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Xeloda

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Xeloda (Capecitabine) is a derivative of fluoropyrimidine carbamate, an oral cytostatic agent that activates in the tumor tissue and exerts a selective cytotoxic effect on it. In vitro capecitabine does not have a cytotoxic effect. In vivo, it is converted to 5-FU, which undergoes further metabolism. The formation of 5-FU occurs predominantly in the tumor tissue under the influence of a tumor angiogenic factor – dTdPase, which minimizes the systemic effect of 5-FU on healthy body tissues.

The sequential enzyme biotransformation of capecitabine in 5-FU creates higher concentrations of the drug in the tumor tissues than in the surrounding healthy tissues. After oral administration of capecitabine to patients with colon cancer, the concentration of 5-FU in the tumor tissue is 3.2 times higher than its concentration in adjacent healthy tissues. The ratio of 5-FU concentrations in the tumor tissue and plasma is 21.4, the ratio of its concentration in healthy tissues and plasma is 8.9. The activity of thymidine phosphorylase in the primary colorectal tumor is 4 times higher than in adjacent healthy tissues.

Indications

  • Combined therapy with docetaxel for locally advanced or metastatic breast cancer with chemotherapy failure including an anthracycline drug;
  • Monotherapy of locally advanced or metastatic breast cancer with the ineffectiveness of chemotherapy with taxanes or anthracycline drugs, or if there are contraindications to anthracycline therapy;
  • Adjuvant therapy for colon cancer;
  • First-line therapy for metastatic colorectal cancer;
  • First-line therapy for stomach cancer.

Dosage regimen

The drug is taken orally, washed down with water, no later than 30 minutes after eating.

Monotherapy

Colorectal cancer, colon cancer, and breast cancer

Xeloda is prescribed at 1250 mg/m2 2 times/day, morning and evening (total daily dose of 2500 mg/m2) for two weeks, followed by a seven-day break.

Combination therapy

Breast cancer

Xeloda is prescribed at 1250 mg/m2 2 times/day for two weeks, followed by a 7-day break, in combination with docetaxel at a dose of 75 mg/m2 once every 3 weeks as an intravenous infusion for 1 hour.

Premedication is carried out before the administration of docetaxel in accordance with the instructions for its use.

Colorectal and stomach cancer

As part of combination therapy, the dose of Xeloda should be reduced to 800-1000 mg/m2 2 times/day for two weeks, followed by a 7-day break or to 625 mg/m2 2 times/day with continuous use. Adding immunobiological preparations to combination therapy does not affect the dose of Xeloda.

Antiemetics and sedation to ensure adequate hydration are prescribed before the administration of cisplatin and oxaliplatin according to the instructions for use of cisplatin and oxaliplatin when used in combination with Xeloda.

In adjuvant therapy of stage III colon cancer, the recommended duration of therapy with Xeloda is 6 months, i.e. 8 courses.

Contraindications

  • Hypersensitivity to capecitabine and other fluoropyrimidine derivatives or any components of the drug;
  • Established deficiency of DPD (dihydropyrimidine dehydrogenase) as for other fluoropyrimidines;
  • Simultaneous administration of sorivudine or its structural analogs, such as brivudine;
  • Severe renal failure (Cl creatinine below 30 ml/min);
  • Pregnancy and lactation;
  • Age up to 18 years (effectiveness and safety of use are not established);
  • contraindications for other components of combination therapy.

Take this drug with caution in the following cases:

  • ischemic heart disease;
  • renal or liver failure;
  • age over 60 years;
  • simultaneous use with oral anticoagulants of the coumarin group.

Side effects

The most common side effects (≥10%):

  • diarrhea;
  • stomatitis;
  • nausea;
  • vomiting;
  • palmar-plantar syndrome;
  • increased fatigue;
  • weakness;
  • lethargy;
  • drowsiness.

Other side effects are:

  • digestive system: diarrhea, vomiting, stomatitis (including ulcerative), lack of appetite, loss of appetite, abdominal pain, epigastric pain, constipation, dry mouth, dyspepsia, candidiasis of the oral cavity; in less than 5% of cases – bloating, esophagitis, gastritis, duodenitis, colitis, hiccups, gastrointestinal bleeding, isolated cases of liver failure and cholestatic hepatitis; their causal relationship with capecitabine has not been established.
  • skin and appendages: palmar-plantar syndrome (paresthesia, edema, hyperemia, peeling of the skin, blistering), dermatitis, dry skin, erythematous rash, erythema, alopecia, pruritus, focal peeling, hyperpigmentation of the skin, violation of the structure and discoloration of the nails onycholysis; in less than 5% of cases – photosensitivity reactions, a syndrome resembling radiation dermatitis, skin cracks.
  • nervous system: headache, sleep disturbance (severe drowsiness, insomnia), paresthesia, dizziness, peripheral neuropathy; in less than 5% of cases – confusion, encephalopathy, cerebellar symptoms (ataxia, dysarthria, imbalance, and coordination), depression.
  • sensory organs: increased lacrimation, conjunctivitis, taste disturbance; very rarely – stenosis of the lacrimal-nasal canal.
  • respiratory system: sore throat, shortness of breath, cough, nosebleeds, dysphonia.
  • musculoskeletal system: arthralgia, myalgia.
  • cardiovascular system: edema of the lower extremities; in less than 5% of cases – cardialgia, angina pectoris, cardiomyopathy, myocardial ischemia, myocardial infarction, heart failure, sudden death, tachycardia, supraventricular arrhythmias, including atrial fibrillation, ventricular extrasystoles.
  • hemopoietic system: anemia, neutropenia, granulocytopenia, lymphocytopenia, thrombocytopenia; in less than 5% of cases – pancytopenia.
  • infections: in less than 5% of cases, infectious complications associated with myelosuppression, weakened immunity and impaired mucosal integrity, local and systemic (bacterial, viral and fungal) infections, possibly fatal, sepsis.
  • changes in laboratory parameters: regardless of their relationship with capecitabine, hyperbilirubinemia, increased ALT/AST activity, hypercreatininemia, increased activity of alkaline phosphatase, hyperglycemia, hypo- or hypercalcemia, hypoalbuminemia, hyponatremia, hypokalemia are found.
  • other: fever; fatigue; weakness; dehydration; weight loss; back pain; lethargy.

Interactions

  • Coumarin anticoagulants: capecitabine enhances the effects of indirect anticoagulants, which can result in impaired coagulation and bleeding several days or months after the start of capecitabine therapy (in one case, a month after its completion). It increases the AUC of warfarin by 57% and INR by 91%.
  • Substrates of cytochrome P450 2C9: studies on the interaction of capecitabine and other drugs metabolized by the isoenzyme 2C9 of the cytochrome P450 system were not conducted.
  • Phenytoin: capecitabine increases the concentration of phenytoin in plasma. It happens due to the suppression of the CYP2C9 isoenzyme under the influence of capecitabine. In patients taking capecitabine concomitantly with phenytoin, it is recommended that the plasma phenytoin concentration be regularly monitored.
  • Antacids containing aluminum and magnesium hydroxide: it slightly increases the concentration of capecitabine and one metabolite (5′-DPCT) in plasma; they do not affect the three main metabolites (5′-DFUR, 5-FU, and FBA) of capecitabine.
  • Calcium folinate (leucovorin) does not affect the pharmacokinetics of capecitabine and its metabolites; it may enhance the toxic effect of capecitabine.
  • Sorivudine and its analogs: potentially can result in a fatal increase in the toxicity of fluoropyrimidines due to the suppression of dihydropyrimidine dehydrogenase (DPD) by sorivudine.