Dosing & Uses
Dosage Forms & Strengths
tablet
- 150mg
- 500mg
Colorectal Cancer
Adjuvant treatment for colon cancer
- Indicated as a single agent for adjuvant treatment in patients with Dukes’ C colon cancer who have undergone complete resection of the primary tumor when treatment with fluoropyrimidine therapy alone is preferred
- Capecitabine was noninferior to 5fluorouracil and leucovorin (5-FU/LV) for disease-free survival; consider results of combination chemotherapy trials, which have shown improvement in disease-free and overall survival, when prescribing single-agent capecitabine in the adjuvant setting
- 1,250 mg/m2 PO BID x 2 weeks, followed by 1-week rest period, given as 3-week cycles for a total of 8 cycles (24 weeks)
First-line monotherapy for metastatic colorectal carcinoma
- Indicated as first-line treatment of metastatic colorectal carcinoma (CRC) when treatment with fluoropyrimidine therapy alone is preferred
- Combination chemotherapy has shown a survival benefit compared with 5-FU/LV alone; survival benefit over 5-FU/LV has not been demonstrated with capecitabine monotherapy; use of capecitabine instead of 5 FU/LV in combinations has not been adequately studied to assure safety or preservation of survival advantage
- 1250 mg/m2 BID x 2 weeks, followed by 1-week rest period, given as 3-week cycles
Breast Cancer
Monotherapy
- Indicated for patients with metastatic breast cancer resistant to both paclitaxel and an anthracycline-containing chemotherapy regimen or resistant to paclitaxel for whom further anthracycline therapy is not indicated (eg, patients who have received cumulative doses of 400 mg/m2 of doxorubicin or doxorubicin equivalents)
- 1250 mg/m2 BID x 2 weeks, followed by 1-week rest period, given as 3-week cycles
Combination with docetaxel
- Indicated in combination with docetaxel for metastatic breast cancer after failure of prior anthracycline-containing chemotherapy
- 1250 mg/m2 PO BID on Days 1-14 plus docetaxel 75 mg/m2 1 hr IV infusion on Day 1 of a 3-week cycle
Dosage Modifications
Grade 1 toxicities: Maintain dose level
Grade 2 toxicities
- 1st occurrence: Interrupt until resolved to grade 0-1; maintain dose
- 2nd occurrence: Interrupt until resolved to grade 0-1; decrease dose to 75% of starting dose
- 3rd occurrence: Interrupt until resolved to grade 0-1; decrease dose to 50% of starting dose
- 4th occurrence: Discontinue permanently
Grade 3 toxicities
- 1st occurrence: Interrupt until resolved to grade 0-1; decrease dose to 75% of starting dose
- 2nd occurrence: Interrupt until resolved to grade 0-1; decrease dose to 50% of starting dose
- 3rd occurrence: Discontinue permanently
Grade 4 toxicities
- Discontinue permanently, OR
- If physician deems it to be in the patient’s best interest to continue, interrupt until resolved to grade 0-1 and decrease dose by 50%
Renal impairment
- Mild (CrCl 51-80 mL/min): No dose reduction necessary
- Moderate (CrCl 30-50 mL/min): Reduce dose to 75% of starting dose (ie, from 1250 mg/m2 to 950 mg/m2 BID)
- Severe (CrCl <30 mL/min): Contraindicated
Hepatic impairment
- Mild-to-moderate: Caution when patients with hepatic dysfunction owing to liver metastases treated with capecitabine
- Severe: Unknown
Safety & efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (19)
- adenovirus types 4 and 7 live, oral
capecitabine decreases effects of adenovirus types 4 and 7 live, oral by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressives may diminish therapeutic effects of vaccines and increase risk of adverse effects (increased risk of infection). Live-attenuated vaccines should be avoided for at least 3mo after cessation of immunosuppressive therapy.
- axicabtagene ciloleucel
capecitabine, axicabtagene ciloleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- brexucabtagene autoleucel
capecitabine, brexucabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- cedazuridine
cedazuridine will increase the level or effect of capecitabine by decreasing metabolism. Avoid or Use Alternate Drug. Cedazuridine, a CDA inhibitor, is used with decitabine to increase systemic exposure of decitabine. Use with other drugs metabolized by CDA may increase levels and toxicities of those drugs.
