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Author Spotlight: Exploring Salidroside's Molecular Mechanisms in Breast Cancer Treatment
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Published on: June 9, 2023

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Efficacy of PI3K inhibitors in advanced breast cancer

B Verret1, J Cortes2, T Bachelot3

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

Annals of Oncology : Official Journal of the European Society for Medical Oncology
|January 14, 2020
PubMed

Insights

Targeting the PI3K/Akt pathway with inhibitors like alpelisib shows promise for breast cancer, especially in endocrine-resistant cases with PIK3CA mutations. Future combinations may improve treatment outcomes.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The phosphoinositide 3 (PI3)-kinase/Akt signaling pathway is crucial in breast cancer, regulating cell growth, proliferation, migration, and apoptosis.
  • Pathway activation correlates with endocrine resistance and poorer prognosis in specific breast cancer subtypes.
  • Deregulation, including PIK3CA mutations, is common in breast cancer.

Purpose of the Study:

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

Main Methods:

  • Review of existing research and clinical trials on PI3K inhibitors in breast cancer.
  • Analysis of data from a large randomized trial leading to alpelisib approval.
  • Examination of the role of PIK3CA mutations and endocrine resistance.

Main Results:

  • Early pan-PI3K inhibitors showed some activity but were limited by side effects.
  • Alpelisib, a specific p110α inhibitor, demonstrated efficacy and improved toxicity in combination with fulvestrant for HR-positive, PIK3CA-mutant, endocrine-resistant breast cancer.
  • The specificity of alpelisib contributes to its therapeutic profile.

Conclusions:

  • PI3K inhibitors, particularly isoform-specific ones like alpelisib, represent a significant advancement in breast cancer therapy.
  • Alpelisib's approval marks a milestone for targeted therapy in endocrine-resistant, PIK3CA-mutant breast cancer.
  • Further research into combination strategies is warranted to optimize PI3K inhibitor treatment for breast cancer patients.
Keywords:
PI3K inhibitorsbreast cancertargeted therapy

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