2009-06-12: Conditions were met

History of changes in PMDA indication

• 2008-01-25: Initial approval for the treatment of unresectable or metastatic renal cell carcinoma.
• 2009-05-20: New additional indication for the treatment of unresectable hepatocellular carcinoma.
• 2014-06-20: New additional indication for the treatment of unresectable differentiated thyroid carcinoma.
• 2016-02-29: Revised indication for the treatment of unresectable thyroid cancer.

Also known as

• Code names: BAY 43-9006, BAY 54-9085
• Brand names: Nexavar, Sorafenat, Soranib