- ciltacabtagene autoleucel
capecitabine, ciltacabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- deferiprone
deferiprone, capecitabine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.
- enoxaparin
capecitabine increases effects of enoxaparin by unspecified interaction mechanism. Avoid or Use Alternate Drug. An additive risk of bleeding with enoxaparin may be seen in thrombocytopenic patients receiving antineoplastic agents like capecitabine.
- erdafitinib
capecitabine will increase the level or effect of erdafitinib by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP2C9 inhibitors, monitor closely for adverse reactions and consider decreasing dose accordingly. If strong CYP2C9 inhibitor is discontinued, consider increasing erdafitinib dose in the absence of any drug-related toxicities.
- fexinidazole
fexinidazole and capecitabine both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels or prolong QT interval.
- idecabtagene vicleucel
capecitabine, idecabtagene vicleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- influenza virus vaccine quadrivalent, adjuvanted
capecitabine decreases effects of influenza virus vaccine quadrivalent, adjuvanted by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressive drugs may reduce the immune response to influenza vaccine.
- influenza virus vaccine trivalent, adjuvanted
capecitabine decreases effects of influenza virus vaccine trivalent, adjuvanted by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressive drugs may reduce the immune response to influenza vaccine.
- lefamulin
lefamulin and capecitabine both increase QTc interval. Avoid or Use Alternate Drug.
- lisocabtagene maraleucel
capecitabine, lisocabtagene maraleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- palifermin
palifermin increases toxicity of capecitabine by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hrbefore, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
- ropeginterferon alfa 2b
ropeginterferon alfa 2b, capecitabine. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Myelosuppressive agents can produce additive myelosuppression. Avoid use and monitor patients receiving the combination for effects of excessive myelosuppression.
- siponimod
capecitabine will increase the level or effect of siponimod by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. Coadministration of siponimod with drugs that cause moderate CYP2C9 AND a moderate or strong CYP3A4 inhibition is not recommended. Caution if siponimod coadministered with moderate CYP2C9 inhibitors alone.
- tisagenlecleucel
capecitabine, tisagenlecleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- tofacitinib
capecitabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
Monitor Closely (61)
- aluminum hydroxide
aluminum hydroxide increases levels of capecitabine by enhancing GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- antithrombin alfa
capecitabine increases effects of antithrombin alfa by unspecified interaction mechanism. Use Caution/Monitor.
- antithrombin III
capecitabine increases effects of antithrombin III by unspecified interaction mechanism. Use Caution/Monitor.
- argatroban
capecitabine increases effects of argatroban by unspecified interaction mechanism. Use Caution/Monitor.
- arsenic trioxide
capecitabine and arsenic trioxide both increase QTc interval. Use Caution/Monitor.
- bedaquiline
capecitabine and bedaquiline both increase QTc interval. Use Caution/Monitor.
- belatacept
belatacept and capecitabine both increase immunosuppressive effects; risk of infection. Use Caution/Monitor.
- bivalirudin
capecitabine increases effects of bivalirudin by unspecified interaction mechanism. Use Caution/Monitor.
- chlorpromazine
capecitabine and chlorpromazine both increase QTc interval. Use Caution/Monitor.
- cholera vaccine
capecitabine decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Immunosuppressive therapies, including irradiation, antimetabolites, alkylating agents, cytotoxic drugs and corticosteroids (used in greater than physiologic doses), may reduce the immune response to cholera vaccine.
- cisapride
capecitabine and cisapride both decrease QTc interval. Use Caution/Monitor.
- dalteparin
capecitabine increases effects of dalteparin by unspecified interaction mechanism. Use Caution/Monitor.
- dengue vaccine
capecitabine decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Immunosuppressive therapies (eg, irradiation, antimetabolites, alkylating agents, cytotoxic drugs, corticosteroids [greater than physiologic doses]) may reduce immune response to dengue vaccine.
- denosumab
capecitabine, denosumab. Other (see comment). Use Caution/Monitor. Comment: Caution should be taken in patients on concomitant immunosuppressants or with impaired immune systems because of increased risk for serious infections.
