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Current and Investigational Agents Targeting the Phosphoinositide 3‐Kinase Pathway
Author(s) -
Tang Laura A.,
Dixon Brianne N.,
Maples Kathryn T.,
Poppiti Kristen M.,
Peterson Tim J.
Publication year - 2018
Publication title -
pharmacotherapy: the journal of human pharmacology and drug therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.227
H-Index - 109
eISSN - 1875-9114
pISSN - 0277-0008
DOI - 10.1002/phar.2173
Subject(s) - idelalisib , phosphoinositide 3 kinase , pi3k/akt/mtor pathway , food and drug administration , kinase , drug development , pharmacology , adverse effect , cancer research , medicine , signal transduction , drug , biology , immunology , microbiology and biotechnology , leukemia , ibrutinib , chronic lymphocytic leukemia
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.