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Efficacy of PI3K inhibitors in advanced breast cancer

B Verret1, J Cortes2,3,4,5, T Bachelot6

  • 1Medical Oncology Department, Gustave Roussy Cancer Campus, Villejuif, France.

Annals of Oncology : Official Journal of the European Society for Medical Oncology
|December 21, 2019
PubMed

Insights

Targeting the phosphoinositide 3 (PI3K)/Akt pathway with inhibitors like alpelisib shows promise for breast cancer, especially in endocrine-resistant cases. This approach offers improved efficacy and toxicity profiles for patients with PIK3CA mutations.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The phosphoinositide 3 (PI3K)/Akt signaling pathway is crucial for breast cancer progression, influencing cell growth, migration, and apoptosis.
  • Deregulation of this pathway, including PIK3CA mutations, is common in breast cancer and linked to endocrine resistance and poor prognosis.

Purpose of the Study:

  • To review current research on PI3K inhibitors in breast cancer treatment.
  • To explore the efficacy and safety of alpelisib, a PI3K inhibitor targeting the p110α isoform.
  • To provide insights into potential future combination therapies involving PI3K inhibitors.

Main Methods:

  • Review of existing scientific literature and clinical trial data on PI3K inhibitors in breast cancer.
  • Analysis of the mechanism of action and clinical outcomes of alpelisib in combination with fulvestrant.
  • Evaluation of the role of PIK3CA mutations in treatment response.

Main Results:

  • Early PI3K inhibitors showed limited activity due to side effects; however, isoform-specific inhibitors like alpelisib have emerged.
  • Alpelisib, in combination with fulvestrant, demonstrated efficacy in patients with endocrine-resistant, PIK3CA-mutant, hormone receptor-positive breast cancer.
  • Alpelisib's specificity for the p110α isoform improved both efficacy and tolerability compared to earlier inhibitors.

Conclusions:

  • PI3K pathway inhibition, particularly with isoform-specific agents like alpelisib, represents a significant advancement in treating specific breast cancer subtypes.
  • Combination strategies involving alpelisib hold promise for enhancing treatment outcomes in endocrine-resistant breast cancer.
  • Further research into novel combinations is warranted to optimize PI3K inhibitor therapy for breast cancer patients.
Keywords:
PI3K inhibitorsbreast cancertargeted therapy

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