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Background
Capecitabine is an orally-administered chemotherapeutic agent used in the treatment of metastatic breast and colorectal cancers. It is a prodrug, that is enzymatically converted to fluorouracil (antimetabolite) in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue.
Properties and Characteristics of Capecitabine
| Drug class | Antimetabolites, Antineoplastics, chemotherapeutic agents |
| Brand Names | Ecansya, Xeloda |
| Synonyms | Capecitabin, Capecitabina, Capécitabine, Capecitabine, Capecitabinum |
| Molecular Formula | C15H22FN3O6 |
| Molecular Weight | 359.3501 g/mol |
| IUPAC Names | pentyl N-{1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-methyloxolan-2-yl]-5-fluoro-2-oxo-1,2-dihydropyrimidin-4-yl}carbamate |
| Structural formula of main components |  |
| Pure active ingredient | Capecitabine |
| Appearance | White to off-white crystalline powder |
| Melting point | 110-121 °C |
| Solubility | In water, 26 mg/mL at 20 °C |
| Excretion | Excreted in urine |
| Available as | Tablet |
| Storage | At room temperature between 68°F to 77°F (20°C to 25°C) |
| Prescription | Doctor prescription is required before consumption |
Uses of Capecitabine
Capecitabine is approved to be used alone or with other drugs to treat:
Breast cancer that has spread. It is used:
- Alone in patients whose cancer cannot be treated with an anthracycline or taxane chemotherapy drug.
- With docetaxel in patients whose cancer was treated with an anthracycline chemotherapy drug but it is no longer working.
Colorectal cancer. It is used:
- Alone or with other chemotherapy in patients who have had surgery to remove stage III colon cancer, to help keep the cancer from coming back after surgery.
- Around the time of surgery, with radiation therapy and other chemotherapy in adults whose rectal cancer has spread to nearby tissues.
- Alone or with other chemotherapy in patients whose colorectal cancer cannot be removed by surgery or has spread to other parts of the body.
Pancreatic adenocarcinoma. It is used with other chemotherapy drugs in adults who have had surgery to remove the cancer, to help keep the cancer from coming back after surgery.
Stomach (gastric) cancer, esophageal cancer, or gastroesophageal junction cancer in adults. It is used with other chemotherapy drugs when the cancer cannot be removed by surgery or has spread to other parts of the body.
Stomach (gastric) cancer or gastroesophageal junction cancer in adults. It is used when the cancer is HER2 positive, has spread to other parts of the body, and has not been treated with a chemotherapy regimen that included capecitabine.
Capecitabine is also being studied in the treatment of other types of cancer.
What are the possible side effects of Capecitabine?
Capecitabine may cause serious side effects including:
Diarrhea. Diarrhea is common with Capecitabine and can sometimes be severe. Stop taking Capecitabine and call your doctor right away if the number of bowel movements you have in a day increases by 4 or more than is usual for you. Ask your doctor about what medicines you can take to treat your diarrhea. If you have severe bloody diarrhea with severe abdominal pain and fever, call your doctor or go to the nearest emergency room right away.
Heart problems. Capecitabine can cause heart problems including: heart attack and decreased blood flow to the heart, chest pain, irregular heartbeats, changes in the electrical activity of your heart seen on an electrocardiogram (ECG), problems with your heart muscle, heart failure, and sudden death. Stop taking it and call your doctor right away if you get any of the following symptoms:
-
- Chest pain
- Shortness of breath
- Feeling faint
- Irregular heartbeats or skipping beats
- Sudden weight gain
- Swollen ankles or legs
Unexplained tiredness
Loss of too much body fluid (dehydration) and kidney failure. Dehydration can happen with Capecitabine and may cause sudden kidney failure that 45 can lead to death. You are at higher risk if you have kidney problems before taking it and also take other medicines that can cause kidney problems.
Nausea, and vomiting are common with Capecitabine. If you lose your appetite, feel weak, and have nausea, vomiting, or diarrhea, you can quickly become Dehydrated.
Stop taking Capecitabine and call your doctor right away if you:
- Vomit 2 or more times in a day.
- Are only able to eat or drink a little now and then, or not at all due to nausea.
- Have diarrhea. See “diarrhea” above.
Serious skin and mouth reactions.
- Capecitabine can cause serious skin reactions that may lead to death. Tell your doctor right away if you develop a skin rash, blisters and peeling of your skin. Your doctor may tell you to stop taking Capecitabine if you have a serious skin reaction. Do not take it again if this happens.
- Capecitabine can also cause “hand and foot syndrome.” Hand and foot syndrome is common with Capecitabine and can cause you to have numbness and changes in sensation in your hands and feet, or cause redness, pain, swelling of your hands and feet. Stop taking Capecitabine and call your doctor right away if you have any of these symptoms and you are not able to do your usual activities. Hand and foot syndrome can lead to loss of fingerprints which could impact your identification.
- You may get sores in your mouth or on your tongue when taking Capecitabine. Stop taking it and call your doctor if you get painful redness, swelling, or ulcers in your mouth and tongue, or if you are having problems eating. Tell your doctor if you have any side effect that bothers you or that does not go away.
