Abstract
Phosphatidylinositol 3-kinase (PI3K) catalytic subunit p110α (PIK3CA) mutations occur in approximately 40% of patients with hormone receptor-positive, human epidermal growth factor receptor 2 (HER2)-negative breast cancer. Alpelisib, a selective oral inhibitor of PI3K, with inhibitory activity predominantly against PIK3CA, has shown synergistic antitumor activity with endocrine therapy against hormone receptor-positive PIK3CA-mutated breast cancer cells in preclinical and early-phase clinical trials. The combination of alpelisib with fulvestrant or an aromatase inhibitor such as letrozole is safe and effective with reversible toxicities. Although clinical activity has been observed independently of PIK3CA mutation status, clinical improvement has been mostly seen in a higher proportion of patients with PIK3CA-mutated tumors. In this review I share current data on alpelisib in breast cancer treatment.
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