(capecitabine) is a nucleoside metabolic inhibitor with antineoplastic activity indicated for: ? Adjuvant Colon Cancer ? Patients with Dukes’ C colon cancer ? Metastatic Colorectal Cancer ? First-line as monotherapy when treatment with fluoropyrimidine therapy alone is preferred ? Metastatic Breast Cancer ? In combination with docetaxel after failure of prior anthracyclinecontaining therapy ? As monotherapy in patients resistant to both paclitaxel and an anthracycline-containing regimen
Nucleoside metabolic inhibitor
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.
Take it with water within 30 min after a meal ? Monotherapy: 1250 mg/m2 twice daily orally for 2 weeks followed by a one week rest period in 3-week cycles ? Adjuvant treatment is recommended for a total of 6 months (8 cycles) ? In combination with docetaxel,the recommended dose of XELODA is 1250 mg/m2 twice daily for 2 weeks followed by a 7-day rest period, combined with docetaxel at 75 mg/m2 as a 1-hour IV infusion every 3 weeks . ? XELODA dosage may need to be individualized to optimize patient management . ? Reduce the dose of XELODA by 25% in patients with moderate renal impairment .
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 Capcitab 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 Capcitab is co-administered with CYP2C9 substrates.
Food: Reduced both the rate and extent of absorption of Capcitab.
Severe Renal Impairment ? Hypersensitivity
Diarrhea,hand-and-foot syndrome,nausea,vomiting,abdominal pain,fatigue/weakness,and hyperbilirubinemia
Nursing Mothers: Discontinue nursing when receiving XELODA treatment.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.
.png&w=384&q=75)