Capecitabine

General information

Capecitabine is a prodrug of fluorouracil, which has been developed as a tumor-selective fluoropyrimidine carbamate in order to achieve high cytotoxic concentrations of fluorouracil in tumor cells. In addition, during daily oral administration, capecitabine mimics continuous fluorouracil administration.

The systemic availability of oral fluorouracil is unacceptably highly variable (0–80%). More consistent availability could be achieved by the concomitant use of reversible or irreversible inhibitors of dihydropyrimidine dehydrogenase, such as 5-chloro-2,4-dihydroxypyridine (reversible) or eniluracil (irreversible). However, phase II/III trials have given disappointing results compared with fluorouracil + leucovorin. In contrast, the fluorouracil prodrug capecitabine has achieved better response rates and equivalent overall survival and time to disease progression compared with fluorouracil + leucovorin in patients with advanced colorectal cancer. Capecitabine has therefore been approved in the USA and Europe as first-line therapy for metastatic colorectal cancer [ ].

Diarrhea is the second most common adverse effect of capecitabine. Less frequently, adverse effects such as mucositis, leopard-like vitiligo, peripheral neuropathy, and onycholysis have been reported [ , ]. Capecitabine should be taken with food.

Organs and systems