Abstract
With the advent of new agents targeting CD20, Bruton's tyrosine kinase, and phosphoinositol-3 kinase for chronic lymphoid leukemia (CLL), more treatment options exist than ever before. B-cell lymphoma-2 (BCL-2) plays a major role in cellular apoptosis and is a druggable target. Small molecule inhibitors of BCL-2 are in active clinical studies. ABT-199 (venetoclax, RG7601, GDC-0199) has been granted breakthrough designation by FDA for relapsed or refractory CLL with 17p deletion. In this review, we summarized the latest clinical development of ABT-199/venetoclax and other novel agents targeting the BCL-2 proteins.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Agammaglobulinaemia Tyrosine Kinase
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / therapeutic use
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Bridged Bicyclo Compounds, Heterocyclic / pharmacology*
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Bridged Bicyclo Compounds, Heterocyclic / therapeutic use
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Humans
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Leukemia, Lymphoid / drug therapy*
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Leukemia, Lymphoid / metabolism
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Phosphatidylinositol 3-Kinases / metabolism
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Protein-Tyrosine Kinases / drug effects*
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Proto-Oncogene Proteins c-bcl-2 / antagonists & inhibitors
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Proto-Oncogene Proteins c-bcl-2 / metabolism*
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Sulfonamides / pharmacology*
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Sulfonamides / therapeutic use
Substances
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Antineoplastic Agents
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BCL2 protein, human
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Bridged Bicyclo Compounds, Heterocyclic
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Proto-Oncogene Proteins c-bcl-2
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Sulfonamides
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Phosphatidylinositol 3-Kinases
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Protein-Tyrosine Kinases
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Agammaglobulinaemia Tyrosine Kinase
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venetoclax