Imatinib (Gleevec)

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.
Route: PO
Extravasation: n/a
Fertility: evidence of harm

For conciseness and simplicity, HemOnc.org 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.

Diseases for which it is used

• Acute lymphocytic leukemia
• Central nervous system (CNS) cancer
• Chronic myelogenous leukemia
• Mast cell diseases
• Melanoma
• Gastrointestinal stromal tumor (GIST)

Patient drug information

• Imatinib (Gleevec) patient drug information (Chemocare)
• Imatinib (Gleevec) patient drug information (UpToDate)

History of changes in FDA indication

• 5/10/2001: Initial FDA approval

Also Known As

CGP 57148b, Enliven, Gleevac, Imalek, Imatib, Imatinib Mesilate, Imatinib Mesylate, STI-571, Temsan, Veenat.