Imatinib Mesylate Tablets | Leukaemia

Imatinib Mesylate Tablets are primarily indicated for the treatment of various cancers, including:

• Chronic Myeloid Leukemia (CML): Used in adult and pediatric patients with Philadelphia chromosome-positive (Ph+) CML in chronic phase, accelerated phase, or blast crisis.
• Acute Lymphoblastic Leukemia (ALL): Indicated for adult patients with relapsed or refractory Ph+ ALL.
• Gastrointestinal Stromal Tumors (GIST): For adult patients with unresectable and/or metastatic malignant GIST.
• Myelodysplastic/Myeloproliferative Diseases (MDS/MPD): Treatment of adult patients with MDS/MPD associated with platelet-derived growth factor receptor (PDGFR) gene rearrangements.
• Systemic Mastocytosis (ASM): For adult patients with ASM without the D816V c-Kit mutation or with unknown c-Kit mutational status.
• Hypereosinophilic Syndrome (HES) and/or Chronic Eosinophilic Leukemia (CEL): Indicated for adult patients with HES/CEL.
• Dermatofibrosarcoma Protuberans (DFSP): Treatment of adult patients with unresectable, recurrent, and/or metastatic DFSP.

Imatinib Mesylate Tablets Characteristics

• Ingredients: Each tablet contains imatinib mesylate as the active ingredient.
• Properties: Imatinib mesylate is a tyrosine kinase inhibitor that targets BCR-ABL, c-Kit, and PDGFR tyrosine kinases.
• Specification: Available in tablet strengths of 100 mg and 400 mg.
• Packaging Specification: Typically packaged in blister packs or bottles containing 30 or 90 tablets, depending on the manufacturer.
• Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
• Expiry Date: 24 months
• Approval Number: H20100263
• Date of Revision: Refer to the specific product labeling for the most recent revision date.
• Manufacturer: Novartis Pharma Stein AG

Guidelines For The Use Of Imatinib Mesylate Tablets

• Dosage and Administration:
  • CML: 400 mg once daily for chronic phase; 600 mg once daily for accelerated phase or blast crisis.
  • Ph+ ALL: 600 mg once daily.
  • GIST: 400 mg once daily; a dose increase up to 800 mg daily (400 mg twice daily) may be considered in patients showing disease progression.
  • MDS/MPD: 400 mg once daily.
  • ASM: 400 mg once daily; for patients with ASM associated with eosinophilia, a starting dose of 100 mg daily is recommended.
  • HES/CEL: 100 mg once daily; dose increase to 400 mg may be considered in the absence of adverse reactions if assessments demonstrate an insufficient response.
  • DFSP: 800 mg daily (400 mg twice daily).

  Doses should be taken with a meal and a large glass of water to minimize gastrointestinal irritation. Dose adjustments may be necessary based on patient response and tolerability.

• Adverse Reactions:Common adverse reactions include edema, nausea, vomiting, muscle cramps, musculoskeletal pain, diarrhea, rash, fatigue, and abdominal pain. Severe adverse reactions may include myelosuppression, hepatotoxicity, and cardiac events. Regular monitoring of blood counts and liver function tests is recommended.

Imatinib Mesylate Tablets Medication Limitations

• Contraindications:Contraindicated in patients with hypersensitivity to imatinib or any of its excipients.
• Precautions:
  • Use with caution in patients with hepatic impairment, renal impairment, or cardiac disease.
  • Monitor for signs of fluid retention, such as weight gain and edema.
  • Advise women of childbearing potential to use effective contraception during treatment and avoid breastfeeding.
  • Regular monitoring of complete blood counts and liver function tests is recommended.

Imatinib Mesylate Tablets Interactions

• Drug Interactions:
  • CYP3A4 Inhibitors: Co-administration with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole) may increase imatinib plasma concentrations; dose reduction may be necessary.
  • CYP3A4 Inducers: Co-administration with strong CYP3A4 inducers (e.g., rifampin, St. John’s Wort) may decrease imatinib plasma concentrations; dose increase may be necessary.
  • Warfarin: Imatinib may increase the anticoagulant effect of warfarin; consider alternative anticoagulants.
  • Acetaminophen: Caution is advised when using acetaminophen concomitantly with imatinib due to potential hepatotoxicity.