- dichlorphenamide
dichlorphenamide and capecitabine both decrease serum potassium. Use Caution/Monitor.
- diclofenac
capecitabine will increase the level or effect of diclofenac by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. Do not exceed diclofenac dose of 50 mg BID
- disopyramide
capecitabine and disopyramide both increase QTc interval. Use Caution/Monitor.
- dofetilide
capecitabine and dofetilide both increase QTc interval. Use Caution/Monitor.
- dronabinol
capecitabine will increase the level or effect of dronabinol by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. Dronabinol is a CYP2C9 substrate.
- eluxadoline
capecitabine increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- ethotoin
capecitabine increases levels of ethotoin by unknown mechanism. Use Caution/Monitor. Based on case reports.
- fingolimod
capecitabine increases effects of fingolimod by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Concomitant therapy is expected to increase the risk of immunosuppression. Use caution when switching patients from long-acting therapies with immune effects. .
- fondaparinux
capecitabine increases effects of fondaparinux by unspecified interaction mechanism. Use Caution/Monitor.
- fosphenytoin
capecitabine increases levels of fosphenytoin by unknown mechanism. Use Caution/Monitor. Based on case reports.
- fostemsavir
capecitabine and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.
- gilteritinib
gilteritinib and capecitabine both increase QTc interval. Use Caution/Monitor.
- glyburide
capecitabine increases levels of glyburide by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. Strong CYP2C9 inhibitors may decrease glyburide metabolism.
- goserelin
capecitabine and goserelin both increase QTc interval. Use Caution/Monitor.
- haloperidol
capecitabine and haloperidol both increase QTc interval. Use Caution/Monitor.
- heparin
capecitabine increases effects of heparin by unspecified interaction mechanism. Use Caution/Monitor.
- histrelin
capecitabine and histrelin both increase QTc interval. Use Caution/Monitor.
- ibutilide
capecitabine and ibutilide both increase QTc interval. Use Caution/Monitor.
- influenza A (H5N1) vaccine
capecitabine decreases effects of influenza A (H5N1) vaccine by Mechanism: pharmacodynamic antagonism. Use Caution/Monitor. Immunosuppressive therapies may reduce immune response to H5N1 vaccine.
- influenza virus vaccine (H5N1), adjuvanted
capecitabine decreases effects of influenza virus vaccine (H5N1), adjuvanted by Mechanism: pharmacodynamic antagonism. Use Caution/Monitor. Immunosuppressive therapies may reduce immune response to H5N1 vaccine.
- lacosamide
capecitabine increases levels of lacosamide by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely. Consider decreasing lacosamide dose when coadministered with strong CYP2C9 inhibitors.
- lenvatinib
capecitabine and lenvatinib both increase QTc interval. Use Caution/Monitor.
- lesinurad
capecitabine will increase the level or effect of lesinurad by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.
- leucovorin
leucovorin increases effects of capecitabine by pharmacodynamic synergism. Use Caution/Monitor.
- meningococcal group B vaccine
capecitabine decreases effects of meningococcal group B vaccine by pharmacodynamic antagonism. Use Caution/Monitor. Individuals with altered immunocompetence may have reduced immune responses to the vaccine.
- methadone
capecitabine and methadone both increase QTc interval. Use Caution/Monitor.
- ofatumumab SC
ofatumumab SC, capecitabine. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.
- olaparib
capecitabine and olaparib both increase pharmacodynamic synergism. Use Caution/Monitor. Coadministration with other other myelosuppressive anticancer agents, including DNA damaging agents, may potentiate and prolongate the myelosuppressive toxicity.
- olodaterol inhaled
capecitabine and olodaterol inhaled both increase QTc interval. Use Caution/Monitor.
- osilodrostat
osilodrostat and capecitabine both increase QTc interval. Use Caution/Monitor.
- ospemifene
capecitabine increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.
- phenytoin
capecitabine increases levels of phenytoin by unknown mechanism. Use Caution/Monitor. Based on case reports.
- procainamide
capecitabine and procainamide both increase QTc interval. Use Caution/Monitor.
