Capecitabine (Xeloda)

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General information

Class/mechanism: Pyrimidine analog, antimetabolite, inhibitor of thymidylate synthase. Converted in vivo to fluorouracil (5-FU), which is metabolized to 5-fluoro-2'-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP inhibits DNA synthesis by binding to thymidylate synthase and inhibiting production of thymidylate; FUTP interferes with RNA processing when it is mistakenly incorporated in place of uridine triphosphate (UTP).[1][2][3]
Route: PO
Extravasation: n/a

For conciseness and simplicity, currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, Medscape, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Patient safety

DPYD intermediate or poor metabolizers: Results in higher adverse reaction risk (severe, life-threatening, or fatal toxicities). No dosage has proven safe in poor metabolizers, and insufficient data are available to recommend a dosage in intermediate metabolizers. Withhold or discontinue in the presence of early-onset or unusually severe toxicity.[4]

EMA has recommended that patients should be tested for the lack of the enzyme dihydropyrimidine dehydrogenase (DPD) before starting cancer treatment with fluorouracil given by injection or infusion (drip) or with the related medicines, capecitabine and tegafur.

Diseases for which it is used

Patient drug information

History of changes in FDA indication

Breast cancer

Colon cancer

  • 6/15/2005: New indication as a single agent for adjuvant treatment in patients with Dukes’ C colon cancer who have undergone complete resection of the primary tumor when treatment with fluoropyrimidine therapy alone is preferred. (Based on X-ACT)

Colorectal cancer

  • 4/30/2001: New indication as first-line treatment of patients with metastatic colorectal carcinoma when treatment with fluoropyrimidine therapy alone is preferred. (Based on Hoff et al. 2001 & Van Cutsem et al. 2001)

History of changes in EMA indication

  • 2/2/2001: Initial market authorization as Xeloda.

Also known as

  • Code name: Ro 09-1978/000
  • Generic names: capecitabine RDT, kapesitabin
  • Brand names: Cabita, Capebin, Capegard, Capnat, Caposib, Capsy, Caxeta, Citabin, Ecansya, Flagoda, Naprocap, Skemca, Xeloda, Xlotabin