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Background: LSZ102 is an orally bioavailable SERD that inhibits ER gene transcription, induces receptor degradation, and blocks ER-dependent cell growth in preclinical models. This study is evaluating LSZ102 as a single agent and in combination with the CDK 4/6 inhibitor ribociclib (LEE011) or the PI3K inhibitor alpelisib (BYL719) in patients (pts) with ER+ ABC. The LSZ102 single agent data are presented below; combination data are not discussed.

Methods: In the dose-escalation phase evaluating single-agent LSZ102 (Arm A), pts (age ≥18 years; ECOG PS 0-1) with histologically confirmed ER+ ABC and progression on endocrine therapy (ET) received LSZ102. The starting dose was 200 mg once daily. The primary objective of Arm A was to characterize the safety and tolerability of LSZ102 and identify a recommended dose for expansion (RDE). Secondary objectives included preliminary antitumor activity …