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imatinib (IM)
Imatinib is a tyrosine kinase inhibitor that blocks the BCR-ABL fusion protein and other kinases, preventing abnormal cell proliferation in chronic myeloid leukemia and gastrointestinal stromal tumors.
Imatinib is a tyrosine kinase inhibitor that blocks the BCR-ABL fusion protein and other kinases, preventing abnormal cell proliferation in chronic myeloid leukemia and gastrointestinal stromal tumors. Used for Chronic myeloid leukemia (CML), Philadelphia chromosome positive, Gastrointestinal stromal tumor (GIST), KIT-positive, Acute lymphoblastic leukemia (ALL), Philadelphia chromosome positive.
At a glance
| Generic name | imatinib (IM) |
|---|---|
| Also known as | Gleevec |
| Sponsor | First Affiliated Hospital, Sun Yat-Sen University |
| Drug class | Tyrosine kinase inhibitor |
| Target | BCR-ABL, KIT, PDGFRA |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
Mechanism of action
Imatinib selectively inhibits the constitutively active BCR-ABL tyrosine kinase that results from the Philadelphia chromosome translocation in chronic myeloid leukemia (CML). By blocking this kinase, it prevents the downstream signaling that drives uncontrolled myeloid cell proliferation. The drug also inhibits KIT and PDGFRA kinases, making it effective in gastrointestinal stromal tumors (GISTs) driven by these mutations.
Approved indications
- Chronic myeloid leukemia (CML), Philadelphia chromosome positive
- Gastrointestinal stromal tumor (GIST), KIT-positive
- Acute lymphoblastic leukemia (ALL), Philadelphia chromosome positive
Common side effects
- Nausea
- Vomiting
- Diarrhea
- Edema (fluid retention)
- Muscle cramps
- Rash
- Fatigue
- Myelosuppression (anemia, thrombocytopenia, neutropenia)
- Hepatotoxicity
Key clinical trials
- Efficacy and Safety of Nilotinib in Patients With a Chronic Disease of the Graft Against the Host (PHASE2)
- Comparison of Clinical Efficacy of Liver Resection, RFA, TACE, and Drug Therapy in Patients with GIST LM
- Correlation Between Imatinib Trough Concentration and Efficacy in Advanced GIST Patients with Different Genotypes
- DS-6157a in Participants With Advanced Gastrointestinal Stromal Tumor (GIST) (PHASE1)
- Ph+/Bcr-Abl+ ALL Imatinib and Nilotinib Rotational Study (PHASE2)
- Evaluating the Safety and Immunogenicity of a Prime-boost Vaccine Regimen of GEO-D02 DNA and MVA/HIV62B With and Without B63521^11 gp120 and IHV01 gp120 Env Proteins in Healthy, HIV-uninfected Adult Participants (PHASE1)
- Phase III Trial Evaluating the Effectiveness of a Dose Adjustment of Imatinib Mesylate on the Molecular Response (PHASE3)
- Etoposide, Prednisone, Vincristine Sulfate, Cyclophosphamide, and Doxorubicin Hydrochloride With Asparaginase in Treating Patients With Acute Lymphoblastic Leukemia or Lymphoblastic Lymphoma (PHASE2)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |