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Capecitabine: a review
Christine M Walko1, Celeste Lindley
1Department of Pharmacotherapy and Experimental Therapeutics, University of North Carolina School of Pharmacy, Chapel Hill, North Carolina 27599-7360, USA. christine_walko@unc.edu
Clinical Therapeutics
|March 15, 2005
Summary
Capecitabine, an oral prodrug of fluorouracil (FU), offers improved tolerability and efficacy in treating various cancers, including breast and colorectal. Its oral administration and tumor-specific conversion make it a valuable option in oncology.
Area of Science:
- Oncology
- Pharmacology
- Drug Development
Background:
- Fluorouracil (FU) is an antimetabolite used against various cancers but causes systemic toxicity due to non-selective action.
- Capecitabine, an oral FU prodrug, was developed to enhance tolerability and intratumoral drug concentrations via tumor-specific conversion.
Purpose of the Study:
- To review capecitabine's clinical pharmacology, mechanism of action, pharmacokinetics, pharmacodynamics, efficacy, adverse effects, drug interactions, and administration.
- To explore ongoing research and future directions for capecitabine in cancer treatment.
Main Methods:
- Literature search of PubMed and International Pharmaceutical Abstracts (1966-2004).
- Included Phase II/III trials and reviewed references for additional sources.
- Incorporated product information from Roche Pharmaceuticals.
Main Results:
- Capecitabine is an oral prodrug converted to FU by thymidine phosphorylase, with higher levels in tumors.
- Demonstrated comparable efficacy to IV FU/leucovorin in colorectal cancer and superior efficacy in combination with docetaxel for metastatic breast cancer.
- Common adverse effects include hyperbilirubinemia, diarrhea, and hand-foot syndrome; generally better tolerated than IV FU/LV.
Conclusions:
- Capecitabine is FDA-approved for metastatic colorectal and breast cancer, with demonstrated benefits in other cancers.
- Its oral administration, improved tolerability, and comparable efficacy make it an attractive option for cancer treatment.
- Capecitabine is a focus for future clinical trials in various oncological indications.