Imitab 400 mg (Imatinib) Tablets

Imitab 400mg (Imatinib) tablets for treatment of CML, GIST and Ph+ ALL

Imitab 400 mg (Imatinib) Tablets

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Introduction

Imitab 400 mg (Imatinib) represents a revolutionary approach in targeted cancer therapy, offering hope to patients with various hematological malignancies and solid tumors. As a potent tyrosine kinase inhibitor, Imitab targets specific molecular abnormalities that drive cancer progression, effectively halting disease advancement while minimizing damage to healthy cells. This precision medicine approach has transformed treatment paradigms for conditions like chronic myeloid leukemia (CML), offering patients improved survival rates and quality of life.

Comprehensive Therapeutic Applications

Imitab demonstrates remarkable efficacy across multiple oncological conditions:

Hematological Malignancies

  • Philadelphia Chromosome Positive Chronic Myeloid Leukemia (Ph+ CML): First-line therapy for newly diagnosed adult and pediatric patients in chronic phase
  • Advanced CML: Effective treatment for accelerated phase or blast crisis, including after interferon-alpha therapy failure
  • Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia (Ph+ ALL): Treatment option for adult patients with relapsed or refractory disease
  • Pediatric Ph+ ALL: Combination therapy with chemotherapy for newly diagnosed patients

Myeloproliferative Disorders

  • Myelodysplastic/Myeloproliferative Diseases: Treatment for conditions associated with PDGFR gene rearrangements
  • Hypereosinophilic Syndrome (HES)/Chronic Eosinophilic Leukemia (CEL): Effective for patients with FIP1L1-PDGFRα fusion kinase
  • Aggressive Systemic Mastocytosis: Treatment option for patients without D816V c-Kit mutation or with unknown c-Kit mutational status

Solid Tumors

  • Gastrointestinal Stromal Tumors (GIST): Treatment for Kit (CD117) positive unresectable and/or metastatic disease
  • Adjuvant GIST Therapy: Post-surgical treatment following complete gross resection of Kit-positive GIST
  • Dermatofibrosarcoma Protuberans: Therapy for unresectable, recurrent and/or metastatic disease

Advanced Mechanism of Action

Imitab’s therapeutic efficacy stems from its precise molecular targeting:

Multiple Kinase Inhibition

Imitab functions by inhibiting multiple tyrosine kinases that drive cancer progression:

  • Bcr-Abl Tyrosine Kinase: Primary target in Ph+ CML and Ph+ ALL
  • c-Kit (CD117): Crucial target in GIST and systemic mastocytosis
  • PDGFRα and PDGFRβ: Key targets in HES/CEL and certain myeloproliferative disorders
  • Additional Kinases: Including discoidin domain receptors (DDR1 and DDR2) and colony stimulating factor receptor (CSF-1R)

Cellular Impact

By inhibiting these kinases, Imitab disrupts critical signaling pathways, leading to:

  • Reduced cancer cell proliferation
  • Inhibition of tumor angiogenesis
  • Promotion of cancer cell apoptosis (programmed cell death)
  • Suppression of metastatic potential

Optimized Dosage Guidelines

Imitab dosing is tailored to specific conditions and patient factors:

Adult Dosing Regimens

  • Ph+ CML Chronic Phase: 400 mg daily
  • Ph+ CML Advanced Phases: 600 mg daily
  • Ph+ ALL: 600 mg daily
  • GIST (Metastatic/Unresectable): 400 mg daily
  • Adjuvant GIST: 400 mg daily
  • Dermatofibrosarcoma Protuberans: 800 mg daily (as 400 mg twice daily)
  • Myelodysplastic/Myeloproliferative Diseases: 400 mg daily
  • HES/CEL and ASM: 100-400 mg daily based on disease characteristics

Pediatric Dosing Guidelines

  • Ph+ CML Chronic Phase: 340 mg/m² daily
  • Ph+ ALL: 340 mg/m² daily

Special Population Considerations

  • Hepatic Impairment: 400 mg daily for mild/moderate impairment; 300 mg daily for severe impairment
  • Administration Guidance: Take with meals and a large glass of water
  • Alternative Administration: Can be dissolved in water or apple juice for patients with difficulty swallowing

