Generic Capecitabine (Capecitabine)

Introduction

Capecitabine is an oral chemotherapy agent used primarily to treat certain solid tumors. It contains the active compound capecitabine, is supplied as 500 mg film-coated tablets, and belongs to the class of antimetabolite prodrugs. The medication is approved for metastatic colorectal cancer, adjuvant colorectal cancer after surgery, and metastatic breast cancer that has progressed following prior therapy. In addition to these indications, capecitabine is investigated for several other oncologic conditions.

What is Capecitabine?

Capecitabine is a fluoropyrimidine prodrug that is converted in the body to 5-fluorouracil (5-FU), the active cytotoxic metabolite. The drug was developed by Roche and received FDA approval in 1998. It is marketed worldwide under brand names such as Xeloda and Tegafur-capecitabine.

Capecitabine is the generic version of well-known medications, containing the active compound capecitabine. Our online pharmacy provides this generic alternative as a cost-effective treatment option.

The tablet formulation contains lactose, microcrystalline cellulose, and magnesium stearate as inactive ingredients. It is designed for oral administration and is supplied in 500 mg strength, which allows flexible dose titration based on body surface area.

How Capecitabine Works

Capecitabine is absorbed through the gastrointestinal tract and undergoes a three-step enzymatic conversion:

1. Carboxylesterase in the liver converts capecitabine to 5′-deoxy-5-fluorocytidine (5′-dFCR).
2. Cytidine deaminase in the liver and tumor tissue transforms 5′-dFCR into 5′-deoxy-5-fluorouridine (5′-dFUR).
3. Thymidine phosphorylase, which is markedly elevated in many tumors, converts 5′-dFUR to 5-fluorouracil (5-FU).

The resulting 5-FU is incorporated into RNA and DNA, disrupting synthesis and triggering apoptosis of rapidly dividing cancer cells. Because thymidine phosphorylase activity is higher in tumor tissue than in most normal tissues, capecitabine achieves a degree of tumor-selective activation, which partly explains its efficacy and tolerability compared with intravenous 5-FU.

Pharmacokinetic studies show peak plasma 5-FU concentrations approximately 1-2 hours after oral dosing, with a terminal half-life of 3-5 hours. Renal excretion accounts for roughly 80 % of the dose, making dose adjustment necessary in patients with impaired kidney function.

Conditions Treated with Capecitabine

• Metastatic colorectal cancer (mCRC). Capecitabine, alone or with oxaliplatin (the XELOX regimen), improves progression-free survival compared with 5-FU alone.
• Adjuvant colorectal cancer after curative resection. Post-operative capecitabine reduces the risk of disease recurrence in stage III disease.
• Metastatic breast cancer (mBC). Capecitabine is indicated after disease progression on anthracycline, taxane, or both; it can be used alone or combined with agents such as trastuzumab in HER2-positive disease.

The drug is effective in these settings because it delivers sustained intracellular 5-FU concentrations within tumor cells, thereby inhibiting DNA synthesis and promoting cell death.

Off-Label and Investigational Uses of Capecitabine

• Head and neck squamous cell carcinoma (HNSCC). Phase II studies have evaluated capecitabine plus radiotherapy as an alternative to standard cisplatin-based chemoradiation, showing comparable response rates. This use is not approved by the FDA or EMA.
• Pancreatic adenocarcinoma. Small-scale trials have combined capecitabine with gemcitabine, reporting modest survival benefits; the regimen remains off-label.
• Gastric and gastro-esophageal junction adenocarcinoma. Capecitabine is sometimes used in combination with oxaliplatin (XELOX) as part of peri-operative treatment protocols, although formal approval varies by region.
• Cholangiocarcinoma. Retrospective analyses suggest activity when capecitabine is paired with radiotherapy or other chemotherapeutics, but regulatory endorsement is lacking.

Caution: Off-label applications have not undergone the comprehensive efficacy and safety evaluation required for formal approval. Patients should discuss any potential off-label therapy with a qualified healthcare provider, who can weigh the evidence against individual risk factors.