- protamine
capecitabine increases effects of protamine by unspecified interaction mechanism. Use Caution/Monitor.
- quinidine
capecitabine and quinidine both increase QTc interval. Use Caution/Monitor.
- quinine
capecitabine and quinine both increase QTc interval. Use Caution/Monitor.
- selpercatinib
capecitabine and selpercatinib both increase QTc interval. Use Caution/Monitor.
- siponimod
siponimod and capecitabine both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
- sipuleucel-T
capecitabine decreases effects of sipuleucel-T by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
- sodium citrate/citric acid
sodium citrate/citric acid increases levels of capecitabine by enhancing GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- terbinafine
capecitabine will increase the level or effect of terbinafine by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.
- trastuzumab
trastuzumab, capecitabine. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- trastuzumab deruxtecan
trastuzumab deruxtecan, capecitabine. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- vandetanib
capecitabine and vandetanib both increase QTc interval. Use Caution/Monitor.
- voclosporin
capecitabine and voclosporin both increase QTc interval. Use Caution/Monitor.
- warfarin
capecitabine will increase the level or effect of warfarin by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely. Closely monitor INR and PT and adjust dose. Increased INR and PT can occur within a few days of initiating capecitabine.
- ziprasidone
capecitabine and ziprasidone both increase QTc interval. Use Caution/Monitor.
Minor (5)
- food
food decreases levels of capecitabine by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown. Food has shown to reduce both the rate and extent of absorption of capecitabine.
- maitake
maitake increases effects of capecitabine by pharmacodynamic synergism. Minor/Significance Unknown. Maitake mushroom has anti-tumor effects (animal/in vitro research).
- taurine
capecitabine decreases levels of taurine by unspecified interaction mechanism. Minor/Significance Unknown.
- vitamin A
vitamin A, capecitabine. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Antioxidants such as vitamin A enhance the efficacy, and reduce toxicity, of antineoplastic drugs.
- vitamin E
vitamin E, capecitabine. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Antioxidants such as vitamin E enhance the efficacy, and reduce toxicity, of antineoplastic drugs.
Adverse Effects
Varies with carcinoma type
10%
Diarrhea
Nausea
Anemia
Lymphopenia
Hand and foot syndrome
Edema
Fatigue
Fever
Headache
Pain
Paresthesia
Alopecia
Dermatitis
Abdominal pain
Anorexia
Appetite decreased
Constipation
Dyspepsia
Stomatitis
Vomiting
Neutropenia
Thrombocytopenia
Dyspnea
Bilirubin increased
Eye irritation
1-10%
Chest pain
Dermatitis
Pruritus
Rash
Dizziness
Headache
Weakness
Dehydration
Dry mouth
Dyspepsia
Taste disturbance
Back pain
Postmarketing reports
Toxic leukoencephalopathy
Angioedema
Warnings
Black Box Warnings
Anticoagulant interactions
- Monitor INR or prothrombin time frequently if coadministered with oral coumarin-derivative anticoagulants (eg, warfarin); adjust warfarin dose accordingly
- Altered coagulation parameters and/or bleeding, including death, reported during concomitant use
- Occurrence: Within several days and up to several months after initiating capecitabine; may also observe within 1 month after discontinuing capecitabine
- Predisposing factors: Age >60 years; cancer
Contraindications
Hypersensitivity to capecitabine or fluorouracil (5-FU)
Severe renal impairment (CrCl <30 mL/min)
Cautions
May result in bleeding, death; monitor anticoagulant response (eg, INR, PT) and adjust anticoagulant dose accordingly
Diarrhea may be severe; interrupt capecitabine treatment immediately until diarrhea resolves or decreases to grade 1; recommend standard antidiarrheal treatments
Cardiotoxicity observed, including MI/ischemia, angina, dysrhythmias, cardiac arrest, cardiac failure, sudden death, ECG changes, and cardiomyopathy; more common with history of coronary artery disease
Increased risk of severe or fatal adverse reactions in patients with low or absent dihydropyrimidine dehydrogenase (DPD) activity; withhold or permanently discontinue capecitabine in patients with evidence of acute early-onset or unusually severe toxicity, which may indicate near complete or total absence of DPD activity; no capecitabine dose has been proven safe in patients with absent DPD activity
