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Published on: October 3, 2025

The PI3K pathway as drug target in human cancer

Kevin D Courtney1, Ryan B Corcoran, Jeffrey A Engelman

  • 1Massachusetts General Hospital Cancer Center, 149 13th St, Charlestown, 02129, USA.

Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology
|January 21, 2010
PubMed

Insights

Phosphatidylinositol 3-kinase (PI3K) signaling drives cancer growth and survival. This review explores PI3K inhibitors for cancer treatment, emphasizing strategic therapeutic combinations for optimal efficacy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The phosphatidylinositol 3-kinase (PI3K) signaling pathway is crucial for cancer cell proliferation, survival, motility, and metabolism.
  • Aberrant PI3K pathway activation, through genetic mutations or amplifications, is common in various cancers.
  • PI3K signaling also influences noncancerous cells within the tumor microenvironment.

Purpose of the Study:

  • To review the role of PI3K signaling in tumor cell growth and survival.
  • To discuss the development and application of PI3K pathway inhibitors in cancer therapy.
  • To explore strategies for the effective use of PI3K inhibitors, alone or in combination with other treatments.

Main Methods:

  • Literature review of preclinical and clinical studies on PI3K signaling and its inhibitors.
  • Analysis of the biological functions of PI3K in cancer and the tumor microenvironment.
  • Synthesis of current therapeutic strategies targeting the PI3K pathway.

Main Results:

  • PI3K signaling is a central regulator of tumor cell growth and survival.
  • Numerous therapeutics targeting the PI3K pathway are under rapid development.
  • Early studies indicate potential for effective therapeutic strategies, but careful planning is needed due to PI3K's broad biological roles.

Conclusions:

  • Targeting the PI3K pathway holds significant promise for cancer treatment.
  • Sophisticated strategies are required to overcome concerns related to PI3K's fundamental roles in diverse biological processes.
  • Combination therapies involving PI3K inhibitors may offer enhanced efficacy in cancer treatment.

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