Description

Simple

A chemotherapy medication used to treat various types of cancers.

Clinical

A nucleoside metabolic inhibitor indicated to treat colon, colorectal and breast cancer.

Overview

Capecitabine is an orally-administered chemotherapeutic agent used in the treatment of metastatic breast and colorectal cancers. Capecitabine is a prodrug, that is enzymatically converted to fluorouracil (antimetabolite) in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue.

Pharmacology

Indication

For the treatment of patients with metastatic breast cancer resistant to both paclitaxel and an anthracycline-containing chemotherapy regimen. May also be used in combination with docetaxel for the treatment of metastatic breast cancer in patients who have failed to respond to, or recurred or relasp... Read more

Pharmacodynamic

Capecitabine is a fluoropyrimidine carbamate with antineoplastic activity indicated for the treatment of metastatic breast cancer and colon cancer. It is an orally administered systemic prodrug that has little pharmacologic activity until it is converted to fluorouracil by enzymes that are expressed... Read more

Mechanism of action

Capecitabine is a prodrug that is selectively tumour-activated to its cytotoxic moiety, fluorouracil, by thymidine phosphorylase, an enzyme found in higher concentrations in many tumors compared to normal tissues or plasma. Fluorouracil is further metabolized to two active metabolites, 5-fluoro-2'-d... Read more

Absorption

Readily absorbed through the GI tract (~70%)

Protein binding

< 60% (mainly albumin)

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

45-60 minutes for capecitabine and its metabolites.

Route of elimination

Capecitabine and its metabolites are predominantly excreted in urine; 95.5% of administered capecitabine dose is recovered in urine. Fecal excretion is minimal (2.6%). The major metabolite excreted in urine is FBAL which represents 57% of the administered dose.About 3% of the administered dose is ex... Read more

Toxicity

Information currently not available.

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Severe Renal Impairment
      • Drugbank Id: DBCOND0045819
      • Modification Of:
        • Base:
          • Name: Renal Impairment
          • Drugbank Id: DBCOND0031781
        • Severity:
          • Includes:
            • severe

Food Interactions

  • Take with food. Take within 30 minutes of the end of breakfast and dinner.

Interactions

Type in a drug name to check for interaction with Capecitabine
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(6R)-Folinic acid
The risk or severity of adverse effects can be increased when (6R)-Folinic acid is combined with Capecitabine.
(6S)-5,6,7,8-tetrahydrofolic acid
The risk or severity of adverse effects can be increased when (6S)-5,6,7,8-tetrahydrofolic acid is combined with Capecitabine.
(R)-warfarin
(R)-warfarin may increase the anticoagulant activities of Capecitabine.
(S)-Warfarin
(S)-Warfarin may increase the anticoagulant activities of Capecitabine.
2-Methoxyethanol
The risk or severity of adverse effects can be increased when Capecitabine is combined with 2-Methoxyethanol.
4-hydroxycoumarin
The risk or severity of bleeding can be increased when Capecitabine is combined with 4-hydroxycoumarin.
5-methyltetrahydrofolic acid
The risk or severity of adverse effects can be increased when 5-methyltetrahydrofolic acid is combined with Capecitabine.
9-(N-methyl-L-isoleucine)-cyclosporin A
The risk or severity of adverse effects can be increased when Capecitabine is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
Abacavir
Abacavir may decrease the excretion rate of Capecitabine which could result in a higher serum level.
Abatacept
The risk or severity of adverse effects can be increased when Capecitabine is combined with Abatacept.
Abciximab
The risk or severity of bleeding can be increased when Abciximab is combined with Capecitabine.
Abetimus
The risk or severity of adverse effects can be increased when Capecitabine is combined with Abetimus.
Acarbose
Acarbose may decrease the excretion rate of Capecitabine which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Capecitabine which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Capecitabine which could result in a higher serum level.
Acenocoumarol
Acenocoumarol may increase the anticoagulant activities of Capecitabine.
Acetaminophen
Acetaminophen may decrease the excretion rate of Capecitabine which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Capecitabine which could result in a lower serum level and potentially a reduction in efficacy.
Acetohexamide
The metabolism of Acetohexamide can be decreased when combined with Capecitabine.
Acetyldigitoxin
Acetyldigitoxin may decrease the cardiotoxic activities of Capecitabine.
6 References
  1. 1 . Walko CM, Lindley C: Capecitabine: a review. Clin Ther. 2005 Jan;27(1):23-44.PubMed: 15763604
  2. 2 . Wagstaff AJ, Ibbotson T, Goa KL: Capecitabine: a review of its pharmacology and therapeutic efficacy in the management of advanced breast cancer. Drugs. 2003;63(2):217-36.PubMed: 12515569
  3. 3 . Koukourakis GV, Kouloulias V, Koukourakis MJ, Zacharias GA, Zabatis H, Kouvaris J: Efficacy of the oral fluorouracil pro-drug capecitabine in cancer treatment: a review. Molecules. 2008 Aug 27;13(8):1897-922.PubMed: 18794792
  4. 4 . Twelves C: Vision of the future: capecitabine. Oncologist. 2001;6 Suppl 4:35-9.PubMed: 11585973
  5. 5 . Milano G, Ferrero JM, Francois E: Comparative pharmacology of oral fluoropyrimidines: a focus on pharmacokinetics, pharmacodynamics and pharmacomodulation. Br J Cancer. 2004 Aug 16;91(4):613-7.PubMed: 15280932
  6. 6 . de Bono JS, Twelves CJ: The oral fluorinated pyrimidines. Invest New Drugs. 2001;19(1):41-59.PubMed: 11291832