Abstract
The deregulated tyrosine kinase activity of the Bcr-Abl fusion protein has been established as the causative molecular event in chronic myelogenous leukemia (CML). Thus the Bcr-Abl tyrosine kinase is an ideal target for pharmacologic inhibition. ST1571 (formerly CGP57148B), is an Abl-specific tyrosine kinase inhibitor that in preclinical studies selectively kills Bcr-Abl-containing cells in vitro and in vivo. The results of clinical studies have demonstrated the potential of molecularly targeted therapies, and ST1571 is emerging as a new therapeutic agent for CML.
MeSH terms
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Antineoplastic Agents / pharmacology*
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Benzamides
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Clinical Trials, Phase I as Topic
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Enzyme Inhibitors / pharmacology*
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Fusion Proteins, bcr-abl / antagonists & inhibitors
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Humans
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Imatinib Mesylate
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Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy*
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Piperazines / pharmacology*
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Piperazines / therapeutic use
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Protein-Tyrosine Kinases / antagonists & inhibitors
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Pyrimidines / pharmacology*
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Pyrimidines / therapeutic use
Substances
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Antineoplastic Agents
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Benzamides
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Enzyme Inhibitors
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Piperazines
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Pyrimidines
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Imatinib Mesylate
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Protein-Tyrosine Kinases
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Fusion Proteins, bcr-abl