Antineoplastic, oral prodrug of 5-FU
Brand names: Xeloda
Updated · Methodology
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.
Sources
ICD-10: C18-C20 · ICD-11: 2B90-2B92
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.
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.
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.
Verbatim lines from the interaction sections, in the language of the label
«DRUG INTERACTIONS: • Allopurinol: Avoid concomitant use of allopurinol with capecitabine. ( 7.1 ) • Leucovorin: Closely monitor for toxicities when capecitabine is coadministered with leucovorin. (…»FDA, section 7 · Open on DailyMed
«DRUG INTERACTIONS: • Allopurinol: Avoid concomitant use of allopurinol with capecitabine. ( 7.1 ) • Leucovorin: Closely monitor for toxicities when capecitabine is coadministered with leucovorin. (…»FDA, section 7 · Open on DailyMed
«DRUG INTERACTIONS: • Allopurinol: Avoid concomitant use of allopurinol with capecitabine. ( 7.1 ) • Leucovorin: Closely monitor for toxicities when capecitabine is coadministered with leucovorin. (…»FDA, section 7 · Open on DailyMed
«Effect of Capecitabine on Other Drugs: CYP2C9 Substrates Capecitabine increased exposure of CYP2C9 substrates [see Clinical Pharmacology (12.3) ], which may increase the risk of adverse reactions…»FDA, section 7 · Open on DailyMed
«Nephrotoxic Drugs: Due of the additive pharmacologic effect, concomitant use of capecitabine with other drugs known to cause renal toxicity may increase the risk of renal toxicity [see Warnings and…»FDA, section 7 · Open on DailyMed
«Nephrotoxic Drugs: Due of the additive pharmacologic effect, concomitant use of capecitabine with other drugs known to cause renal toxicity may increase the risk of renal toxicity [see Warnings and…»FDA, section 7 · Open on DailyMed
«DRUG INTERACTIONS: • The following drugs may increase the risk of serious skin reactions: bendamustine, thiazide diuretics, ampicillin and amoxicillin. ( 7.1 ) • Capecitabine: Avoid concomitant use…»FDA, section 7 · Open on DailyMed
«Medicamentos afectados por la administración concomitante de ácido fólico: El ácido fólico puede potenciar la toxicidad de la capecitabina.»AEMPS, section 4.5 · Open on CIMA
«Drugs that Affect Phenytoin Concentrations: Antineoplastic agents Capecitabine, fluorouracil»FDA, section 7 · Open on DailyMed
«CYP450 Interactions: CYP2C9 amiodarone, capecitabine, cotrimoxazole, etravirine, fluconazole, fluvastatin, fluvoxamine, metronidazole, miconazole, oxandrolone, sulfinpyrazone, tigecycline…»FDA, section 7 · Open on DailyMed
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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.
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.
Direct links to regulator labels. Open in a new tab.
Everolimus, Fluorouracil, Methotrexate, Nintedanib, Sunitinib, Vincristine