Capecitabine (Xeloda)

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).
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org 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.

Diseases for which it is used

• Breast cancer
• Colon cancer
• Esophageal cancer
• Gastric cancer
• Hepatobiliary cancer
• Neuroendocrine tumors
• Pancreatic cancer
• Rectal cancer

Patient drug information

• Capecitabine (Xeloda) package insert pages 34-37
• Capecitabine (Xeloda) patient drug information (Chemocare)
• Capecitabine (Xeloda) patient drug information (UpToDate)

History of changes in FDA indication

• 4/30/1998: Initial FDA approval "for the treatment of patients with metastatic breast cancer resistant to both paclitaxel and an anthracycline-containing chemotherapy regimen or resistant to paclitaxel and for whom further anthracycline therapy is not indicated, eg, patients who have received cumulative doses of 400 mg/m2 of doxorubicin or doxorubicin equivalents. Resistance is defined as progressive disease while on treatment, with or without an initial response, or relapse within 6 months of completing treatment with an anthracycline-containing adjuvant regimen."
• 4/30/2001: New indication "as first-line treatment of patients with metastatic colorectal carcinoma when treatment with fluoropyrimidine therapy alone is preferred."
• 9/7/2001: New indication "in combination with docetaxel is indicated for the treatment of patients with metastatic breast cancer after failure of prior anthracycline containing chemotherapy.
• 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.