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Gleevec (imatinib)
Gleevec works by blocking the activity of specific enzymes involved in cancer cell growth and proliferation.
Gleevec (imatinib) is a small molecule kinase inhibitor developed by Novartis, targeting the receptor tyrosine-protein kinase erbB-2. It was FDA-approved in 2001 for various indications, including chronic myeloid leukemia, gastrointestinal stromal tumor, and dermatofibrosarcoma protuberans. Gleevec is now off-patent, with 16 generic manufacturers available. Its half-life is 22 hours, and bioavailability is 98%. As a kinase inhibitor, Gleevec works by blocking the activity of specific enzymes involved in cancer cell growth and proliferation.
At a glance
| Generic name | imatinib |
|---|---|
| Sponsor | Novartis |
| Drug class | Kinase Inhibitor |
| Target | Receptor tyrosine-protein kinase erbB-2 |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2001 |
Mechanism of action
Imatinib mesylate is protein-tyrosine kinase inhibitor that inhibits the BCR-ABL tyrosine kinase, the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in CML. Imatinib inhibits proliferation and induces apoptosis in BCR-ABL positive cell lines as well as fresh leukemic cells from Philadelphia chromosome positive chronic myeloid leukemia. Imatinib inhibits colony formation in assays using ex vivo peripheral blood and bone marrow samples from CML patients.In vivo, imatinib inhibits tumor growth of BCR-ABL transfected murine myeloid cells as well as BCR-ABL positive leukemia lines derived from CML patients in blast crisis.Imatinib is also an inhibitor of the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-kit, and inhibits PDGF- and SCF-mediated cellular events. In vitro, imatinib inhibits proliferation and induces apoptosis in GIST cells, which express an activating c-kit m
Approved indications
- Blastic phase chronic myeloid leukemia
- Chronic Myelocytic Leukemia Accelerated Phase
- Chronic eosinophilic leukemia
- Chronic phase chronic myeloid leukemia
- Dermatofibrosarcoma protuberans
- Gastrointestinal stromal tumor
- Idiopathic hypereosinophilic syndrome
- Myelodysplastic/myeloproliferative diseases with re-arrangements of the gene for platelet-derived growth factor receptor (PDGFR)
- Philadelphia Chromosome Positive Chronic Myelocytic Leukemia
- Philadelphia chromosome-positive acute lymphoblastic leukemia
- Systemic mast cell disease
Common side effects
- Fluid retention
- Superficial edema
- Nausea
- Muscle cramps
- Musculoskeletal pain
- Diarrhea
- Rash and related terms
- Fatigue
- Headache
- Joint pain
- Abdominal pain
- Nasopharyngitis
Drug interactions
- CYP3A4 inducers
- CYP3A4 inhibitors
- Grapefruit juice
- Drugs metabolized by CYP3A4
- Warfarin
- Drugs metabolized by CYP2D6
- Methotrexate (high doses >500 mg/m²)
Key clinical trials
- A Treatment Study Protocol for Participants 0-45 Years With Acute Lymphoblastic Leukaemia (PHASE3)
- Asciminib & Standard-of-Care Integration in Maintenance Therapy for POST Allogeneic Stem Cell Transplant (Allo-HSCT) of Patient With Ph+ B-ALL or Blastic Transformed CML (PHASE2)
- Trial of Imatinib for Hospitalized Adults With COVID-19 (PHASE3)
- Neoadjuvant Imatinib and Fampridine in KIT Mutant Gastrointestinal Stromal Tumor (PHASE1)
- Asciminib as Initial Therapy for Patients With Chronic Myeloid Leukemia in Chronic Phase (PHASE2)
- A Study to Evaluate Axatilimab Versus Best Available Therapy in Participants With Chronic Graft Versus Host Disease After at Least 2 Prior Lines of Systemic Therapy (PHASE3)
- Imatinib Mesylate or Dasatinib in Treating Patients With Previously Untreated Chronic Phase Chronic Myelogenous Leukemia (PHASE2)
- A Study to Evaluate Axatilimab Versus Best Available Therapy in Pediatric Participants With Chronic Graft-Versus-Host Disease After at Least 2 Prior Lines of Systemic Therapy (AGAVE-256) (PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Gleevec CI brief — competitive landscape report
- Gleevec updates RSS · CI watch RSS
- Novartis portfolio CI