Xeloda: Targeted Oral Chemotherapy for Advanced Cancers
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Synonyms | |||
Xeloda (capecitabine) is an orally administered prodrug chemotherapy agent specifically designed for targeted activation within tumor tissue. As a fluoropyrimidine carbamate, it offers a sophisticated mechanism of delivery, converting enzymatically to 5-fluorouracil (5-FU) preferentially at the tumor site, thereby maximizing cytotoxic effects while potentially minimizing systemic exposure. This innovative approach provides a critical therapeutic option for patients with metastatic colorectal cancer, metastatic breast cancer, and following adjuvant colon cancer treatment, representing a significant advancement in convenience and targeted treatment strategy over traditional continuous intravenous infusions.
Features
- Chemotherapeutic classification: Fluoropyrimidine carbamate (prodrug of 5-fluorouracil)
- Administration: Oral tablet formulation (150 mg and 500 mg film-coated)
- Activation pathway: Undergoes a three-step enzymatic conversion to 5-fluorouracil, with the final step catalyzed by thymidine phosphorylase, an enzyme often concentrated in tumor tissues
- Dosing schedule: Typically administered on a 3-week cycle (2 weeks of treatment followed by 1 week of rest)
- Bioavailability: Nearly 100% following oral administration under fed conditions
- Primary metabolites: 5’-deoxy-5-fluorocytidine (5’-DFCR) and 5’-deoxy-5-fluorouridine (5’-DFUR)
Benefits
- Oral Administration Convenience: Eliminates the need for frequent clinic visits for intravenous infusions, allowing patients to maintain greater normalcy in their daily routines and reducing the burden on healthcare infrastructure.
- Tumor-Selective Activation: The unique enzymatic activation mechanism aims to deliver a higher concentration of the active cytotoxic drug (5-FU) directly within cancer cells, potentially enhancing efficacy while sparing some healthy tissues.
- Proven Efficacy in Multiple Indications: Demonstrates significant clinical benefit as both a monotherapy and in combination regimens for advanced colorectal and breast cancers, supported by robust clinical trial data.
- Established Safety Profile: While side effects exist, its safety and management protocols are well-documented, allowing oncologists to proactively monitor and mitigate adverse events.
- Flexible Dosing Adjustments: The oral tablet form allows for precise and individualized dose modifications based on patient tolerance and toxicity, a flexibility not easily achievable with fixed IV doses.
- Foundation for Combination Therapy: Serves as an effective backbone for combination with other chemotherapeutic agents and targeted therapies, expanding treatment possibilities.
Common use
Xeloda is indicated for the treatment of patients with:
- Metastatic Colorectal Cancer: Approved as first-line treatment, either as a single agent or, more commonly, in combination with other chemotherapy drugs like oxaliplatin (XELOX regimen).
- Dukes’ C Colon Cancer: Approved for adjuvant treatment following complete resection of the primary tumor when fluoropyrimidine therapy alone is preferred.
- Metastatic Breast Cancer: Approved for treatment of patients resistant to both paclitaxel and an anthracycline-containing chemotherapy regimen, or resistant to paclitaxel and for whom further anthracycline therapy is not indicated. It is also used in combination with docetaxel after failure of prior anthracycline-containing chemotherapy.
Dosage and direction
Dosing is highly individualized based on body surface area (BSA), indication, combination therapy, and patient tolerance. The following represents common dosing paradigms. All dosing must be determined and supervised by a qualified oncologist.
- Monotherapy for Metastatic Colorectal or Breast Cancer: 1250 mg/m² administered orally twice daily (morning and evening, equivalent to 2500 mg/m² total daily dose) for 2 weeks, followed by a 1-week rest period. This constitutes one 3-week cycle.
- Combination Therapy (e.g., XELOX): Often reduced to 1000 mg/m² twice daily for 2 weeks, combined with oxaliplatin IV on Day 1 of each cycle, followed by a 1-week rest.
- Adjuvant Treatment for Colon Cancer: 1250 mg/m² twice daily for 2 weeks followed by a 1-week rest period, for a total of 8 cycles (24 weeks).
- Administration: Tablets should be swallowed whole with water within 30 minutes after a meal. This significantly improves tolerability and absorption. Doses are typically divided approximately 12 hours apart.
Precautions
- Myelosuppression: Xeloda can cause neutropenia, thrombocytopenia, and anemia. Complete blood counts must be monitored regularly before and during treatment.
- Diarrhea: Can be severe, leading to dehydration, electrolyte imbalance, and renal impairment. Deaths from severe diarrhea have been reported. Treatment should be interrupted immediately upon the onset of Grade 2+ diarrhea and managed with standard antidiarrheal agents (e.g., loperamide) and fluid/electrolyte replacement.
- Cardiotoxicity: May cause cardiotoxicity including myocardial infarction/ischemia, angina, dysrhythmias, and cardiac arrest. Use with caution in patients with a history of coronary artery disease.
- Dihydropyrimidine Dehydrogenase (DPD) Deficiency: Patients with partial or complete absence of DPD activity are at significantly increased risk of severe, life-threatening, or fatal toxicity (e.g., neutropenia, neuropathy, diarrhea, mucositis). Testing for DPD deficiency should be considered.
- Renal Impairment: Patients with moderate to severe renal impairment (creatinine clearance below 50 mL/min) have a significantly increased exposure to capecitabine and its metabolites, leading to a higher risk of severe adverse reactions. Dose adjustment is mandatory.
