Abstract
Asciminib, a first-in-class allosteric inhibitor of BCR::ABL1 kinase activity, is now approved for the treatment of patients with chronic-phase chronic myeloid leukemia who failed 2 lines of therapy or in patients with the T315I mutation. Promising attributes include high specificity and potency against BCR::ABL1, activity against most kinase domain mutations, and potential for combination therapy with ATP-competitive tyrosine kinase inhibitors. Clinicians now have expanded third-line options, which in most cases will involve a choice between asciminib and ponatinib.
© 2022 by The American Society of Hematology.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents* / pharmacology
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Drug Resistance, Neoplasm
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Fusion Proteins, bcr-abl / genetics
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Humans
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Leukemia, Myelogenous, Chronic, BCR-ABL Positive* / drug therapy
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Leukemia, Myelogenous, Chronic, BCR-ABL Positive* / genetics
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Leukemia, Myeloid, Chronic-Phase* / drug therapy
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Mutation
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Niacinamide / analogs & derivatives
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Protein Kinase Inhibitors / pharmacology
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Protein Kinase Inhibitors / therapeutic use
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Pyrazoles
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Treatment Failure
Substances
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Antineoplastic Agents
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Protein Kinase Inhibitors
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Pyrazoles
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asciminib
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Niacinamide
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Fusion Proteins, bcr-abl