Current and Investigational Agents Targeting the Phosphoinositide 3-Kinase Pathway

Laura A Tang1, Brianne N Dixon1, Kathryn T Maples1

  • 1Department of Pharmacy, Memorial Sloan Kettering Cancer Center, New York.

Pharmacotherapy
|August 19, 2018
PubMed

Insights

Targeting the phosphoinositide 3-kinase (PI3K) pathway is crucial for treating various cancers. Newer PI3K inhibitors offer improved isoform specificity to reduce side effects compared to earlier treatments.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The phosphoinositide 3-kinase (PI3K) pathway is frequently altered in solid tumors and hematologic malignancies.
  • Approved PI3K inhibitors like idelalisib and copanlisib have shown efficacy but are associated with off-target toxicities.

Purpose of the Study:

  • To review and compare emerging PI3K inhibitors.
  • To highlight mechanistic differences and adverse effect profiles of these agents.

Main Methods:

  • Literature review of PI3K pathway inhibitors.
  • Analysis of mechanistic data and clinical trial results.
  • Comparison of adverse event profiles.

Main Results:

  • Newer PI3K inhibitors are being developed with enhanced isoform specificity.
  • These agents aim to mitigate the toxicity associated with earlier, less specific inhibitors.
  • Significant differences exist in the mechanistic actions and side effect profiles among investigational PI3K agents.

Conclusions:

  • Isoform-specific PI3K inhibitors represent a promising advancement in cancer therapy.
  • Understanding these differences is critical for optimizing treatment strategies and managing patient safety.
  • Further research is needed to fully elucidate the therapeutic potential and safety of novel PI3K inhibitors.

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