Is Capecitabine the Right Medication for You?

Capecitabine is most appropriate for adult patients with:

• Histologically confirmed metastatic or adjuvant colorectal cancer who are able to swallow oral tablets.
• Metastatic breast cancer that has progressed after standard anthracycline and taxane regimens.

Clinical scenarios that favor capecitabine include:

• Preference for oral chemotherapy to reduce infusion-center visits.
• Prior intolerance to continuous 5-FU infusion (e.g., due to catheter complications).
• Adequate renal function (creatinine clearance ≥ 30 mL/min) and hepatic function (bilirubin ≤ 1.5 × ULN).

Contraindications include known hypersensitivity to capecitabine or any of its excipients, severe renal impairment (creatinine clearance < 30 mL/min), and concomitant use of sorivudine-containing drugs (due to fatal drug-interaction risk). Pregnant or breastfeeding individuals should avoid capecitabine because of documented fetal toxicity.

Risks, Side Effects, and Interactions

Common

• Diarrhea - often mild to moderate; may require antidiarrheal agents.
• Hand-Foot Syndrome (palmar-plantar erythrodysesthesia). Redness, swelling, and pain on palms or soles; dose modification can alleviate symptoms.
• Nausea and vomiting - usually controllable with standard anti-emetics.
• Mucositis - inflammation of the oral mucosa; oral hygiene measures help.

Rare

• Cardiotoxicity - occasional cases of angina-like chest pain or myocardial ischemia.
• Severe alopecia - less frequent than with taxanes but reported.
• Hyperbilirubinemia - isolated elevations in liver enzymes.

Serious

• Myelosuppression - neutropenia, leukopenia, and thrombocytopenia; monitor complete blood counts regularly.
• Severe Hand-Foot Syndrome - may progress to ulceration and infection, necessitating treatment interruption.
• Stevens-Johnson syndrome/toxic epidermal necrolysis - extremely rare but life-threatening skin reactions.

Drug-Drug Interactions

• Anticoagulants (e.g., warfarin). Capecitabine may enhance anticoagulant effect; INR should be monitored.
• CYP2C9 inhibitors (e.g., fluconazole). May increase capecitabine exposure, raising toxicity risk.
• Radiation therapy. Concurrent use can intensify mucosal and dermal toxicity.

Drug-Food Interactions

• Alcohol - excessive intake can exacerbate liver toxicity and worsen hand-foot syndrome.
• High-fat meals - do not significantly affect absorption; however, the tablet should be taken with food to reduce gastrointestinal upset.

Patients should always disclose all concomitant medications, including over-the-counter products and herbal supplements.

Use: Dosing, Missed Dose, Overdose

Standard dosing is based on body surface area (BSA). The most common regimen for colorectal cancer is 1,250 mg/m² (divided into two 625 mg doses) taken twice daily for 14 consecutive days, followed by a 7-day rest period. For breast cancer, a typical schedule is 1,000 mg/m² twice daily for 14 days, then a 7-day break. Dose adjustments are recommended for renal impairment (e.g., 75 % of the standard dose if creatinine clearance is 30-50 mL/min).

Missed dose: If a patient forgets a dose, they should take it as soon as they remember, provided it is at least 8 hours before the next scheduled dose. If the dosing interval is less than 8 hours, skip the missed dose and resume the regular schedule; do not double-dose.

Overdose: In case of suspected overdose, patients should seek immediate medical attention. Symptoms may include severe diarrhea, vomiting, neutropenia, and profound hand-foot syndrome. Supportive care-intravenous fluids, anti-emetics, and close hematologic monitoring-is the mainstay of management.

Practical precautions:

• Take capecitabine with a meal or within 30 minutes after eating to improve tolerance.
• Avoid alcohol and limit intake of grapefruit products, which can interfere with metabolism.
• Do not operate heavy machinery or drive if experiencing significant neuropathy or severe fatigue.

FAQ

• What should I do with my capecitabine tablets during a long flight?

