Xeloda^® (Tablets) Instructions for Use

Marketing Authorization Holder

F. Hoffmann-La Roche, Ltd (Switzerland)

Manufactured By

Productos Roche, S.A. De C.V. (Mexico)

Or

Hoffmann-La Roche, Inc. (USA)

Labeled By

ORTAT, JSC (Russia)

ATC Code

L01BC06 (Capecitabine)

Active Substance

Capecitabine (Rec.INN registered by WHO)

Dosage Forms

	Xeloda®	Film-coated tablets, 150 mg: 60 pcs.
		Film-coated tablets, 500 mg: 120 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets light peach (light milky pink) in color, oblong, biconvex, with the engraving “XELODA” on one side and “150” on the other side of the tablet.

Excipients: lactose – 15.6 mg, microcrystalline cellulose – 7.2 mg, croscarmellose sodium – 6 mg, hypromellose (3 mPa.s) – 4.5 mg, magnesium stearate – 2.7 mg.

Shell composition Opadry Pink 03A14309 (hypromellose (6 mPa.s), talc, titanium dioxide (E171), iron oxide yellow (E172), iron oxide red (E172)) – 8.5 mg.

10 pcs. – blisters made of PVC/PVDF film and aluminum foil (6) – cardboard packs.

Film-coated tablets peach (milky pink) in color, oblong, biconvex, with the engraving “XELODA” on one side and “500” on the other side of the tablet.

Excipients: lactose – 52 mg, microcrystalline cellulose – 24 mg, croscarmellose sodium – 20 mg, hypromellose (3 mPa.s) – 15 mg, magnesium stearate – 9 mg.

Shell composition Opadry Pink 03A14380 (hypromellose (6 mPa.s), talc, titanium dioxide (E171), iron oxide yellow (E172), iron oxide red (E172)) – 18 mg.

10 pcs. – blisters made of PVC/PVDF film and aluminum foil (12) – cardboard packs.

Clinical-Pharmacological Group

Antitumor drug. Antimetabolite

Pharmacotherapeutic Group

Antineoplastic agent, antimetabolite

Pharmacological Action

Antitumor agent. It has a selective cytotoxic effect. In tumor tissue, capecitabine is converted to 5-fluorouracil under the action of thymidine phosphorylase (tumor angiogenic factor). The activity of thymidine phosphorylase in the primary tumor is 4 times higher than in healthy tissue, so the concentration of 5-fluorouracil in tumor tissue is higher than in healthy tissue and in plasma.

In both healthy and tumor cells, 5-fluorouracil is metabolized to form 5-fluoro-2-deoxyuridine monophosphate and 5-fluorouridine triphosphate, which have a cytotoxic effect.

Indications

Locally advanced or metastatic breast cancer, after failure of chemotherapy containing paclitaxel and an anthracycline-containing drug, or when there are contraindications to anthracycline therapy.

ICD codes

Dosage Regimen

Take tablets within 30 minutes after a meal with water.

The recommended starting dose for metastatic breast cancer is 1250 mg/m² administered twice daily (morning and evening).

Calculate the total daily dose based on the patient’s body surface area. Divide the total daily dose into two equal doses.

Use the 500 mg and 150 mg film-coated tablets in combination to achieve the correct dose.

Administer treatment in 3-week cycles: take the drug for 2 weeks, followed by a 1-week rest period.

Do not crush or split tablets.

Adjust the dose based on tolerance and toxic reactions according to the prescribing information.

For patients with a moderate renal impairment (creatinine clearance 30-50 mL/min), reduce the starting dose to 950 mg/m² twice daily.

Withhold treatment immediately for Grade 2 or higher adverse events.

Resume treatment at a reduced dose after the adverse event resolves to Grade 0-1.

Adverse Reactions

From the digestive system: diarrhea, nausea, vomiting, stomatitis, abdominal pain, constipation, epigastric pain, dyspepsia, dry mouth, flatulence, loose stools, anorexia, decreased appetite, oral candidiasis, hyperbilirubinemia, taste disturbance.

From the nervous system: increased fatigue, weakness, pronounced drowsiness, headache, paresthesia, dizziness, sleep disorders, asthenia.

From the skin and subcutaneous tissues: palmar-plantar erythrodysesthesia syndrome, dermatitis, dry skin, alopecia, itching, focal peeling, skin hyperpigmentation, skin cracks.

Other: increased lacrimation, fever, possible dehydration, weight loss, possible shortness of breath, cough, limb pain, lower back pain, myalgia, cardiotoxic effect (most likely in patients with coronary artery disease), edema of the lower extremities, anemia.

Contraindications

History of severe unpredictable reactions when treated with fluoropyrimidine, hypersensitivity to capecitabine and 5-fluorouracil.

Use in Pregnancy and Lactation

Adequate and strictly controlled clinical studies on the safety of capecitabine use during pregnancy have not been conducted. Experimental studies have shown that capecitabine has fetotoxic and teratogenic effects. Use during pregnancy is not recommended. Women of childbearing potential should use reliable methods of contraception during treatment.

It is not known whether capecitabine is excreted in breast milk. If use during lactation is necessary, the expected benefit of treatment for the mother and the existing risk for the child should be assessed.

Use in Hepatic Impairment

During treatment, patients with mild and moderate hepatic impairment due to liver metastases require careful medical supervision.

Pediatric Use

The safety and efficacy of capecitabine use in children have not been studied.

Geriatric Use

During treatment, elderly persons require careful medical supervision.

Special Precautions

During treatment, patients with mild and moderate hepatic impairment due to liver metastases and elderly persons require careful medical supervision.

In case of moderate or severe hyperbilirubinemia, capecitabine intake should be temporarily discontinued until values return to mild severity.

The safety and efficacy of capecitabine use in children have not been studied.

Effect on ability to drive vehicles and operate machinery

Use with caution in patients engaged in potentially hazardous activities that require high concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use of capecitabine with coumarin anticoagulants, coagulation parameters may be impaired and bleeding may develop (it is necessary to regularly monitor coagulation parameters).

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.