Capecitabine

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Information about Capecitabine

Capecitabine is a pyrimidine analogue used as an antineoplastic agent to treat metastatic and advanced forms of breast and colon cancer, often in combination with other agents. 

Liver safety of Capecitabine

Capecitabine is associated with a low rate of transient serum aminotransferase elevations during therapy but has been only rarely implicated in cases of clinically apparent acute liver injury

Mechanism of action of Capecitabine

Capecitabine (kap" e sye' ta been) is a pyrimidine analogue (pentyloxycarbonyl-deoxy-fluorocytidine) that has antineoplastic action against several solid tumors, including breast and colon cancers.  Capecitabine is a prodrug of 5-fluorouracil (5-FU) and is converted to this active metabolite intracellularly, where it acts by interfering with DNA, RNA and protein synthesis and inhibiting cell division.  Unlike 5-FU, capecitabine can be given by mouth.  Furthermore, capecitabine is converted to 5-FU in a three step process, the first of which takes place in the liver and the last two predominantly in tumor cells, which may account for why it is better tolerated than 5-FU. 

FDA approval information for Capecitabine

Capecitabine was approved for use as an anticancer agent in the United States in 1998 and is currently an important component of several cancer chemotherapeutic regimens.  Current indications include advanced, metastatic breast cancer and colorectal cancers, usually after failure of first line therapies. 


Dosage and administration for Capecitabine

Capecitabine is available as tablets of 150 and 500 mg generically and under the brand name Xeloda.  The recommended dose is based upon body surface area and renal function, but is generally initiated in a dose of 2.5 grams per meter squared in two divided doses daily for 2 weeks, followed by a 1 week rest period and then repeated at irregular intervals in 3 week cycles. 

Side effects of Capecitabine

Common side effects include bone marrow suppression, diarrhea, nausea, vomiting, hand-foot syndrome, fatigue, weakness, headache, dizziness, insomnia, paresthesias, abdominal pain, stomatitis, and rash.

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