Capecitabine was developed as a prodrug of FU, with the goal of improving tolerability and intratumor drug concentrations through tumor-specific conversion to the active drug. Pharma cokinetics. How capecitabine works . Mechanisms of Action . 5-Fluorouracil (5-FU) is widely used in the treatment of cancer. Capecitabine is a Nucleoside Metabolic Inhibitor. Both normal and tumor cells metabolize 5-FU to 5-fluoro-2’-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). 12.1 Mechanism of Action 12.3 . Common side effects include abdominal pain, vomiting, diarrhea, weakness, and rashes. Capecitabine may increase the anticoagulant effects of warfarin increasing the INR several days up to several months after initiating capecitabine or within one month after stopping the therapy. Capecitabine is an oral medication for treating advanced breast cancer that is resistant to combination therapy with the drugs of choice, paclitaxel ( Taxol ) and a drug from the anthracycline family of … Capecitabine is a type of chemotherapy called an anti metabolite. Data sources include IBM Watson Micromedex (updated 4 May 2020), Cerner Multum™ (updated 2 June 2020), Wolters Kluwer™ … Xeloda - Clinical Pharmacology Mechanism of Action. [5] These two drugs have distinct mechanisms of action, only partially overlapping toxicities, and single-agent activities in colorectal cancer. Metastatic Colorectal Cancer 14.3 Breast Cancer. 35 PK studies in patients showed rapid gastrointestinal absorption of capecitabine, followed by extensive conversion to 8, with only low systemic levels of 5-FU. Enzymes convert capecitabine to 5-fluorouracil (5-FU) in vivo. For breast cancer it is often used together with docetaxel. Interferes with protein synthesis 3. Mechanism of action 5-fluorouracil Inhibition of thymidylate synthase (potentiated by addition of leucovorin) Incorporation of fraudulent bases into DNA and RNA Raltitrexed Direct inhibitor of thymidylate synthase Capecitabine As for 5-fluorouracil Irinotecan Topoisomerase I poison Oxaliplatin
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The purpose of this article is to review the available information on capecitabine with respect to clinical pharmacology, mechanism of action, pharmacokinetic and pharmacodynamic properties, clinical efficacy for breast and colorectal cancer adverse-effect profile, documented drug interactions, dosage and administration, and future directions of ongoing research. Drugs.com provides accurate and independent information on more than 24,000 prescription drugs, over-the-counter medicines and natural products. These metabolites cause cell injury by two different mechanisms. Enzymes convert capecitabine to 5-fluorouracil (5-FU) in vivo. 5-FU cannot be methylated by thymidylate synthase, causing sustained inhibition of the enzyme and decreased production of dTMP. Capecitabine has been prescribed for a client, and the client asks the nurse about the action of the medication. Preclinical studies demonstrated that sequential administration of low-dose irinotecan plus capecitabine was highly curative in in vivo xenograft models of human colorectal cancer. 12.1 Mechanism of Action. CAPECITABINE is converted to 5-FLUOROURACIL in cancer cells . Risk factors include >60 years of age and cancer. Capecitabine (6) is an orally administered fluoropyrimidine carbamate that is metabolized in vivo to 5-FU (3). This has happened within several days and up to several months after capecitabine was started. 14.1 . Other serious side effects include allergic reactions. It is given by injection into a vein.. Common side effects include numbness, feeling tired, nausea, diarrhea, and low blood cell counts. This material is provided for educational purposes only and is not intended for medical advice, diagnosis or treatment. What is capecitabine (Xeloda), and how does it work (mechanism of action)? Often it is used together with fluorouracil and folinic acid (leucovorin) in advanced cancer. You might have it as a treatment for a number of different types of cancer. Some tumors are inherently more sensitive than others to the metabolic actions of 5-FU. Its spectrum of activity and pharmacokinetic profile are similar to infusional fluorouracil. 15 REFERENCES 16 HOW SUPPLIED/STORAGE AND HANDLING 17 PATIENT COUNSELING INFORMATION Capecitabine (Xeloda) Capecitabine (also known as Xeloda) is a type of chemotherapy. 13 NONCLINICAL TOXICOLO GY . Processes enzymes needed for cellular growth