Imatinib Mesylate

Generic Name

Imatinib Mesylate

Other Names

• Gleevec
• Glivec

Drug Class

• Tyrosine Kinase Inhibitor

Chemical Formula

C29H31N7O.CH4O3S

Molecular Weight

589.715 g/mol

Mechanism of Action

• Inhibits tyrosine kinases, particularly BCR-ABL, c-KIT, and PDGF receptors

Indications

• Chronic Myeloid Leukemia (CML)
• Acute Lymphoblastic Leukemia (ALL)
• Gastrointestinal Stromal Tumors (GIST)
• Dermatofibrosarcoma Protuberans (DFSP)

Common Dosage Forms

• Tablet

Typical Dosage

• 400mg daily for CML
• 600mg daily for GIST

Pediatric Dosage

• Dose based on body weight and condition

Geriatric Dosage

• Usually similar to adult dosage but may require adjustments based on renal function

Side Effects

• Nausea
• Vomiting
• Muscle cramps
• Fluid retention
• Fatigue

Contraindications

• Hypersensitivity to imatinib
• Severe liver disease

Pregnancy Category

• D

Lactation Safety

• Use with caution, potential risk to the infant

Drug Interactions

• Strong CYP3A4 inhibitors
• Strong CYP3A4 inducers
• Proton Pump Inhibitors may decrease imatinib levels

Overdose Symptoms

• Nausea
• Vomiting
• Myelosuppression

Antidote for Overdose

• Supportive care and monitoring

Storage Conditions

• Store at room temperature (20-25°C)
• Protect from light and moisture

Pharmacokinetics

• Absorption: Well absorbed orally
• Distribution: Extensively distributed, including crossing the blood-brain barrier
• Metabolism: Primarily hepatic via CYP3A4
• Excretion: Mainly in feces and urine

Precautions

• Monitor liver function regularly
• Monitor blood counts
• Cardiac monitoring for QT prolongation

Warnings

• Risk of myelosuppression
• Risk of fluid retention and edema
• Potential for severe hepatotoxicity

Others

• Imatinib may need dose adjustment in renal impairment