- Hand-and-Foot Syndrome (Palmar-Plantar Erythrodysesthesia): A common dermatologic toxicity characterized by numbness, dysesthesia, paresthesia, tingling, painless or painful swelling, erythema, desquamation, blistering, and severe pain. Dose interruption and modification are required for Grade 2 or 3 reactions.
- Hyperbilirubinemia: Frequent monitoring of liver function tests is required. Dose modifications are necessary for severe liver dysfunction.
Contraindications
Xeloda is contraindicated in patients with:
- Known severe hypersensitivity to capecitabine or any component of the formulation.
- Known hypersensitivity to 5-fluorouracil.
- Patients with known complete absence of dihydropyrimidine dehydrogenase (DPD) activity.
- Severe renal impairment (creatinine clearance below 30 mL/min [Cockcroft and Gault]).
- Concomitant administration with sorivudine or its chemically related analogues (e.g., brivudine). This combination is contraindicated due to the risk of severe and potentially fatal enhancement of fluoropyrimidine toxicity.
Possible side effect
Adverse reactions are common and often dose-limiting. They include:
- Very Common (≥1/10): Diarrhea, nausea, vomiting, stomatitis, abdominal pain, Hand-and-Foot Syndrome, fatigue, anorexia, dermatitis, neutropenia, thrombocytopenia, anemia, hyperbilirubinemia.
- Common (≥1/100 to <1/10): Constipation, dyspepsia, dehydration, dizziness, headache, insomnia, peripheral neuropathy, eye irritation, dyspnea, fever, edema, nail disorder.
- Uncommon (≥1/1,000 to <1/100): Neutropenic sepsis, agranulocytosis, leukoencephalopathy, cardiomyopathy, ventricular arrhythmia, GI bleeding, hepatitis, jaundice, anaphylaxis, angioedema.
Drug interaction
- Antacids: Concomitant use of aluminum- and magnesium-hydroxide containing antacids may increase capecitabine exposure; monitor for toxicity.
- Allopurinol: Concomitant use may decrease the efficacy of capecitabine and should generally be avoided unless for the treatment of hyperuricemia.
- Warfarin (and other Coumarin Derivatives): Xeloda consistently enhances the anticoagulant effect of warfarin, significantly increasing INR and the risk of bleeding. INR must be monitored frequently, and warin dose adjusted accordingly, in all patients taking both drugs.
- Phenytoin: Capecitabine may increase plasma concentrations of phenytoin; monitor phenytoin levels.
- Leucovorin: Concomitant use increases the concentration of 5-fluorouracil, potentially increasing toxicity.
- Other Chemotherapy Agents: Interactions are complex and expected; combination regimens are designed and monitored by oncologists.
Missed dose
A missed dose should not be replaced. The next dose should be taken at the usual scheduled time. Patients should be instructed to never take a double dose to make up for a missed one, as this significantly increases the risk of severe toxicity.
Overdose
Overdose would be expected to manifest as severe forms of the known toxicities: severe nausea, vomiting, diarrhea, GI irritation and bleeding, bone marrow suppression (severe neutropenia, thrombocytopenia), and acute neurological toxicity. There is no specific antidote for capecitabine overdose. Treatment consists of immediate discontinuation of the drug and initiation of supportive measures, including aggressive hydration, antiemetics, antidiarrheals, hematologic support (e.g., growth factors, transfusions), and treatment of any subsequent infections. Hemodialysis is unlikely to be effective due to the drug’s high protein binding and extensive metabolism.
Storage
- Store at room temperature, 20°C to 25°C (68°F to 77°F).
- Keep in the original container to protect from moisture and light.
- Keep out of reach of children and pets.
- Do not flush unused medication down the toilet or pour it into a drain. Consult a healthcare professional or pharmacist on proper disposal methods, often through a take-back program.
Disclaimer
This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has been compiled from various sources believed to be accurate but cannot be guaranteed. Dosing, indications, and safety information may change.
Reviews
- Clinical Oncologist, Academic Medical Center: “Xeloda has been a cornerstone of our oral chemotherapy arsenal for over two decades. Its role in metastatic colorectal cancer, particularly in the XELOX regimen, provides a highly effective and more convenient alternative to infusional 5-FU/leucovorin. The predictable toxicity profile, primarily hand-foot syndrome and diarrhea, allows for proactive management and dose modification. Its tumor-activated mechanism remains a compelling feature, though vigilant monitoring for DPD deficiency is now a non-negotiable standard of care prior to initiation.”
- Oncology Pharmacist, Community Hospital: “From a pharmacy perspective, the switch to an oral fluoropyrimidine simplifies logistics for patients and the healthcare system. However, it places a greater responsibility on the patient for adherence and on the clinical team for patient education. We spend considerable time counseling on the timing of doses with food, the critical importance of reporting diarrhea immediately, and the early signs of hand-foot syndrome. The drug interaction with warfarin is one of the most significant we manage, requiring extremely close INR monitoring.”
- Patient (Metastatic Breast Cancer): “After failing several IV chemo regimens, moving to an oral treatment like Xeloda gave me a sense of control and normalcy back. No more ports or hours at the infusion center. The side effects were challenging—the hand-foot syndrome was painful and the fatigue was real—but my team was able to adjust the dose so I could manage them. It allowed me to spend more quality time with my family during treatment.”