pharmacopeia
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/api/v1/drug/capecitabine

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SERIOUS ADVERSE REACTIONS OR DEATH IN PATIENTS WITH COMPLETE DPD DEFICIENCY and BLEEDING WITH CONCOMITANT USE OF VITAMIN K ANTAGONISTS Increased risk of serious adverse reactions or death in patients with complete DPD deficiency Test patients for genetic variants of DPYD prior to initiating capecitabine tablets unless immediate treatment is necessary. Avoid use of capecitabine tablets in patients with certain homozygous or compound heterozygous DPYD variants that result in complete DPD deficiency [see Warnings and Precautions ( 5.1 )]. Increased risk of bleeding with concomitant use of Vitamin K antagonists Altered coagulation parameters and/or bleeding, including death, have been reported in patients taking c apecitabine tablets concomitantly with oral vitamin K antagonists, such as warfarin [see Warnings and Precautions ( 5.2 ) , Drug Interactions (7.2 ) ] . Clinically significant increases in prothrombin time (PT) and international normalized ratio (INR) have been reported in patients who were on stable doses of a vitamin K antagonist at the time capecitabine tablets was introduced. These events occurred in patients with and without liver metastases. Monitor INR more frequently and adjust the dose of the vitamin K antagonist as appropriate [see Drug Interactions (7.2) ] .

Mechanism of action

Sourced from openFDA

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).

Nucleic Acid SynthesisThymidylate Synthetase

Indications

Sourced from openFDA
  • Capecitabine tablet is 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.ICD-10: C18.9

Contraindications

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  • Capecitabine tablets are contraindicated in patients with history of severe hypersensitivity reaction to fluorouracil or capecitabine [see Adverse Reactions ( 6.1 )].contraindicated

Dosage & administration

Sourced from openFDA

Adjuvant Treatment of Colon Cancer • Single agent: 1,250 mg/m 2 twice daily orally for the first 14 days of each 21-day cycle for a maximum of 8 cycles. ( 2.1 ) In combination with Oxaliplatin-Containing Regimens: 1,000 mg/m 2 orally twice daily for the first 14 days of each 21-day cycle for a maximum of 8 cycles in combination with oxaliplatin 130 mg/m 2 administered intravenously on day 1 of each cycle. ( 2.2) Perioperative Treatment of Rectal Cancer • With Concomitant Radiation Therapy: 825 mg/m 2 orally twice daily ( 2.2 ) • Without Radiation Therapy: 1,250 mg/m 2 orally twice daily ( 2.2 ) Unresectable or Metastatic Colorectal Cancer: • Single agent: 1,250 mg/m 2 twice daily orally for the first 14 days of each 21-day cycle until disease progression or unacceptable toxicity. ( 2.2 ) • In Combination with Oxaliplatin: 1,000 mg/m 2 orally twice daily for the first 14 days of each 21-day cycle until disease progression or unacceptable toxicity in combination with oxaliplatin 130 mg/m 2 administered intravenously on day 1 of each cycle. ( 2.2 ) Advanced or Metastatic Breast Cancer: • Single agent: 1,000 mg/m 2 or 1,250 mg/m 2 twice daily orally for the first 14 days of each 21-day cycle until disease progression or unacceptable toxicity.

Warnings & precautions

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• Cardiotoxicity : May be more common in patients with a prior history of coronary artery disease. Withhold capecitabine tablets for cardiotoxicity as appropriate. The safety of resumption of capecitabine tablets in patients with cardiotoxicity that has resolved has not been established. ( 2.5 , 5.3 ) • Diarrhea : Withhold capecitabine tablets and then resume at same or reduced dose, or permanently discontinue, based on severity and occurrence. ( 2.5 , 5.4 ) • Dehydration : Optimize hydration before starting capecitabine tablets. Monitor hydration status and kidney function at baseline and as clinically indicated. Withhold capecitabine tablets and then resume at same or reduced dose, or permanently discontinue, based on severity and occurrence. ( 2.5 , 5.5 ) • Renal Toxicity : Monitor renal function at baseline and as clinically indicated. Optimize hydration before starting capecitabine tablets. Withhold capecitabine tablets and then resume at same or reduced dose, or permanently discontinue, based on severity and occurrence. ( 2.5 , 5.6 ) • Serious Skin Toxicities : Monitor for new or worsening serious skin reactions. Permanently discontinue capecitabine tablets in patients who experience a severe cutaneous adverse reaction. ( 5.7 ) • Palmar-Plantar Erythrodysesthesia Syndrome : Withhold capecitabine tablets then resume at same or reduced dose, or permanently discontinue, based on severity and occurrence. ( 2.5 , 5.8 ) • Myelosuppression : Monitor complete blood count at baseline and before each cycle.

