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.

Indication

Capecitabine is indicated as treatment for a variety of cancer types. For colorectal cancer, capecitabine is indicated as a single agent or a component of a combination chemotherapy regiment for the adjuvant treatment of stage III colon cancer and treatment unresectable or metastatic colorectal cancer. It can also be used as a part of a combination chemotherapy perioperative treatment of adult locally advanced rectal cancer. For breast cancer, capecitabine is indicated for advanced or metastatic breast cancer as a single agent if an anthracycline- or taxane-containing chemotherapy is not indicated or as a regimen with docetaxel after disease progression on prior anthracycline-containing chemotherapy. For gastric, esophageal, or gastroesophageal junction (GEJ) cancer, capecitabine is indicated as a component of a combination chemotherapy treatment for the treatment of adult unresectable or metastatic gastric, esophageal, or GEJ cancer or adult HER2-overexpressing metastatic gastric or GEJ adenocarcinoma who have not received prior treatment for metastatic disease. Finally, for pancreatic cancer, capecitabine is indicated as adjuvant treatment for adult pancreatic adenocarcinoma as a component of a combination chemotherapy regimen.

Associated Conditions

Advanced or Metastatic Breast Cancer
Carcinoma of Gallbladder
Cholangiocarcinoma
Hepatocellular Carcinoma
Locally Advanced Rectal Cancer (LARC)
Metastatic Adenocarcinoma of the Gastroesophageal Junction
Metastatic Gastric Cancers
Metastatic Neuroendocrine Tumors
Pancreatic Adenocarcinoma
Pancreatic Cancer, Advanced or Metastatic
Platinum-resistant Epithelial Ovarian Cancer
Refractory Fallopian Tube Carcinoma
Stage III Colon Cancer
Unresectable or Metastatic Colorectal Cancer
Metastatic pancreatic endocrine carcinoma
Refractory peritoneal cancer
Refractory, metastatic Colorectal carcinoma
Unresectable, metastatic Esophageal Cancer
Unresectable, metastatic Gastric Cancer
Unresectable, metastatic Gastroesophageal Junction Cancer

Research Report

Published: Jul 16, 2025

Capecitabine (DB01101): A Comprehensive Monograph on its Pharmacology, Clinical Efficacy, and Therapeutic Landscape

Executive Summary

Capecitabine is an orally administered fluoropyrimidine carbamate that has become a cornerstone chemotherapeutic agent in the modern oncology armamentarium.[1] Identified by DrugBank ID DB01101 and CAS Number 154361-50-9, it functions as a rationally designed, systemic prodrug that is relatively inert until it undergoes a multi-step enzymatic conversion to its active cytotoxic moiety, 5-fluorouracil (5-FU).[1] A key feature of its design is a tumor-selective activation process, driven by the higher concentrations of the enzyme thymidine phosphorylase in many malignant tissues compared to healthy ones. This mechanism is intended to generate high local concentrations of 5-FU at the site of malignancy, thereby enhancing the therapeutic index and mimicking the pharmacokinetic profile of a continuous 5-FU infusion without the associated complexities of intravenous administration.[1]

The clinical utility of capecitabine is well-established, with regulatory approvals from the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for a broad spectrum of solid tumors. Its primary indications include the adjuvant and metastatic treatment of colorectal cancer, the management of advanced or metastatic breast cancer, and integral roles in combination regimens for gastric, esophageal, and pancreatic cancers.[1]

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Clinical Trials

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Title	Posted	Study ID	Phase	Status	Sponsor
Induction Cetuximab (IM-C225), Gemcitabine, and Oxaliplatin in Pancreatic Cancer Patients	2006/06/20	NCT00338039	Phase 2	Completed	M.D. Anderson Cancer Center
E7389 Versus Capecitabine in Patients With Locally Advanced or Metastatic Breast Cancer Previously Treated With Anthracyclines and Taxanes	2006/06/15	NCT00337103	Phase 3	Completed	Eisai Inc.
S0425 Oxaliplatin, Capecitabine, and RT in Treating Patients W/Stomach Cancer That Can Be Removed By Surgery	2006/06/12	NCT00335959	Phase 2	Terminated	SWOG Cancer Research Network
Combination Study of a New Taxane and Capecitabine in Patients With Metastatic Breast Cancer	2006/05/18	NCT00327743	Phase 1	Completed	Sanofi
Tolerance and Pharmacokinetics With Capecitabine 5 Out of 7 Days Regimen	2006/05/11	NCT00324610	Phase 1	UNKNOWN	Association Pour La Recherche des Thérapeutiques Innovantes en Cancérologie
Bevacizumab, Radiation Therapy, and Combination Chemotherapy in Treating Patients Who Are Undergoing Surgery for Locally Advanced Nonmetastatic Rectal Cancer	2006/05/04	NCT00321685	Phase 2	Completed	National Cancer Institute (NCI)
Capecitabine, Docetaxel and Gemcitabine in Patients With Advanced Pancreas Cancer	2006/05/03	NCT00320749	Phase 1	Completed	Tony Bekaii-Saab
Combination of Cetuximab, Capecitabine, and Oxaliplatin With or Without Bevacizumab	2006/05/03	NCT00321100	Phase 2	Terminated	Fox Chase Cancer Center
Gemcitabine and Capecitabine in Patients With Advanced Pancreatic Cancer	2006/04/20	NCT00316420	Phase 1	Completed	Swedish Medical Center
Study of Bevacizumab Combined With Capecitabine and Either Oxaliplatin or Irinotecan as First Course of Treatment for Patients With Colorectal Cancer That Has Spread Beyond the Colon	2006/04/13	NCT00314353	Phase 2	Terminated	NSABP Foundation Inc

FDA Drug Approvals

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Approved Product	Manufacturer	NDC Code	Route	Strength	Effective Date
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EMA Drug Approvals

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Approved Product	Authorization Holder	Status	Issued Date
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HSA Drug Approvals

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NMPA Drug Approvals

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PPB Drug Approvals

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TGA Drug Approvals

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Health Canada Drug Approvals

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CIMA AEMPS Drug Approvals

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Philippines FDA Drug Approvals

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Saudi SFDA Drug Approvals

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Malaysia NPRA Drug Approvals

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UK EMC Drug Information

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