Alpelisib in the treatment of metastatic HR plus breast cancer withPIK3CAmutations

Since the US FDA approval of everolimus/exemestane in July 2012, and of the first CDK 4/6 inhibitor, palbociclib, combined with endocrine treatment in February 2015, a third class of therapeutic compounds, the PI3K inhibitors, has been introduced to the arsenal of targeted therapies overcoming endocrine resistance in hormone receptor-positive metastatic breast cancer. Alpelisib (PIQRAY(R)) is the first of these novel agents yielding promising clinical results, giving an impetus to further development of tailored endocrine anticancer treatments. Herein, we review its pharmacodynamic and pharmacokinetic properties, safety and efficacy data, as well as Phase III SOLAR-1 trial, prompting FDA approval of alpelisib in hormone receptor-positive metastatic breast cancer harboringPIK3CAmutations. Furthermore, implications for clinical use and current research will also be discussed.

Automated summary

Alpelisib is the first novel PI3K inhibitor with promising clinical results for hormone receptor-positive metastatic breast cancer harboring PIK3CA mutations, prompting further development of tailored endocrine anticancer treatments.