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30 January 2026

Comparison Between Alpelisib Plus Endocrine Therapy and Everolimus Plus Endocrine Therapy After CDK4/6 Inhibitors Progression in Patients with PIK3CA-Mutant Metastatic Breast Cancer: A Single-Center Retrospective Study

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1
Department of Medical Oncology, Bank of Cyprus Oncology Center, 32 Acropoleos Avenue, Nicosia 2006, Cyprus
2
Department of Medical Oncology, German Medical Institute, 1 Nikis Avenue, Limassol 4108, Cyprus
3
Biostatistics Unit, The Cyprus Institute of Neurology and Genetics, 6 Iroon Avenue, Nicosia 2371, Cyprus
4
School of Medicine, University of Cyprus, Panepistimiou 1, Nicosia 2408, Cyprus
This article belongs to the Section Cancer Drug Development

Simple Summary

Alpelisib, an α-specific PI3K inhibitor, was approved as the first targeted therapy against PIK3CA-mutant metastatic breast cancer. Nevertheless, its efficacy post CDK4/6 inhibitors failure has not yet been tested in a randomized trial. Everolimus, an mTOR inhibitor, is still in use in many countries, but, like alpelisib, it has never been evaluated at a randomized trial level after CDK4/6 inhibitor failure in PIK3CA-mutant metastatic breast cancer. In this single-center retrospective study, we compare alpelisib plus endocrine therapy with everolimus plus endocrine therapy in patients with PIK3CA-mutant metastatic breast cancer who progressed on CDK4/6 inhibitors.

Abstract

Background: Evidence on the efficacy of alpelisib in combination with fulvestrant after progression on CKD4/6 inhibitors (CDK4/6i) is derived from a single non-comparative prospective study. Conversely, the effectiveness of everolimus plus exemestane on PIK3CA-mutant metastatic breast cancer (BC) after CDK4/6i failure has never been investigated in a prospective study. In this retrospective study, we compared alpelisib plus endocrine therapy (ET) with everolimus plus exemestane in patients with PIK3CA-mutant metastatic BC post-CDK4/6i progression. Methods: We tracked 40 patients treated with alpelisib plus ET and 22 treated with everolimus plus exemestane. We further identified 42 patients who did not harbor PIK3CA mutations (PIK3CA-wild-type group) and received everolimus as a subsequent treatment after progression on CDK4/6i. The timeframe spanned from 1st March 2020 to 30th November 2024. Results: The median progression-free survival (PFS) for the alpelisib group was 4.9 months compared to 4.5 months for the everolimus group [Hazard ratio (HR), 1.22; 95% CI, 0.65–2.28; p-value = 0.53]. The median overall survival (OS) was 9.6 months and 18.3 months for alpelisib and everolimus, respectively (HR, 0.67; 95% CI, 0.25–1.76; p-value = 0.47). Median PFS in the PIK3CA-mutant everolimus plus ET group was 4.5 months (95% CI, 2.8–6.7) compared to 5 months (95% CI, 3.5–6.9) for the PIK3CA-wild-type everolimus plus ET group (HR, 0.77; 95% CI, 0.46–1.29; p-value = 0.32). The most common side effects in the alpelisib group were hyperglycemia (57.5%), rash (27.5%), and anorexia (22.5%), while the most common side effects in the everolimus group were fatigue (40.9%) and stomatitis (27.3%). Conclusion: Our results regarding the efficacy of alpelisib plus ET were inferior to those reported in the current literature. Conversely, outcomes of everolimus plus exemestane were consistent with the current literature, denoting that the combination is an acceptable treatment option for patients with PIK3CA-mutant metastatic BC.

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