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
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]
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/09/17 | Not Applicable | Not yet recruiting | Sun Yat-sen University | ||
2025/09/10 | Not Applicable | Terminated | National Cancer Centre, Singapore | ||
2025/09/05 | Not Applicable | Not yet recruiting | |||
2025/09/04 | Not Applicable | Recruiting | |||
2025/09/04 | Not Applicable | Not yet recruiting | Sun Yat-sen University | ||
2025/09/03 | Not Applicable | Not yet recruiting | |||
2025/09/02 | Not Applicable | Recruiting | |||
2025/08/27 | Not Applicable | Completed | |||
2025/08/20 | Not Applicable | Not yet recruiting | First Affiliated Hospital of Guangxi Medical University | ||
2025/08/12 | Not Applicable | Recruiting | CSPC ZhongQi Pharmaceutical Technology Co., Ltd. |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Sun Pharmaceutical Industries, Inc. | 62756-238 | ORAL | 150 mg in 1 1 | 6/6/2023 | |
| Physicians Total Care, Inc. | 54868-5260 | ORAL | 500 mg in 1 1 | 6/7/2012 | |
| Dr. Reddy's Laboratories Limited | 55111-497 | ORAL | 500 mg in 1 1 | 12/21/2022 | |
| Golden State Medical Supply, Inc. | 51407-639 | ORAL | 150 mg in 1 1 | 4/19/2023 | |
| Physicians Total Care, Inc. | 54868-4143 | ORAL | 150 mg in 1 1 | 6/7/2012 | |
| Hikma Pharmaceuticals USA Inc. | 0054-0272 | ORAL | 500 mg in 1 1 | 5/8/2017 | |
| H2-Pharma, LLC | 61269-475 | ORAL | 500 mg in 1 1 | 4/14/2023 | |
| State of Florida DOH Central Pharmacy | 53808-0411 | ORAL | 500 mg in 1 1 | 5/20/2010 | |
| Golden State Medical Supply, Inc. | 51407-640 | ORAL | 500 mg in 1 1 | 4/19/2023 | |
| Accord Healthcare Inc. | 16729-072 | ORAL | 150 mg in 1 1 | 1/4/2024 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 2/2/2001 | ||
Authorised | 11/19/2012 | ||
Authorised | 4/20/2012 | ||
Authorised | 4/20/2012 | ||
Authorised | 4/20/2012 | ||
Authorised | 4/20/2012 | ||
Authorised | 4/20/2012 | ||
Authorised | 4/20/2012 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| CAPECITABINE ALVOGEN FILM COATED TABLETS 500 MG | SIN14580P | TABLET, FILM COATED | 500 mg | 7/31/2014 | |
| CAPETERO CAPECITABINE TABLETS 150MG | SIN14798P | TABLET | 150.00mg | 6/24/2015 | |
| XELODA TABLETS 150 mg | SIN10678P | TABLET, FILM COATED | 150 mg | 1/20/1999 | |
| CAPETERO CAPECITABINE TABLETS 500MG | SIN14799P | TABLET | 500.00mg | 6/24/2015 | |
| INCITABINE FILM COATED TABLET 150MG | SIN16264P | TABLET, FILM COATED | 150 mg | 7/6/2021 | |
| INCITABINE FILM COATED TABLET 500MG | SIN16265P | TABLET, FILM COATED | 500 mg | 7/6/2021 | |
| KAPETRAL FILM-COATED TABLET 150MG | SIN15368P | TABLET, FILM COATED | 150.000 mg | 11/29/2017 | |
| CAPECITABINE ALVOGEN FILM COATED TABLETS 150 MG | SIN14581P | TABLET, FILM COATED | 150.000 mg | 7/31/2014 | |
| INTACAPE FILM COATED TABLET 500 MG | SIN15464P | TABLET, FILM COATED | 500 mg | 4/10/2018 | |
| INTACAPE FILM COATED TABLET 150 MG | SIN15463P | TABLET, FILM COATED | 150 mg | 4/10/2018 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| INTACAPE 500 TABLETS 500MG | N/A | i & c (hong kong) limited | N/A | N/A | 5/14/2025 |
| INTACAPE 150 TABLETS 150MG | N/A | i & c (hong kong) limited | N/A | N/A | 5/14/2025 |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| Capecitabine Sandoz capecitabine 150mg film coated tablet blister pack | 201797 | Medicine | A | 1/31/2014 | |
| APO-CAPECITABINE capecitabine 500 mg tablet blister pack | 202741 | Medicine | A | 1/16/2014 | |
| CAPECITABINE-DRLA capecitabine 150 mg tablet blister pack | 200935 | Medicine | A | 6/24/2013 | |