Adverse reactions

Sourced from openFDA

The following clinically significant adverse reactions are described elsewhere in the labeling: Cardiotoxicity [see Warnings and Precautions ( 5.3 )] Diarrhea [see Warnings and Precautions ( 5.4 )] Dehydration [see Warnings and Precautions ( 5.5 )] Renal Toxicity [see Warnings and Precautions ( 5.6 )] Serious Skin Toxicities [see Warnings and Precautions ( 5.7 )] Palmar-Plantar Erythrodysesthesia Syndrome [see Warnings and Precautions ( 5.8 )] Myelosuppression [see Warnings and Precautions ( 5.9 )] Hyperbilirubinemia [see Warnings and Precautions ( 5.10 )] • Most common adverse reactions in patients who received capecitabine tablets as a single agent for the adjuvant treatment for colon cancer (>30%) were palmar-plantar erythrodysesthesia syndrome, diarrhea, and nausea. ( 6.1 ) • Most common adverse reactions (>30%) in patients with metastatic colorectal cancer who received capecitabine tablets as a single agent were anemia, diarrhea, palmar-plantar erythrodysesthesia syndrome, hyperbilirubinemia, nausea, fatigue, and abdominal pain. ( 6.1 ) • Most common adverse reactions (>30%) in patients with metastatic breast cancer who received capecitabine tablets with docetaxel were diarrhea, stomatitis, palmar-plantar erythrodysesthesia syndrome, nausea, alopecia, vomiting, edema, and abdominal pain. ( 6.1 ) • Most common adverse reactions (>30%) in patients with metastatic breast cancer who received capecitabine tablets as a single agent were lymphopenia, anemia, diarrhea, handand- foot syndrome, nausea, fatigue, vomiting, and dermatitis.

Use in specific populations

Sourced from openFDA

• Lactation : Advise not to breastfeed. ( 8.2 ) • Hepatic Impairment : Monitor patients with hepatic impairment more frequently for adverse reactions. (8.7) 8.1 Pregnancy Risk Summary Based on findings in animal reproduction studies and its mechanism of action [see Clinical Pharmacology ( 12.1 )], capecitabine tablets can cause fetal harm when administered to a pregnant woman. Available human data with capecitabine tablets use in pregnant women is not sufficient to inform the drug-associated risk. In animal reproduction studies, administration of capecitabine to pregnant animals during the period of organogenesis caused embryolethality and teratogenicity in mice and embryolethality in monkeys at 0.2 and 0.6 times the exposure (AUC) in patients receiving the recommended dose of 1,250 mg/m 2 twice daily, respectively (see Data). Advise pregnant women of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Pharmacokinetics

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Metabolism
The AUC of capecitabine and its metabolite 5’-DFCR increases proportionally over a dosage range of 500 mg/m 2 /day to 3,500 mg/m 2 /day (0.2 to 1.4 times the approved recommended dosage). The AUC of capecitabine’s metabolites 5’-DFUR and fluorouracil increased greater than proportional to the dose.

Overdosage

Sourced from openFDA

Administer uridine triacetate within 96 hours for management of capecitabine tablets overdose. Although no clinical experience using dialysis as a treatment for capecitabine tablets overdose has been reported, dialysis may be of benefit in reducing circulating concentrations of 5’-DFUR, a low– molecular-weight metabolite of the parent compound.

Approval history

Sourced from openFDA
  • Apr 30, 1998NDANDA020896Cheplapharm
  • Sep 16, 2013ANDAANDA091649Teva Pharms Usa
  • Apr 23, 2015ANDAANDA202593Accord Hlthcare
  • Dec 12, 2016ANDAANDA207456Shilpa
  • Nov 27, 2017ANDAANDA207652Alkem Labs Ltd
  • Apr 17, 2018ANDAANDA210604Eugia Pharma
  • Jul 2, 2018ANDAANDA209365Msn
  • Jun 21, 2019ANDAANDA204668Sun Pharm

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
90,022 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Diarrhoea13,52015%
  2. 2Death8,7809.8%
  3. 3Nausea8,3599.3%
  4. 4Palmar-plantar Erythrodysaesthesia Syndrome6,6167.3%
  5. 5Fatigue6,4047.1%
  6. 6Vomiting6,2066.9%
  7. 7Disease Progression6,0096.7%
  8. 8Malignant Neoplasm Progression3,9024.3%
  9. 9Off Label Use3,7594.2%
  10. 10Asthenia3,3633.7%
  11. 11Decreased Appetite3,2193.6%
  12. 12Neutropenia3,0823.4%
  13. 13Neuropathy Peripheral2,8313.1%
  14. 14Dehydration2,7353.0%
  15. 15Dyspnoea2,6432.9%

Literature

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Recent PubMed references pinned to Capecitabine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 2,695 ClinicalTrials.gov registrations naming Capecitabine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Capecitabine. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Frequently asked questions

How does Capecitabine work?
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).
What is Capecitabine used for?
According to FDA labeling, Capecitabine carries indications including: Capecitabine tablet is 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Capecitabine?
Capecitabine is classified as Pyrimidine analogues, Nucleoside Metabolic Inhibitor, Nucleic Acid Synthesis Inhibitors, Thymidylate Synthetase Inhibitors, Decreased DNA Integrity, Decreased RNA Integrity, Increased Cellular Death.
What are the brand names for Capecitabine?
Capecitabine is marketed under brand names including Xeloda.
What are the contraindications for Capecitabine?
Capecitabine labeling lists contraindications including: Capecitabine tablets are contraindicated in patients with history of severe hypersensitivity reaction to fluorouracil or capecitabine [see Adverse Reactions ( 6.1 )].. Always consult the full prescribing information and a clinician.
Note. Data for capecitabine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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