Pharmacokinetic Profile

Imitab 400 mg demonstrates favorable pharmacokinetic properties:

Absorption and Distribution

  • Excellent Bioavailability: 98% oral absorption
  • Peak Concentration: Reached within 2-4 hours post-dose
  • Dose Proportionality: Linear AUC increases with doses from 25-1,000 mg
  • Protein Binding: 95% bound to plasma proteins, primarily albumin and α1-acid glycoprotein

Metabolism and Elimination

  • Primary Metabolism: CYP3A4-mediated
  • Active Metabolite: N-demethylated piperazine derivative (similar potency to parent compound)
  • Elimination Route: Predominantly fecal (68%) with some urinary elimination (13%)
  • Half-Life: Approximately 18 hours for Imatinib; 40 hours for active metabolite

Clinical Considerations

Important factors to consider when prescribing Imitab:

Drug Interactions

  • CYP3A4 Inducers: May reduce Imitab exposure; consider alternative agents
  • CYP3A4 Inhibitors: May increase Imitab exposure; monitor for toxicity
  • CYP3A4 Substrates: Imitab increases exposure of narrow therapeutic window medications
  • CYP2D6 Substrates: Use caution with narrow therapeutic window medications
  • Anticoagulation: Low-molecular weight or standard heparin preferred over warfarin
  • Dietary Considerations: Avoid grapefruit juice due to CYP3A4 inhibition

Safety Monitoring

Regular monitoring is recommended for:

  • Complete Blood Counts: Weekly for first month, biweekly for second month, then periodically
  • Liver Function: Before treatment initiation and monthly thereafter
  • Renal Function: Baseline and periodically throughout treatment
  • Cardiac Function: Particularly in patients with risk factors for heart failure
  • Thyroid Function: In patients undergoing levothyroxine replacement
  • Growth Parameters: In pediatric patients

Managing Common Adverse Effects

Proactive management enhances treatment adherence:

Hematological Effects

  • Dose adjustments for cytopenias (anemia, neutropenia, thrombocytopenia)
  • Temporary treatment interruption for severe cases

Non-Hematological Effects

  • Fluid Retention/Edema: Regular weight monitoring and diuretic therapy if needed
  • Hepatotoxicity: Dose modification based on liver function test results
  • Gastrointestinal Issues: Supportive care for nausea, vomiting, diarrhea
  • Dermatological Reactions: Monitoring for severe skin reactions
  • Cardiac Effects: Careful management of congestive heart failure or left ventricular dysfunction

Special Precautions

Important considerations for specific patient populations:

Pregnancy and Breastfeeding

  • Contraception: Effective contraception required during treatment and for 15 days after
  • Pregnancy Risk: Should not be used during pregnancy unless clearly necessary
  • Breastfeeding: Not recommended during treatment and for 15 days after

Pediatric Patients

  • Growth Monitoring: Regular height and weight assessment
  • Developmental Assessment: Monitoring for potential developmental impacts

Elderly Patients

  • Well-tolerated with no specific dose adjustments required
  • Consider comorbidities and concomitant medications

Quality Assurance

Imitab 400 mg tablets are manufactured by Eskayef Pharmaceuticals Ltd., a leading pharmaceutical company with over three decades of excellence in medication production. Each tablet undergoes rigorous quality control testing to ensure consistent potency, purity, and effectiveness for optimal therapeutic outcomes.

Storage Instructions

To maintain product integrity:

  • Store below 30°C in a cool, dry place
  • Protect from light
  • Keep out of reach of children

Conclusion

Imitab 400 mg (Imatinib) stands as a breakthrough targeted therapy in oncology, offering life-changing treatment options for patients with various hematological malignancies and solid tumors. Through its precise inhibition of disease-driving kinases, Imitab provides effective disease control while maintaining quality of life. Available through Orio Pharma with worldwide delivery within 3-7 working days, Imitab represents hope and healing for cancer patients globally, reflecting our commitment to compassionate care and therapeutic excellence in challenging oncological conditions.

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