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imatinib

Brand and Other Names: Gleevec
Mechanism of Action:

Imatinib mesylate is a protein-tyrosine kinase inhibitor that inhibits the BCR-ABL tyrosine kinase, the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in CML. Imatinib inhibits proliferation and induces apoptosis in BCR-ABL positive cell lines as well as fresh leukemic cells from Philadelphia chromosome positive chronic myeloid leukemia. Imatinib inhibits colony formation in assays using ex vivo peripheral blood and bone marrow samples from CML patients.

Indications:

Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans. Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors.

Route: oral
Dose:

The prescribed dose should be administered orally, with a meal and a large glass of water. Doses of 400 mg or 600 mg should be administered once daily, whereas a dose of 800 mg should be administered as 400 mg twice a day.

Adverse Reactions:

The most frequently reported drug-related adverse reactions were edema, nausea and vomiting, muscle cramps, musculoskeletal pain, diarrhea and rash .

Contraindication:

None

Warnings and Precautions:

Fluid Retention and Edema, Hematologic Toxicity, Congestive Heart Failure and Left Ventricular Dysfunction, Hepatotoxicity, Hemorrhage, Gastrointestinal Disorders, Hypereosinophilic Cardiac Toxicity, Dermatologic Toxicities, Hypothyroidism, Embryo-Fetal Toxicity, Growth Retardation in Children and Adolescents, Tumor Lysis Syndrome, Impairments Related to Driving and Using Machinery, Renal Toxicity

Description:

Imatinib is a small molecule kinase inhibitor.

See package insert for full prescribing information.