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Phosphatidylinositol 3-kinase (PI3K) inhibitors as cancer therapeutics

Akintunde Akinleye, Parthu Avvaru, Muhammad Furqan

  • 1Division of Hematology/Oncology, Department of Medicine, New York Medical College and Westchester Medical Center, Valhalla, NY 10595, USA. DELONG_LIU@NYMC.EDU.

Journal of Hematology & Oncology
|November 23, 2013
PubMed

Insights

Phosphatidylinositol 3-kinases (PI3K) pathway dysregulation drives cancer. This review covers PI3K signaling, inhibitors, and their clinical trials for novel anti-cancer drug development.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Phosphatidylinositol 3-kinases (PI3Ks) are crucial lipid kinases regulating cell proliferation, survival, and motility.
  • Aberrant PI3K pathway signaling is implicated in one-third of human cancers and influences therapeutic responses.
  • PI3K is a validated target for developing novel anti-cancer agents.

Purpose of the Study:

  • To review key molecules within the PI3K signaling pathway.
  • To discuss preclinical models and clinical trials of small-molecule PI3K inhibitors.
  • To highlight idelalisib's advancement in clinical trials for specific lymphomas.

Main Methods:

  • Literature review of PI3K signaling pathways.
  • Analysis of preclinical data for PI3K inhibitors.
  • Summary of clinical trial outcomes for PI3K-targeted therapies.

Main Results:

  • Several potent and selective small-molecule PI3K inhibitors have been developed.
  • At least fifteen PI3K inhibitors have entered clinical trials for cancer treatment.
  • Idelalisib has reached Phase III trials for indolent non-Hodgkin's lymphoma and mantle cell lymphoma.

Conclusions:

  • Small-molecule PI3K inhibitors represent a promising class of anti-cancer drugs.
  • Targeting the PI3K pathway offers therapeutic potential across various malignancies.
  • Ongoing clinical investigations continue to evaluate the efficacy and safety of PI3K inhibitors.

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