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At a glance

Capecitabine is an oral chemotherapy medication used in the treatment of colorectal cancer, breast cancer, and gastric cancer. It is a prodrug that is converted to 5-fluorouracil in the body, interfering with DNA and RNA synthesis in cancer cells, slowing their growth and destroying them.

Indications
  • Adjuvant colon cancer (Dukes' C colon cancer)
  • Metastatic colorectal cancer (first-line monotherapy)
  • Metastatic breast cancer (in combination with docetaxel or as monotherapy)
  • Gastric cancer (in combination with platinum-based compound)
Pharmacology

Capecitabine is a prodrug that is selectively converted to fluorouracil in tumors by thymidine phosphorylase. Fluorouracil is further metabolized to two active metabolites: FdUMP and FUTP. FdUMP inhibits thymidylate synthase, blocking DNA synthesis. FUTP is incorporated into RNA in place of UTP, interfering with RNA processing and protein synthesis.

Dosage

Monotherapy (Colorectal and Breast Cancer): 1250 mg/m² twice daily (oral) for 2 weeks, followed by a 1-week rest period; 3-week cycles. Adjuvant treatment: 6 months (8 cycles) recommended.

In combination with docetaxel (Breast Cancer): 1250 mg/m² twice daily (2 weeks) + docetaxel 75 mg/m² IV (1 hour) every 3 weeks.

Gastric Cancer (with platinum-based compound): 1000 mg/m² twice daily for 14 days, followed by a 7-day rest period.

Renal impairment (CrCl 30-50 mL/min): 950 mg/m² twice daily (when starting dose is 1250 mg/m²). CrCl <30: Avoid use.

Hepatic impairment: Caution required; dose adjustment may be needed.

BSA calculation example: A person weighing 64 kg and height 1.64 m (BSA 1.7 m²) should take 4 tablets of 500 mg and 1 tablet of 150 mg twice daily.

Side effects

Common side effects: Vomiting, weakness, nausea, abdominal pain, diarrhea, blisters on fingers/feet (hand-foot syndrome), fatigue, loss of appetite, stomatitis (mouth inflammation), skin rash, dry/itchy skin, fever, infection, chest pain.

Serious (rare): Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), severe diarrhea (may lead to dehydration and renal failure), cardiotoxicity, hyperbilirubinemia, bone marrow suppression (neutropenia, thrombocytopenia).

Decreased blood cells (especially white blood cells) increase susceptibility to infections; monitor CBC regularly.

Use in pregnancy

Unsafe during pregnancy (Category D). Definite evidence of risk to the developing baby. Advise women of potential risk to the fetus. May be used in life-threatening situations if benefits outweigh risks. Use effective contraception during and after treatment.

Pregnancy Category: D — always consult a doctor before taking during pregnancy.

Precautions & warnings
  • Diarrhea: Stop treatment until diarrhea resolves to Grade 1; use standard antidiarrheal treatments. Severe diarrhea may lead to dehydration and renal failure.
  • Hand-foot syndrome: Interrupt treatment until symptoms resolve or decrease in intensity.
  • Cardiotoxicity: Common in patients with prior history of coronary artery disease; caution required.
  • Dehydration and renal failure: Stop treatment until dehydration is corrected; potential risk of acute renal failure.
  • DPD deficiency: Withhold or permanently discontinue in patients with evidence of acute early-onset or unusually severe toxicity (may indicate near complete or total absence of DPD activity).
  • Hematologic: Do not treat patients with neutrophil counts <1.5x10⁹/L or thrombocyte counts <100x10⁹/L.
  • Coagulopathy: Monitor anticoagulant response (INR) and adjust dose accordingly (risk of bleeding).
  • Do not use during pregnancy and lactation (Category D).
  • Know your response before driving (may cause dizziness and tiredness).
Overdose effects

Overdose symptoms: Nausea, vomiting, diarrhea, mucositis, gastrointestinal irritation and bleeding, bone marrow depression. Treatment: Supportive and symptomatic medical interventions aimed at correcting clinical manifestations and preventing complications.

Storage conditions

Store in a dry place below 30°C. Protect from light. Keep out of reach of children.

Capecitabine — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.