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Imatinib mesylate (STI571)

M.D. Anderson Cancer Center · Phase 3 active Small molecule

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 other cancers.

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 other cancers. Used for Chronic myeloid leukemia (CML), Philadelphia chromosome positive, Gastrointestinal stromal tumors (GIST), Acute lymphoblastic leukemia (ALL), Philadelphia chromosome positive.

At a glance

Generic nameImatinib mesylate (STI571)
Also known asGleevec, Imatinib, NSC-716051, Glivec/Gleevec
SponsorM.D. Anderson Cancer Center
Drug classTyrosine kinase inhibitor
TargetBCR-ABL, PDGF receptor, c-KIT
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

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 other tyrosine kinases including PDGF receptor and c-KIT, making it effective in additional malignancies.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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