Products
Capecitabine is commercially available in the form of film-coated tablets (Xeloda, generic). It has been approved in many countries since 1998.
Structure and properties
Capecitabine (C15H22FN3O6, Mr = 359.4 g/mol) is a prodrug and is converted to the cell-toxic 5-fluorouracil, the active drug, in a three-step process. Capecitabine exists as a white crystalline powder that is soluble in water. It is a fluoropyrimidine carbamate.
Effects
Capecitabine (ATC L01BC06) has cytotoxic properties. The effects are due to blockade of DNA and RNA synthesis and inhibition of cell division. The active metabolite 5-fluorouracil is formed predominantly, but not exclusively, in the tumor. The final step of activation is catalyzed by the enzyme thymidine phosphorylase, which is present at elevated levels in some tumors.
Indications
- Colon cancer (colon carcinoma, colorectal carcinoma).
- Breast cancer (mammary carcinoma)
- Cancer of the esophagus (esophageal cancer).
- Cancer of the stomach (adenocarcinoma of the stomach).
Dosage
According to the professional information. The film-coated tablets are usually taken twice daily and within 30 minutes after a meal.
Contraindications
- Hypersensitivity
- Dihydropyrimidine dehydrogenase deficiency
- Pregnancy and lactation
- Severe renal and/or hepatic insufficiency.
- Combination with brivudine or chemically related agents such as sorivudine.
For complete precautions, see the drug label.
Interactions
Drug-drug interactions have been described with anticoagulants (vitamin K antagonists), CYP2C9 substrates, antacids, allopurinol, and other cytostatic agents.
Adverse effects
The most common potential adverse effects include diarrhea, hand-foot syndrome, nausea, vomiting, abdominal pain, fatigue, weakness, and hyperbilirubinemia. Numerous other and severe adverse reactions are observed.
