Colorectal Cancer: Capecitabine is indicated 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. It is indicated as first-line treatment of patients with metastatic colorectal carcinoma when treatment with fluoropyrimidine therapy alone is preferred. Breast Cancer: Capecitabine in combination with docetaxel is indicated for the treatment of patients with metastatic breast cancer after failure of prior anthracycline-containing chemotherapy. Monotherapy is also indicated 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. Pancreatic Cancer: Capecitabine is indicated for the first line treatment of patients with locally advanced and metastatic pancreatic cancer in combination with gemcitabine. Oesophagogastric Cancer: Capecitabine is indicated for the first line treatment of patients with advanced oesophagogastric cancer.
Capecitabine is a preparation of Capecitabine, an orally-administered chemotherapeutic agent used in the treatment of cancers. Capecitabine is a prodrug, that is enzymatically converted to fluorouracil (antimetabolite) in the tumour, where it inhibits DNA synthesis and slows growth of tumour tissue.
Capecitabine is a prodrug that is selectively tumour-activated to its cytotoxic moiety, fluorouracil, by thymidine phosphorylase, an enzyme found in higher concentrations in many tumours compared to normal tissues or plasma. Fluorouracil is further metabolized to two active metabolites, 5-fluoro-2'-deoxyuridine 5-monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP), within normal and tumour cells. These metabolites cause cell injury by two different mechanisms. First, FdUMP and the folate cofactor, N5-10 methylenetetrahydrofolate, bind to thymidylate synthase (TS) to form a covalently bound ternary complex. This binding inhibits the formation of thymidylate from 2-deoxyuridylate. Thymidylate is the necessary precursor of thymidine triphosphate, which is essential for the synthesis of DNA, therefore a deficiency of this compound can inhibit cell division. Secondly, nuclear transcriptional enzymes can mistakenly incorporate FUTP in place of uridine triphosphate (UTP) during the synthesis of RNA. This metabolic error can interfere with RNA processing and protein synthesis through the production of fraudulent RNA.
In case of stage-III colon cancer and locally advanced or metastatic breast cancer: 1.25 gm/m2 twice daily for 14 days, followed by a 7-day interval, given as 3-week cycles for a total 8 cycles . For metastatic colorectal cancer, in combination therapy it is administered as 0.8-1 gm/m2 twice daily for 14 days repeated after 7 days interval.
Anticoagulants: Anticoagulant response (INR or prothrombin time) should be monitored frequently in order to adjust the anticoagulant dose as needed.
Phenytoin: Phenytoin levels should be monitored in patients taking Capecitabine concomitantly with phenytoin. The phenytoin dose may need to be reduced.
Leucovorin: The concentration of 5-fluorouracil is increased and its toxicity may be enhanced by leucovorin.
CYP2C9 substrates: Care should be exercised when Capecitabine is co-administered with CYP2C9 substrates.
Food: Reduced both the rate and extent of absorption of Capecitabine.
Capecitabine is contraindicated in patients with known dihydropy rimidine dehydrogenase (DPD) deficiency, it is also contraindicated in patients with severe renal impairment (creatinine clearance below 30 ml/min), and in patients with known hypersensitivity to Capecitabine. Patients receiving therapy with capecitabine should be monitored by a physician experienced in the use of cancer chemotherapeutic agents. Most adverse reactions are reversible and do not need to result in discontinuation, although doses may need to be withheld or reduced. During therapy, tablets should not be broken to adjust the dose.
myocardial infarction, angina; hand-foot syndrome (numbness, tingling, pain, redness, or blistering of the palms of the hands and soles of the feet). This can lead to the disappearance of fingerprints in some patients; diarrhea (sometimes severe), nausea, stomatitis; neutropenia, anemia, thrombocytopenia; Hyperbilirubinemia.
Pregnancy Category D. There is positive evidence of human fetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
The manifestations of acute overdose include nausea, vomiting, diarrhea, mucositis, gastrointestinal irritation and bleeding, and bone marrow depression. Medical management of overdose should include customary therapeutic and supportive medical interventions aimed at correcting the presenting clinical manifestations and preventing their possible complications.
Keep in a dry place and store below 30°C. Protect from light and keep out of the reach of children.
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