section name header

Pronunciation

i-MAT-i-nib

Classifications

Therapeutic Classification: antineoplastics

Pharmacologic Classification: enzyme inhibitors

Indications

High Alert


Action

  • Inhibits kinases, which may be produced by malignant cell lines.
Therapeutic effects:
  • Inhibits production of malignant cell lines with decreased proliferation of leukemic cells in CML, hypereosinophilic syndrome and/or chronic eosinophilic leukemia, and ALL and malignant cells in GI stromal tumor, myelodysplastic/myeloproliferative disease, aggressive systemic mastocytosis, and dermatofibrosarcoma protuberans.

Pharmacokinetics

Absorption: Well absorbed (98%) following oral administration.

Distribution: Unknown.

Protein Binding: 95%.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme 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.

Time/Action Profile

(plasma concentrations of imatinib)

ROUTEONSETPEAKDURATION
POunknown2–4 hr24 hr



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

Interactions

Drug-drug:

Route/Dosage

Chronic Myeloid Leukemia

Renal Impairment

Hepatic Impairment

Gastrointestinal Stromal Tumors

Renal Impairment

Hepatic Impairment

Ph+ Acute Lymphoblastic Leukemia

Renal Impairment

Hepatic Impairment

Myelodysplastic/Myeloproliferative Diseases

Renal Impairment

Hepatic Impairment

Aggressive Systemic Mastocytosis

Renal Impairment

Hepatic Impairment

Hypereosinophilic Syndrome and/or Chronic Eosinophilic Leukemia

Renal Impairment

Hepatic Impairment

Dermatofibrosarcoma Protuberans

Renal Impairment

Hepatic Impairment

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Gleevec

Code

NDC Code