Sorafenib

Products

Sorafenib is commercially available in the form of film-coated tablets (Nexavar). It has been approved in many countries since 2006.

Structure and properties

Sorafenib (C21H16ClF3N4O3, Mr = 464.8 g/mol) is present in drugs as sorafenibtosilate, a white to yellowish or brownish powder that is practically insoluble in water.

Effects

Sorafenib (ATC L01XE05) has antiproliferative, antitumor, and antiangiogenic properties. The effects are due to inhibition of several kinases (multi-kinase inhibitor). These include RAF, c-KIT, FLT, VEGFR and PDGFR. The half-life is between 25 to 48 hours. In clinical trials, sorafenib has been shown to statistically significantly prolong survival.

Indications

  • Hepatocellular carcinoma
  • Advanced renal cell carcinoma
  • Thyroid carcinoma (end stage)

Dosage

According to the professional information. Tablets are taken twice daily fasting or with a light, low-fat meal.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Sorafenib is metabolized by CYP3A4, UGT1A9, and UGT1A1 and undergoes marked enterohepatic cycling.

Adverse effects

The most common potential adverse effects include:

  • Joint pain
  • Bleeding, high blood pressure
  • Digestive disorders such as diarrhea, nausea, vomiting and constipation.
  • Hypophosphatemia, lack of appetite, weight loss.
  • Infections, lymphopenia
  • Fatigue, pain, fever
  • Dry skin, rash, hair loss, hand-foot syndrome, itching.