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]

Dose adjustments

  • Strong CYP3A4 inducers: increase starting dose by at least 50%, and carefully monitor
  • Mild to moderate hepatic impairment: no adjustment needed
  • Severe hepatic impairment: 25% decrease in recommended dose
  • Mild renal impairment (CrCl 40 to 59): dose no greater than 600 mg/d
  • Moderate renal impairment (CrCl 20 to 39): decrease starting dose by 50%, increase as tolerated but no greater than 400 mg/d
  • Severe renal impairment: use with caution

Diseases for which it is established (work in progress)

Diseases for which it is used

Patient drug information

History of changes in FDA indication

Chronic myelogenous leukemia

  • 5/10/2001: Initial accelerated approval for the treatment of patients with chronic myeloid leukemia (CML) in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy.
    • 12/8/2003: Converted to regular approval.
  • 12/20/2002: Additional accelerated approval for the treatment of newly diagnosed adult patients with Philadelphia chromosome positive chronic myeloid leukemia (CML). (Indication expanded to first-line)
    • 5/27/2009: Converted to regular approval.
  • 5/20/2003: Additional indication for the treatment of pediatric patients with Ph+ chronic phase CML whose disease has recurred after stem cell transplant or who are resistant to interferon alpha therapy. (Indication expanded to the relapsed/refractory pediatric population)
  • 9/27/2006: Additional accelerated approval as a single agent for the treatment of pediatric patients with newly diagnosed Philadelphia chromosome positive chronic myelogenous leukemia (Ph+ CML). (Pediatric indication expanded to first-line)
    • 4/1/2011: Converted to regular approval.

Dermatofibrosarcoma protuberans (DFSP)

Gastrointestinal stromal tumor

Hypereosinophilic syndrome (HES)

Myelodysplastic syndrome


Systemic mastocytosis

History of changes in EMA indication

  • 7/11/2001: Initial marketing authorization as Glivec.

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 1.2 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)