Abstract
Prevalent molecular alterations of the phosphoinositide 3-kinase (PI3K) pathway are found on solid tumors and are expressed in leukocytes, making it a desirable target in both solid and hematologic malignancies. In recent years, two agents targeting this pathway have been approved by the United States Food and Drug Administration, idelalisib and copanlisib, with many others under investigation. Due to the off-target effects seen with these agents, those under development have varying isoform specificity that mitigates toxicity. In this review, we attempt to illustrate the varying differences among these agents, both mechanistically as well as highlight differences in their respective adverse effect profiles.
Keywords:
PI3K; copanlisib; idelalisib; phosphoinositide 3-kinase pathway.
© 2018 Pharmacotherapy Publications, Inc.
MeSH terms
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Antineoplastic Agents / administration & dosage*
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Antineoplastic Agents / adverse effects
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Antineoplastic Agents / pharmacology
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Drug Development / methods
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Drugs, Investigational / administration & dosage
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Drugs, Investigational / adverse effects
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Drugs, Investigational / pharmacology
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Enzyme Inhibitors / administration & dosage
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Enzyme Inhibitors / adverse effects
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Enzyme Inhibitors / pharmacology
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Hematologic Neoplasms / drug therapy
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Hematologic Neoplasms / enzymology
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Hematologic Neoplasms / pathology
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Humans
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Molecular Targeted Therapy
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Neoplasms / drug therapy*
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Neoplasms / enzymology
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Neoplasms / pathology
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Phosphatidylinositol 3-Kinase / metabolism
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Phosphoinositide-3 Kinase Inhibitors*
Substances
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Antineoplastic Agents
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Drugs, Investigational
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Enzyme Inhibitors
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Phosphoinositide-3 Kinase Inhibitors
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Phosphatidylinositol 3-Kinase