The Precision-Guided Use of PI3K Pathway Inhibitors for the Treatment of Solid Malignancies

Phosphatidylinositol-3-kinase (PI3K)/AKT/mammalian target of rapamycin (MTOR) pathway hyperactivation is seen in a multitude of malignancies. Due to the importance of this pathway in numerous critical cellular functions, preclinical and clinical investigations have aimed to target this pathway as an...

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Bibliographic Details
Main Authors: Alexa E. Schmitz, Shirsa Udgata, Katherine A. Johnson, Dustin A. Deming
Format: Article
Language:English
Published: MDPI AG 2025-05-01
Series:Biomedicines
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Online Access:https://www.mdpi.com/2227-9059/13/6/1319
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Summary:Phosphatidylinositol-3-kinase (PI3K)/AKT/mammalian target of rapamycin (MTOR) pathway hyperactivation is seen in a multitude of malignancies. Due to the importance of this pathway in numerous critical cellular functions, preclinical and clinical investigations have aimed to target this pathway as an anti-cancer therapeutic strategy. This has led to the development of PI3K, AKT, and MTOR inhibitors for use in cancer patients, leading to multiple FDA approvals over the past decade. In this review, we outline therapeutic targets in PI3K/AKT/MTOR signaling in solid tumors, the current state of using inhibitors of this pathway to treat patients whose cancers possess activating mutations in <i>PIK3CA</i>, <i>AKT1/2</i>, or <i>MTOR</i>, and exciting new inhibitors that are entering clinical trials.
ISSN:2227-9059