Current and Investigational Agents Targeting the Phosphoinositide 3‐Kinase Pathway
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 Stat...
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| Veröffentlicht in: | Pharmacotherapy 2018-10, Vol.38 (10), p.1058-1067 |
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| container_title | Pharmacotherapy |
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| creator | Tang, Laura A. Dixon, Brianne N. Maples, Kathryn T. Poppiti, Kristen M. Peterson, Tim J. |
| description | 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. |
| doi_str_mv | 10.1002/phar.2173 |
| format | Article |
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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. 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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.</description><subject>1-Phosphatidylinositol 3-kinase</subject><subject>copanlisib</subject><subject>idelalisib</subject><subject>Leukocytes</subject><subject>phosphoinositide 3‐kinase pathway</subject><subject>PI3K</subject><subject>Solid tumors</subject><subject>Toxicity</subject><issn>0277-0008</issn><issn>1875-9114</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2018</creationdate><recordtype>article</recordtype><recordid>eNp1kMtOwkAYRidGI4gufAHTxJWLwlw6ly4JUSGSSAyuJ0M7bYdAW2daSXc-gs_okzgIunP1L_6Tky8HgGsEhwhCPKoLZYcYcXIC-khwGsYIRaegDzHnIYRQ9MCFc2uPIhbhc9AjEGEoqOiD5aS1VpdNoMo0mJXv2jUmV42pSrUJxrn_uGCpbK4bU-ZBU-hgUVSuLipTVs40JtUB-fr4fDKlcv6nmmKnuktwlqmN01fHOwCvD_fLyTScPz_OJuN5mBBKSEjThEHBYhJlKYY0iyEXjAvFcRKr1YoqyjjTSZxREnOW6VQlcaKZhoREiKiUDMDtwVvb6q310-W6aq1f7iRGyKuQ8FEG4O5AJbZyzupM1tZsle0kgnLfT-77yX0_z94cje1qq9M_8jeYB0YHYGc2uvvfJBfT8cuP8huZFHsw</recordid><startdate>201810</startdate><enddate>201810</enddate><creator>Tang, Laura A.</creator><creator>Dixon, Brianne N.</creator><creator>Maples, Kathryn T.</creator><creator>Poppiti, Kristen M.</creator><creator>Peterson, Tim J.</creator><general>Wiley Subscription Services, Inc</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QP</scope><scope>7TK</scope><scope>K9.</scope><orcidid>https://orcid.org/0000-0002-8013-3529</orcidid></search><sort><creationdate>201810</creationdate><title>Current and Investigational Agents Targeting the Phosphoinositide 3‐Kinase Pathway</title><author>Tang, Laura A. ; Dixon, Brianne N. ; Maples, Kathryn T. ; Poppiti, Kristen M. ; Peterson, Tim J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3533-5dc6086934fd205f9078678a72c9abb5a5676ec9f53976fedac9ce6e033413ad3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2018</creationdate><topic>1-Phosphatidylinositol 3-kinase</topic><topic>copanlisib</topic><topic>idelalisib</topic><topic>Leukocytes</topic><topic>phosphoinositide 3‐kinase pathway</topic><topic>PI3K</topic><topic>Solid tumors</topic><topic>Toxicity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Tang, Laura A.</creatorcontrib><creatorcontrib>Dixon, Brianne N.</creatorcontrib><creatorcontrib>Maples, Kathryn T.</creatorcontrib><creatorcontrib>Poppiti, Kristen M.</creatorcontrib><creatorcontrib>Peterson, Tim J.</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><jtitle>Pharmacotherapy</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Tang, Laura A.</au><au>Dixon, Brianne N.</au><au>Maples, Kathryn T.</au><au>Poppiti, Kristen M.</au><au>Peterson, Tim J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Current and Investigational Agents Targeting the Phosphoinositide 3‐Kinase Pathway</atitle><jtitle>Pharmacotherapy</jtitle><addtitle>Pharmacotherapy</addtitle><date>2018-10</date><risdate>2018</risdate><volume>38</volume><issue>10</issue><spage>1058</spage><epage>1067</epage><pages>1058-1067</pages><issn>0277-0008</issn><eissn>1875-9114</eissn><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. 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| fulltext | fulltext |
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| ispartof | Pharmacotherapy, 2018-10, Vol.38 (10), p.1058-1067 |
| issn | 0277-0008 1875-9114 |
| language | eng |
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| source | Wiley Journals |
| subjects | 1-Phosphatidylinositol 3-kinase copanlisib idelalisib Leukocytes phosphoinositide 3‐kinase pathway PI3K Solid tumors Toxicity |
| title | Current and Investigational Agents Targeting the Phosphoinositide 3‐Kinase Pathway |
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