Interrupt capecitabine treatment until dehydration is corrected; potential risk of acute renal failure secondary to dehydration; monitor and correct dehydration
Can cause fetal harm; advise women of the potential risk to the fetus
Severe mucocutaneous reactions, Steven-Johnson Syndrome (SJS) and Toxic Epidermal Necrolysis (TEN), reported; discontinue therapy in patients who experience a severe mucocutaneous reaction during treatment; capecitabine may induce hand-and-foot syndrome; interrupt capecitabine treatment until hand-and-foot syndrome event resolves or decreases in intensity; persistent or severe hand-and-foot syndrome can eventually lead to loss of fingerprints
Hyperbilirubinemia reported; interrupt therapy immediately until it resolves or decreases in intensity
Do not treat patients with baseline neutrophil counts <1.5 x 109;/L or thrombocyte counts <100 x 109;/L; if grade 3-4 neutropenia or thrombocytopenia occurs, stop therapy until condition resolves
Caution in geriatric patients; greater risk of grade 3 or 4 adverse reactions
Monitor carefully with mild-to-moderate hepatic dysfunction owing to liver metastases; effect of severe hepatic dysfunction on capecitabine disposition unknown
Use in combination with irinotecan has not been adequately studied
Drug interaction overview
-
Warfarin
- Monitor INR and PT frequently; modify warfarin dose accordingly
- Increased INR/PT observed with coadministration; presumed mechanism is CYP2C9 inhibition by capecitabine
-
Phenytoin
- Monitor phenytoin level frequently; phenytoin dose may need to be reduced
- Presumed mechanism is CYP2C9 inhibition by capecitabine
-
Leucovorin
- 5-FU, an active metabolite of capecitabine, is increased and its toxicity may be enhanced by leucovorin
- Deaths from severe enterocolitis, diarrhea, and dehydration reported in older patients receiving weekly leucovorin and 5-FU
-
CYP2C9 substrates
- Caution if coadministered with CYP2C9 substrates
- Other than warfarin, formal drug-drug interaction studies have not been conducted with other CYP2C9 substrates
-
Allopurinol
- Avoid coadministration
- Coadministration may decrease concentration of capecitabine’s active metabolites
Pregnancy & Lactation
Pregnancy
Based on findings in animal reproduction studies and its mechanism of action, fetal harm may occur when administered to pregnant females; limited available human data are not sufficient to inform drug-associated risk during pregnancy
Pregnancy testing recommended for females of reproductive potential before initiating therapy
Animal studies
- Therapy in pregnant animals during organogenesis caused embryo lethality and teratogenicity in mice and embryo lethality in monkeys at 0.2 and 0.6 times, respectively, the exposure (AUC) in patients
Contraception
- Females of reproductive potential: Use effective contraception during treatment and for 6 months after last dose
- Males with female partners of reproductive potential: Use effective contraception during treatment and for 3 months after last dose
Infertility
- Based on animal studies, may impair fertility in females and males
Lactation
Data are unavailable regarding presence in human milk, effects on milk production, or effects on breastfed infants; drug metabolites were present in milk of lactating mice
Owing to potential for serious adverse reactions from exposure in breastfed infants, advise females not to breastfeed during therapy and for 2 weeks after final dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Fluoropyrimidine carbamate with antineoplastic activity; it is a prodrug of 5’-deoxy-5-fluorouridine (F'-DFCR), which is then converted to 5-fluorouracil (5-FU)
Both normal and tumor cells metabolize 5-FU to 5-fluoro-2’-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP)
FdUMP and FUTP
- These metabolites cause cell injury by 2 different mechanisms
- First, FdUMP and the folate cofactor, N5-10-methylenetetrahydrofolate, bind to thymidylate synthase to form a covalently bound ternary complex; this binding inhibits thymidylate formation from 2’-deoxyuridylate; thymidylate is the necessary precursor of thymidine triphosphate, which is essential for DNA synthesis, so that a deficiency of this compound can inhibit cell division
