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Nilotinib, Imatinib

Seoul St. Mary's Hospital · Phase 3 active Small molecule

Nilotinib and Imatinib are tyrosine kinase inhibitors that block BCR-ABL and other kinase signaling pathways to suppress abnormal cell proliferation in chronic myeloid leukemia and gastrointestinal stromal tumors.

Nilotinib and Imatinib are tyrosine kinase inhibitors that block BCR-ABL and other kinase signaling pathways to suppress abnormal cell proliferation in chronic myeloid leukemia and gastrointestinal stromal tumors. Used for Chronic myeloid leukemia (CML), chronic phase, Chronic myeloid leukemia (CML), accelerated phase and blast crisis, Gastrointestinal stromal tumor (GIST), KIT-positive.

At a glance

Generic nameNilotinib, Imatinib
Also known asNilotinib (AMN107): Tasigna, Imatinib (STI571): Gleevec
SponsorSeoul St. Mary's Hospital
Drug classTyrosine kinase inhibitor (TKI)
TargetBCR-ABL, KIT, PDGFRA
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

Both drugs inhibit the constitutively active BCR-ABL fusion protein that drives chronic myeloid leukemia (CML) by binding to the ATP-binding pocket of the kinase domain. Nilotinib is a second-generation inhibitor with improved potency and selectivity compared to imatinib, while imatinib was the first-in-class BCR-ABL inhibitor. Both also inhibit KIT and PDGFRA, making them effective in gastrointestinal stromal tumors (GISTs).

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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