  • Store the tablets in their original container at room temperature, away from direct sunlight. If the flight exceeds 8 hours, consider a small insulated pouch to protect against extreme temperature changes.

• Can I split a 500 mg capecitabine tablet to adjust the dose?

  • The tablets are not scored and are formulated for intact swallowing. Splitting may lead to dose inaccuracy; instead, discuss alternative dosing schedules with your provider.

• Is there a specific time of day that reduces hand-foot syndrome?

  • No definitive timing has been proven to prevent the syndrome. Maintaining consistent dosing intervals and taking the medication with food are more reliable strategies.

• Do the tablets contain any allergens such as gluten or soy?

  • Capecitabine tablets are gluten-free. Some formulations may include soy-derived excipients; verify the exact product label if soy allergy is a concern.

• How should I store capecitabine in a hot climate?

  • Keep the medication in a cool, dry place below 30 °C (86 °F). If ambient temperatures frequently exceed this, store the bottle in a refrigerator (do not freeze) and allow it to reach room temperature before use.

• Will capecitabine interfere with urine drug testing?

  • Capecitabine and its metabolites are not known to cause false-positive results on standard illicit-drug screens.

• Can I take vitamin supplements while on capecitabine?

  • Most multivitamins are safe, but high-dose antioxidants (e.g., vitamin C > 1 g/day) may theoretically reduce chemotherapy effectiveness; discuss any high-dose supplement with a pharmacist.

• What is the difference between capecitabine and intravenous 5-fluorouracil?

  • Capecitabine is an oral prodrug that is metabolized to 5-FU preferentially within tumor tissue, potentially offering more convenient administration and a different toxicity profile.

• Are there any clinical trials evaluating capecitabine for rare cancers?

  • Yes, ongoing phase II studies are exploring capecitabine combined with immunotherapy agents in Merkel cell carcinoma and certain sarcomas. Participation requires specialist referral.

• How long does it take for hand-foot syndrome to resolve after stopping capecitabine?

  • Symptoms usually improve within 2-4 weeks after dose reduction or discontinuation, though full recovery may take several months depending on severity.

Glossary

Prodrug

An inactive compound that is metabolized in the body to produce an active pharmacologic agent.

Thymidine phosphorylase

An enzyme highly expressed in many tumors that converts capecitabine’s intermediate metabolite into the active chemotherapeutic 5-fluorouracilFoot Syndrome (Palmar-Plantar Erythrodysesthesia)**

A dose-limiting toxicity characterized by redness, swelling, and pain on the palms and soles, commonly associated with capecitabine.

BSA (Body Surface Area)

A calculated measurement (in m²) used to personalize chemotherapy dosing, derived from a patient’s height and weight.

Buying Capecitabine from Our Online Pharmacy

Capecitabine can be obtained conveniently through our online pharmacy. We source the generic medication directly from licensed, FDA-registered manufacturers, ensuring that every batch meets stringent quality standards. Because we operate as a pharmacy-broker service, we can offer the product at a price close to the manufacturer’s cost, providing a cost-effective alternative for patients who face high out-of-pocket expenses or limited availability through local pharmacies.

Our fulfillment network guarantees discreet packaging and reliable delivery-typically within 7 for express shipping and about 3 weeks for regular airmail to most regions. The service is fully compliant with international pharmacy regulations, and each shipment is tracked from our secure warehouse to the patient’s doorstep.

Patients who value privacy, affordability, and assured product authenticity will find our online pharmacy a trustworthy partner in accessing capecitabine when conventional channels are inaccessible or financially burdensome.

Disclaimer

The information presented about Capecitabine is intended for general educational purposes only and does not replace professional medical advice. All therapeutic decisions, including the consideration of off-label applications, must be made under the direct supervision of a qualified healthcare professional. Readers are assumed to be competent adults capable of making health choices. Our online pharmacy provides access to Capecitabine for individuals who may encounter limited availability through conventional pharmacies, insurance-based dispensing, or who seek affordable generic options. Always consult a qualified provider before initiating, modifying, or discontinuing any medication.