Capecitabine

Capecitabine tablets are a nucleoside metabolic inhibitor indicated for: Colorectal Cancer adjuvant treatment of patients with Stage III colon cancer as a single agent or as a component of a combination chemotherapy regimen. ( 1.1 ) perioperative treatment of adults with locally advanced rectal cancer as a component of chemoradiotherapy. ( 1.1 ) treatment of patients with unresectable or metastatic colorectal cancer as a single agent or as a component of a combination chemotherapy regimen.

12.1 Mechanism of Action Capecitabine is metabolized to fluorouracil in vivo. Both normal and tumor cells metabolize fluorouracil to 5-fluoro-2’-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). These metabolites cause cell injury by two different mechanisms. First, FdUMP and the folate cofactor, N 5-10 -methylenetetrahydrofolate, bind to thymidylate synthase (TS) to form a covalently bound ternary complex. This binding inhibits the formation of thymidylate from 2’-deoxyuridylate.

Pharmacokinetic profiling of Capecitabine demonstrates an elimination half-life of Elimination kinetics span 8 to 18 hours per Capecitabine clinical pharmacology with Consistent 70%–82% gastrointestinal absorption profile for Capecitabine systemic bioavailability; clearance proceeds via cytochrome cyp2c9 biotransformation with dual hepatorenal elimination, reaching clinical onset within cmax attained 2–4 hours post-administration of capecitabine.

Titration schedules for Capecitabine (500 mg/1 Tablet, Film Coated → 150 mg/1 Tablet, Film Coated → 150 mg/1 Tablet → 500 mg/1 Tablet → 150mg Tablet) require excluding capecitabine tablets are contraindicated in patients with history of severe hypersensitivity reaction to fluorouracil or capecitabine .; history of severe hypersensitivity reactions to fluorouracil or capecitabine ( 4 ); real-world patient logs highlight nausea (13.1% of reports), diarrhea (10.4% of reports), headache (7.3% of reports) alongside a 85.00% Worth-It consensus.