Absorption: Well absorbed (98%) following oral administration.
Distribution: Unknown.
Protein Binding: 95%.
Metabolism/Excretion: Mostly metabolized by the CYP3A4 enzyme system to N-demethyl imatinib, which is as active as imatinib. Excreted mostly in feces as metabolites. 5% excreted unchanged in urine.
Half-life: Imatinib 18 hr; N-desmethyl imatinib 40 hr.
Contraindicated in:
Use Cautiously in:
CV: HF.
EENT: epistaxis, nasopharyngitis, blurred vision.
GU: nephrotoxicity.
Neuro: fatigue, headache, weakness, dizziness, somnolence.
Resp: cough, dyspnea, pneumonia.
GI: HEPATOTOXICITY, abdominal pain, anorexia, constipation, diarrhea, dyspepsia, nausea, vomiting.
Derm: DRUG RASH WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), petechiae, pruritus, skin rash.
F and E: edema (including pleural effusion, pericardial infusion, pulmonary edema, and superficial edema), hypokalemia.
Endo: ↓growth (in children), hypothyroidism.
Hemat: BLEEDING, NEUTROPENIA, THROMBOCYTOPENIA.
Metab: weight gain.
MS: arthralgia, muscle cramps, musculoskeletal pain, myalgia.
Misc: TUMOR LYSIS SYNDROME, fever, night sweats.
Drug-Drug:
Drug-Food:
Chronic Myeloid Leukemia
Gastrointestinal Stromal Tumors
Ph+ Acute Lymphoblastic Leukemia
Myelodysplastic/Myeloproliferative Diseases
Aggressive Systemic Mastocytosis
Hypereosinophilic Syndrome and/or Chronic Eosinophilic Leukemia
Dermatofibrosarcoma Protuberans
Hepatic Impairment
Renal Impairment
NDC Code*