- Second, nuclear transcriptional enzymes can mistakenly incorporate FUTP in place of uridine triphosphate (UTP) during RNA synthesis; this metabolic error can interfere with RNA processing and protein synthesis
Absorption
Peak Plasma Time: 1.5 hr (capecitabine); 2 hr (5-FU)
Food
- Food reduces both rate and extent of capecitabine absorption of capecitabine
- In all clinical trials, patients were instructed to administer capecitabine within 30 minutes after a meal
- Recommended to administer with food
Distribution
Protein bound: <60% (primary to albumin ~35%)
Metabolism
Enzymatic metabolism to 5-FU
- In the liver, carboxylesterase hydrolyzes much of the compound to 5’-DFCR
- Cytidine deaminase (in most tissues, including tumors) subsequently converts 5’-DFCR to 5’-DFUR
- Thymidine phosphorylase then hydrolyzes 5’-DFUR to active drug 5-FU
Elimination
Half-life: 0.75 hr (parent capecitabine and 5-FU)
Excretion: urine (95%)
Dialyzable: yes
Pharmacogenomics
Dihydropyrimidine dehydrogenase (DPD), an enzyme encoded by the DPYD gene, is the rate-limiting step in pyrimidine catabolism and deactivates >80% of 5FU standard doses and the 5-FU prodrug capecitabine
Contraindicated in patients with DPD deficiency; causes severe toxicity with conventional doses (ie, grade III/IV toxicity and potentially fatal neutropenia, mucositis, and diarrhea)
Because true DPD deficiency is rare and the clinical implications of partial deficiency are still unclear, screening for mutations before initiating therapy is not warranted
Administration
Oral Administration
Swallow tablets whole with water within 30 minutes after a meal
If tablets must be cut or crushed, this should be done by a professional trained in safe handling of cytotoxic drugs using appropriate equipment and safety procedures
Storage
Store at 25ºC (77ºF); excursions permitted to 15-30ºC (59-86ºF)
Keep container tightly closed
Follow applicable special handling and disposal procedures for cytotoxic drugs
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| capecitabine oral - | 500 mg tablet |  | |
| capecitabine oral - | 150 mg tablet |  | |
| capecitabine oral - | 500 mg tablet |  | |
| capecitabine oral - | 150 mg tablet |  | |
| capecitabine oral - | 150 mg tablet |  | |
| capecitabine oral - | 500 mg tablet |  | |
| capecitabine oral - | 150 mg tablet |  | |
| capecitabine oral - | 500 mg tablet |  | |
| capecitabine oral - | 500 mg tablet |  | |
| capecitabine oral - | 500 mg tablet |  | |
| capecitabine oral - | 500 mg tablet |  | |
| capecitabine oral - | 150 mg tablet |  | |
| capecitabine oral - | 150 mg tablet |  | |
| capecitabine oral - | 150 mg tablet |  | |
| Xeloda oral - | 500 mg tablet |  | |
| Xeloda oral - | 150 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
capecitabine oral
CAPECITABINE - ORAL
(KAP-e-SYE-ta-been)
COMMON BRAND NAME(S): Xeloda
WARNING: People taking capecitabine along with certain "blood thinners" (anticoagulants such as warfarin or phenprocoumon) may have a higher chance of serious, rarely fatal bleeding. Your risk may be higher because you have cancer, or if you are older than 60 years. Bleeding has occurred during treatment and as long as one month after stopping capecitabine.If you are using an anticoagulant, blood lab tests (INR/PT) will be closely checked. Tell your doctor right away if you have any signs of bleeding or bruising (such as bloody/black/tarry stools). You should be tested for a DPD enzyme deficiency before you start treatment with capecitabine. Ask your doctor for more details.
USES: Capecitabine is used to treat breast, colon, or rectal cancer. It works by slowing or stopping the growth of cancer cells.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking capecitabine and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth as directed by your doctor, usually 2 times a day; once in the morning and once in the evening. Swallow the tablets whole with a full glass of water (8 ounces/240 milliliters) within 30 minutes after a meal. Do not crush or split the tablets. If you have trouble swallowing the tablets whole, ask your health care professional for advice. Your doctor may direct you to take this medication in a treatment cycle. Carefully follow your doctor's instructions.The dosage is based on your medical condition, body size, and response to treatment. Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of side effects will increase.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.
