Name Capecitabine
Classes Anticancer/Antineoplastic Agent
Antimetabolites
Diseases Breast Cancer
Cancer
Colon Cancer
Colorectal Cancer

Capecitabine

Capecitabine is an antineoplastic agent from the class called the antimetabolites. In vivo, enzymes convert capecitabine to 5-fluorouracil (5-FU). 5-FU is metabolized by both normal and tumor cells to 5-fluoro-2'-deoxyuridine monophosphate (FdUMP) and 5-fluouridine triphosphate (FUTP). These metabolites harm cells through two distinct mechanisms which ultimately inhibits the production of thymidylate, RNA & proteins. 

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 anthracycline containing therapy
  • As monotherapy in patients resistant to both paclitaxel and an anthracycline-containing regimen
  • Take Capecitabine 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 Capecitabine 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
  • Capecitabine dosage may need to be individualized to optimize patient management
  • Reduce the dose of Capecitabine by 25% in patients with moderate renal impairment

Most common adverse reactions were-

  • diarrhea
  • hand-and-foot syndrome
  • nausea
  • vomiting
  • abdominal pain
  • fatigue/weakness
  • jaundice
  • Coagulopathy: May result in bleeding, death. Monitor anticoagulant response (e.g., INR) and adjust anticoagulant dose accordingly. 
  • Cardiotoxicity: Common in patients with a prior history of coronary artery disease. 
  • Diarrhea: May be severe. Interrupt Capeciabine treatment immediately until diarrhea resolves or decreases to grade 1. Recommend standard antidiarrheal treatments.
  • Increased Risk of Severe or Fatal Adverse Reactions in Patients with Lo w or Absent Dihydropyrimidine Dehydrogenase (DPD) Activity: Withhold or permanently discontinue Capeciabine in patients with evidence of acute early-onset or unusually severe toxicity, which may indicate near complete or total absence of DPD activity. No Capeciabine dose has been proven safe in patients with absent DPD activity. 
  • Dehydration and Renal Failure: Interrupt Capeciabine treatment until dehydration is corrected. Potential risk of acute renal failure secondary to dehydration. Monitor and correct dehydration. 
  • Pregnancy: Can cause fetal harm. Advise women of the potential risk to the fetus. 
  • Mucocutaneous and Dermatologic Toxicity: Severe mucocutaneous reactions, Steven-Johnson Syndrome (SJS) and Toxic Epidermal Necrolysis (TEN), have been reported. Capeciabine should be permanently discontinued in patients who experience a severe mucocutaneous reaction during treatment. Capeciabine may induce hand-and-foot syndrome. Interrupt Capeciabine treatment until the hand-and-foot syndrome event resolves or decreases in intensity. 
  • Hyperbilirubinemia: Interrupt Capeciabine treatment immediately until the hyperbilirubinemia resolves or decreases in intensity. 
  • Hematologic: Do not treat patients with neutrophil counts <1.5 x 109/L or thrombocyte counts <100 x 109/L. If grade 3-4 neutropenia or thrombocytopenia occurs, stop therapy until condition resolves.

Contraindication

Contraindicated in patients with hypersensitivity to capecitabine.

Contraindicated in patients with severe Renal Impairment.