| CAPECITABINE APOTEX capecitabine 150 mg tablet blister pack | 202726 | Medicine | A | 1/16/2014 | |
| CAPECCORD capecitabine 150 mg film-coated tablet blister pack | 213032 | Medicine | A | 7/22/2014 | |
| CAPECITABINE-DRLA capecitabine 500 mg tablet blister pack | 200933 | Medicine | A | 6/24/2013 | |
| CAPECCORD capecitabine 500 mg film-coated tablet blister pack | 213036 | Medicine | A | 7/22/2014 | |
| XELOCCORD capecitabine 150 mg film-coated tablet blister pack | 213038 | Medicine | A | 7/22/2014 | |
| APO-CAPECITABINE capecitabine 150 mg tablet blister pack | 202737 | Medicine | A | 1/16/2014 | |
| XELOCCORD capecitabine 500 mg film-coated tablet blister pack | 213044 | Medicine | A | 7/22/2014 |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| CAPECITABINE | sanis health inc | 02514990 | Tablet - Oral | 500 MG | 10/22/2021 |
| SANDOZ CAPECITABINE | 02421917 | Tablet - Oral | 150 MG | 7/23/2014 | |
| CAPECITABINE | 02519879 | Tablet - Oral | 150 MG | 6/15/2022 | |
| ACH-CAPECITABINE | 02426765 | Tablet - Oral | 500 MG | 9/19/2014 | |
| TEVA-CAPECITABINE | teva canada limited | 02400030 | Tablet - Oral | 500 MG | 8/19/2013 |
| MINT-CAPECITABINE | mint pharmaceuticals inc | 02508028 | Tablet - Oral | 500 MG | 10/5/2021 |
| APO-CAPECITABINE | 02434504 | Tablet - Oral | 150 MG | N/A | |
| APO-CAPECITABINE | 02434512 | Tablet - Oral | 500 MG | N/A | |
| ACH-CAPECITABINE | 02426757 | Tablet - Oral | 150 MG | 9/19/2014 | |
| XELODA | 02238454 | Tablet - Oral | 500 MG | 9/10/1998 |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| ZAPECINE 150 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | Zaphyr Pharmaceuticals Ireland Limited | 79672 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Diagnóstico Hospitalario | Not Commercialized |
| CAPECITABINA GLENMARK 150 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | 84871 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Diagnóstico Hospitalario | Commercialized | |
| XELCIP 500 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | Cipla Europe | 78583 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Diagnóstico Hospitalario | Not Commercialized |
| CAPECITABINA ACCORD 150 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | 112762005 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Diagnóstico Hospitalario | Not Commercialized | |
| CAPECITABINA GLENMARK 500 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | 84872 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Diagnóstico Hospitalario | Commercialized | |
| CAPECITABINA DR. REDDYS 500 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | Reddy Pharma Iberia S.A. | 81312 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Diagnóstico Hospitalario | Not Commercialized |
| XELCIP 150 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | Cipla Europe | 77860 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Diagnóstico Hospitalario | Not Commercialized |
| CAPECITABINA TARBIS 500 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | Tarbis Farma S.L. | 89071 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Diagnóstico Hospitalario | Commercialized |
| CAPECITABINA ACCORD 500 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | 112762027 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Diagnóstico Hospitalario | Commercialized | |
| CAPECITABINA AUROVITAS SPAIN 150 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | Aurovitas Spain, S.A.U. | 76946 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Diagnóstico Hospitalario | Not Commercialized |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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