Antineoplastic, oral prodrug of 5-FU
ATC code: L01BC06 (Capecitabine)
Brand names
Xeloda
Oral prodrug sequentially converted in the body by hepatic carboxylesterase → cytidine deaminase → thymidine phosphorylase (mainly in tumour tissue) into active 5-fluorouracil. Metabolism is tumour-selective – thymidine phosphorylase is often overexpressed in colorectal and breast cancer. Like 5-FU, catabolised by DPD – DPD deficiency leads to fatal toxicity.
First line
Capecitabine is an oral alternative to IV 5-FU in colorectal cancer (adjuvant and metastatic), breast and gastric cancer. ESMO 2024 includes capecitabine in CAPOX and CAPIRI regimens as a 5-FU substitute – outpatient convenience. DPD deficiency testing mandatory before starting.
2 pairs found. Sorted from critical to minor.
Mechanism
Capecitabine is a 5-FU prodrug, same fatal mechanism via brivudine DPD inhibition.
Symptoms
Severe myelosuppression, grade III hand-foot syndrome, mucositis, diarrhoea.
Management
Combination contraindicated. Minimum 4-week washout.
Mechanism
Capecitabine raises INR 4-fold or more via CYP2C9 inhibition – Xeloda Section 4.4 boxed warning.
Symptoms
Severe bleeding within first weeks of course.
Management
Check INR every 3-4 days. Switch to LMWH preferred.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
Strictly contraindicated. Contraception in men and women 6 months after withdrawal.
Breastfeeding contraindicated.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Capecitabine is evaluated for the following indications with varying evidence strength: Colorectal cancer (evidence tier A). See the full indication matrix with dosing and citations above on this page.
Common side effects of Capecitabine (≥ 1 in 100): Hand-foot syndrome (more frequent and severe than with 5-FU), Nausea, diarrhoea, Stomatitis, Fatigue, Myelosuppression. See the Safety section for uncommon and serious reactions.
FDA category D. Strictly contraindicated. Contraception in men and women 6 months after withdrawal.
Breastfeeding contraindicated.
Capecitabine is contraindicated in: Complete DPD deficiency; Combination with brivudine, sorivudine; Severe renal impairment (eGFR below 30 mL/min); Pregnancy; Known 5-FU hypersensitivity. Full list in the Safety section.