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What is Capecitabine? |
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Capecitabine is an orally-administered
chemotherapeutic agent used in the treatment of metastatic
breast and colorectal cancers. Capecitabine is a prodrug,
that is enzymatically converted to 5-fluorouracil in the
tumor, where it inhibits DNA synthesis and slows growth of
tumor tissue. The activation of capecitabine follows a
pathway with three enzymatic steps and two intermediary
metabolites, 5'-deoxy-5-fluorocytidine (5'-DFCR) and
5'-deoxy-5-fluorouridine (5'-DFUR), to form 5-fluorouracil.
Capecitabine is marketed under the trade name Xeloda
(Roche). |
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Indications of Capecitabine |
Capecitabine is FDA-approved for:
Adjuvant in colorectal cancer Stage III Dukes' C - used as
first-line monotherapy.
Metastatic colorectal cancer - used as first-line
monotherapy, if appropriate.
Metastatic breast cancer - used in combination with
docetaxel, after failure of anthracycline-based treatment.
Also as monotherapy, if the patient has failed paclitaxel-based
treatment, and if anthracycline-based treatment has either
failed or cannot be continued for other reasons (i.e., the
patient has already received the maximum lifetime dose of an
anthracycline).
In the UK, capecitabine is approved by the National
Institute for Health and Clinical Excellence (NICE) for
colon and colorectal cancer, and locally advanced or
metastatic breast cancer. |
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Dose of Capecitabine |
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The usual starting dose is 2,500 mg/m2/day in
two divided doses, 12 hours apart. One cycle includes two
weeks of treatment followed by one week without treatment.
Cycles can be repeated every three weeks. |
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Dose Adjustments of Capecitabine |
For mild renal dysfunction (creatinine
clearance 30-50 mL/min), it is recommended to reduce dose by
25%.
For severe renal dysfunction (creatinine clearance <30 mL/min),
treatment is not recommended.
There is no recommendation for hepatic dysfunction.
For elderly patients, lower doses may be required due to
higher incidences of serious adverse reactions. |
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Side effects of Capecitabine |
Potential major adverse reactions include:
Cardiovascular: EKG changes, myocardial infarction, angina
(these may be more common in patients with pre-existing
coronary artery disease)
Dermatological: Hand-foot syndrome (numbness, tingling,
pain, redness, or blistering of the palms of the hands and
soles of the feet)
Gastrointestinal: Diarrhea (sometimes severe), nausea,
stomatitis
Hematological: Neutropenia, anemia, thrombocytopenia
Hepatic: Hyperbilirubinemia |
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Drug Interactions of Capecitabine |
May interact with warfarin and increase
bleeding risk.
May inhibit cytochrome CYP2C9 enzyme, and therefore increase
levels of substrates such as phenytoin and other substrates
of CYP2C9.
Much as fluorouracil, the concomitant use of leucovorin may
increase both the efficacy and the toxicity of capecitabine.
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Disclaimer:
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Information on this page is provided for
general information purposes. You should not make a clinical
treatment decision based on information contained in this
page without consulting other references including the
package insert of the drug, textbooks and where relevant,
expert opinion. We cannot be held responsible for any errors
you make in administering drugs mentioned on this page, nor
for use of any erroneous information contained on this
page. |
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