SIDE EFFECTS: Nausea, vomiting, loss of appetite, constipation, tiredness, weakness, headache, dizziness, trouble sleeping, or changes in taste may occur. Nausea and vomiting can be severe. In some cases, your doctor may prescribe medication to prevent or relieve nausea and vomiting. Eating several small meals, not eating before treatment, or limiting activity may help lessen some of these effects. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Diarrhea is a common side effect of this medication. Drink plenty of fluids unless directed otherwise. Your doctor may also prescribe medication (such as loperamide) to help lessen diarrhea. Vomiting or diarrhea that doesn't stop may result in dehydration. Contact your doctor promptly if you notice any symptoms of dehydration, such as unusual decreased urination, unusual dry mouth/thirst, or dizziness/lightheadedness.Temporary hair loss may occur. Normal hair growth should return after treatment has ended. Also, temporary nail changes may occur.People using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.Stop taking capecitabine and tell your doctor right away if any of these very serious side effects occur: severe nausea/vomiting (vomiting 2 or more times per day, unable to eat or keep food/fluids in your stomach), painful redness/swelling/sores in mouth or on your tongue.Capecitabine may make you develop a skin problem called hand-foot syndrome. To help prevent this, protect your hands and feet from heat or increased pressure. Avoid activities such as using hot dishwater, taking tub baths, jogging, long walks, or using garden or household tools such as screwdrivers. Symptoms may include pain, swelling, redness, blisters, or numbness of the hands/feet. Your doctor may prescribe medication (such as balm) to help with symptoms. If symptoms affect your usual activities, get medical help right away.For men and women of childbearing age, this medication may affect your ability to have children. Ask your doctor for more details.This medication may lower your ability to fight infections. This may make you more likely to get a serious (rarely fatal) infection or make any infection you have worse. Tell your doctor right away if you have any signs of infections (such as sore throat that doesn't go away, fever, chills, cough).Tell your doctor right away if you have any serious side effects, including: easy bruising/bleeding, mental/mood changes (such as depression), swelling of the ankles/feet, vision changes, signs of kidney problems (such as change in the amount of urine), yellowing eyes/skin, dark urine.Get medical help right away if you have any very serious side effects, such as: chest/jaw/left arm pain, unusual sweating, fainting, slow/fast/irregular heartbeat.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, such as: rash/blisters/peeling, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other side effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking capecitabine, tell your doctor or pharmacist if you are allergic to it; or to 5-fluorouracil; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: lack of a certain enzyme (dihydropyrimidine dehydrogenase - DPD), blood disorders (such as bone marrow suppression), heart problems (such as heart failure), kidney disease, liver problems.Capecitabine can make you more likely to get infections or may worsen any current infections. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.Tell your health care professional that you are using capecitabine before having any immunizations/vaccinations. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.This medication may make you more sensitive to the sun. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors. Get medical help right away if you get sunburned or have skin blisters/redness.This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the side effects of this medication, especially nausea, vomiting, diarrhea, and hand-foot syndrome.Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while you are using capecitabine. Capecitabine may harm an unborn baby. Ask about reliable forms of birth control. Women of childbearing age should use reliable forms of birth control during treatment and for 6 months after the last dose. Men with female partners of childbearing age should use reliable forms of birth control during treatment and for 3 months after the last dose. If you or your partner become pregnant, talk to your doctor right away about capecitabine's risks and benefits.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.It is unknown if this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug is not recommended during treatment and for 2 weeks after the last dose. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: See also Warning section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (such as prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.A product that may interact with this drug is: allopurinol.Capecitabine is very similar to fluorouracil. Do not use medications containing fluorouracil while using capecitabine.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as bilirubin, complete blood counts, kidney/liver function) should be done while you are taking this medication. Keep all medical and lab appointments.
MISSED DOSE: If you miss a dose, skip the missed dose. Take your next dose at the regular time and check with your doctor. Do not double the dose to catch up.
STORAGE: Store in a tightly closed container at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).
Information last revised December 2021. Copyright(c) 2022 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