- Increased level of bilirubin in your blood and liver problems. Increased bilirubin in your blood is common with Capecitabine. Your doctor will check you for these problems during treatment with Capecitabine.
- Decreased white blood cells, platelets, and red blood cell counts. Your doctor will do blood tests during treatment with Capecitabine to check your blood cell counts.
If your white blood cell count is very low, you are at increased risk for infection. Call your doctor right away if you develop a fever of 100.5º F or greater or have other signs and symptoms of infection. People 80 years of age or older may be more likely to develop severe or serious side effects with Capecitabine.
What are the most common side effects of Capecitabine?
The most common side effects of Capecitabine include:
- Diarrhea
- Hand and foot syndrome
- Nausea
- Vomiting
- Stomach-area (abdominal) pain
- Tiredness
- Weakness
- Increased amounts of red blood cell breakdown products (bilirubin) in your blood
If you have any questions about your condition or treatment, talk to your doctor.
Drug Interactions
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.
- Measles Virus Vaccine, Live
- Mumps Virus Vaccine, Live
- Rotavirus Vaccine, Live
- Rubella Virus Vaccine, Live
- Tegafur
- Varicella Virus Vaccine, Live
- Zoster Vaccine, Live
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Aceclofenac
- Acenocoumarol
- Adenovirus Vaccine
- Allopurinol
- Azanidazole
- Bacillus of Calmette and Guerin Vaccine, Live
- Benznidazole
- Brivudine
- Carvedilol
- Cedazuridine
What other drugs interact with Capecitabine?
If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.
Capecitabine has no known severe interactions with other drugs.
Serious interactions of capecitabine include:
- Adenovirus type 4 and 7 live, oral
- Enoxaparin
- Influenza virus vaccine trivalent, adjuvanted
- Palifermin
- Tofacitinib
- Warfarin
Capecitabine has moderate interactions with 32 different drugs.
Minor interactions of capecitabine include:
- Food
- Maitake
- Taurine
- Vitamin A
- Vitamin E
This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist.
Mechanism of Action
Capecitabine is a prodrug that is selectively tumour-activated to its cytotoxic moiety, fluorouracil, by thymidine phosphorylase. Fluorouracil is further metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP), within normal and tumour cells. FdUMP inhibits DNA synthesis by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate. The active moiety of capecitabine, fluorouracil, is cell cycle phase-specific (Sphase).
Capecitabine Dosage
Take capecitabine exactly as prescribed by your doctor. Follow the directions on your prescription label carefully. Your doctor will determine the best dose for you.
Standard Starting Dose
- The recommended dose of capecitabine is 1250 mg/m2 given by mouth twice daily for 2 weeks. This is followed by by a 1-week rest period.
- In those with Dukes’ C colon cancer is recommended for a total of 6 months.
In Combination with Docetaxel (Metastatic Breast Cancer)
- The recommended dose of capecitabine is 1250 mg/m2 twice daily for 2 weeks. This is followed by a 1-week rest period.
- You will be carefully monitored for toxicity.
- Doses of capecitabine should be adjusted as necessary to accommodate tolerance to treatment.
Capecitabine Overdose
If you take too much capecitabine call your healthcare provider or local Poison Control Center or seek emergency medical attention right away.
If capecitabine is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if an overdose is suspected, seek emergency medical attention.
What special precautions should I follow?
Before taking capecitabine,
- Tell your doctor and pharmacist if you are allergic to capecitabine, fluorouracil (Adrucil, 5-FU), any other medications, or any of the ingredients in capecitabine tablets. Ask your pharmacist for a list of the ingredients.
- Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention the medications listed in the IMPORTANT WARNING section and any of the following: allopurinol (Aloprim, Lopurin, Zyloprim), leucovorin, and phenytoin (Dilantin). Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Other medications may also interact with capecitabine, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
- Talk to your doctor about whether testing for dihydropyrimidine dehydrogenase (DPD) enzyme deficiency (a lack of a naturally occurring enzyme in your body) should be done prior to starting capecitabine. Tell your doctor if you have been told that you have or ever had DPD enzyme deficiency. Your doctor may probably tell you not to take capecitabine.
- Tell your doctor if you have or have ever had kidney, liver, or heart disease.
- Tell your doctor if you are pregnant or plan to become pregnant. You should not plan to have children while you are taking capecitabine. You should use a reliable method of birth control to prevent pregnancy in yourself or your partner during your treatment with capecitabine. Capecitabine may harm the fetus.tell your doctor if you are breast-feeding. You should not breast-feed during your treatment with capecitabine.
Capecitabine and Pregnancy
Tell your doctor if you are pregnant or think you may be pregnant.
The FDA categorizes medications based on safety for use during pregnancy. Five categories – A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.
This medication falls into category D. Capecitabine may harm your unborn child. Use effective birth control while taking capecitabine.
Capecitabine and Lactation
Tell your doctor if you are breastfeeding or plan to breastfeed. It is not known if capecitabine is excreted in human breast milk or if it will harm your nursing baby.
