Imatinib (Gleevec)

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General information

Class/mechanism: Tyrosine kinase inhibitor, inhibits multiple tyrosine kinases, including Bcr-Abl tyrosine kinase, the constitutively active tyrosine kinase resulting from the Philadelphia chromosome abnormality in CML; the receptor tyrosine kinases for platelet-derived growth factor (PDGF), stem cell factor (SCF), and c-kit, which is the activating mutation found in gastrointestinal stromal tumor (GIST) tumors.[1][2][3]
Route: PO
Extravasation: n/a
Fertility: evidence of harm [4]

For conciseness and simplicity, currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

Also known as

  • Code names: CGP 57148, CGP57148B, STI-571
  • Generic names: imatinib mesilate, imatinib mesylate
  • Brand names: Enliven, Glivec, Gleevac, Gleevec, Imalek, Imatib, Temsan, Veenat


  1. 1.0 1.1 Imatinib (Gleevec) package insert
  2. Imatinib (Gleevec) package insert (locally hosted backup)
  3. Gleevec manufacturer's website
  4. Pye SM, Cortes J, Ault P, Hatfield A, Kantarjian H, Pilot R, Rosti G, Apperley JF. The effects of imatinib on pregnancy outcome. Blood. 2008 Jun 15;111(12):5505-8. Epub 2008 Mar 5. link to original article PubMed
  5. Imatinib (Gleevec) patient drug information (Chemocare)
  6. Imatinib (Gleevec) patient drug information (UpToDate)