Capecitabine: an overview of the side effects and their management

• Published in: Anti-cancer drugs Vol. 19; no. 5; pp. 447 - 464
• Main Authors: Saif, Muhammad Wasif, Katirtzoglou, Nikos A, Syrigos, Kostas N
• Format: Journal Article
• Language: English
• Published: England Lippincott Williams & Wilkins, Inc 01-06-2008
• Subjects: Administration, Oral; Age Factors; Antimetabolites, Antineoplastic - administration & dosage; Antimetabolites, Antineoplastic - adverse effects; Antimetabolites, Antineoplastic - therapeutic use; Breast Neoplasms - drug therapy; Capecitabine; Colorectal Neoplasms - drug therapy; Deoxycytidine - administration & dosage; Deoxycytidine - adverse effects; Deoxycytidine - analogs & derivatives; Deoxycytidine - therapeutic use; Drug Interactions; Female; Fluorouracil - administration & dosage; Fluorouracil - adverse effects; Fluorouracil - analogs & derivatives; Fluorouracil - therapeutic use; Humans; Male; Patient Education as Topic; Prodrugs - administration & dosage; Prodrugs - adverse effects; Prodrugs - therapeutic use
• ISSN: 0959-4973; 1473-5741
• DOI: 10.1097/CAD.0b013e3282f945aa

Xeloda (capecitabine), a thymidine phosphorylase activated fluoropyrimidine carbamate, is currently the only universally approved orally administered 5-fluorouracil (5-FU) prodrug. It belongs to a newer generation of orally administered fluoropyrimidines. It has been developed because of the clinical need for efficient, tolerable and convenient agents, which do not require continuous infusion. Capecitabine is not a cytotoxic drug in itself, but via a three-step enzymatic cascade, it is converted to 5-FU mainly within human cancer cells. While the drug compares favorably with 5-FU in patients with advanced or metastatic colorectal cancer and pretreated breast cancer, it also has an improved toxicity profile, mainly of gastrointestinal and dermatologic effects with a significantly lower incidence of grade 3/4 myelotoxicity compared with infusional 5-FU-based chemotherapy. Capecitabineʼs selective activation within the tumor allows for less systemic toxicity events. A gradient of fluoropyrimidine toxicity is observedhigh in the US and low in East Asia. In addition, there is a discrepancy in tolerance of dose among patients treated in the US vs. Europe. Although patients can take the drug orally in the convenience of their own home, the key to successful management of capecitabine is the clinicianʼs awareness of its severe, but low in incidence, adverse effects, and the patientsʼ education, emphasizing compliance with the treatment plan, prevention and timely recognition of its toxicities.