Optimizing Early-stage Clinical Pharmacology Evaluation to Accelerate Clinical Development of Giredestrant in Advanced Breast Cancer.

ABSTRACT:

Purpose

We describe the clinical pharmacology characterization of giredestrant in a first-in-human study.

Experimental design

This phase Ia/Ib dose-escalation/-expansion study (NCT03332797) evaluated the safety, pharmacokinetics, pharmacodynamics, and preliminary antitumor activity of giredestrant in estrogen receptor-positive HER2-negative locally advanced/metastatic breast cancer. The single-agent dose-escalation stage evaluated giredestrant 10, 30, 90, or 250 mg once daily. The dose-expansion stage evaluated single-agent giredestrant at 30, 100, and 250 mg once daily. Dose-escalation and -expansion phases also evaluated giredestrant 100 mg combined with palbociclib 125 mg.

Results

Following single-dose oral administration, giredestrant was rapidly absorbed and gene

SUBMITTER: Malhi V 

PROVIDER: S-EPMC10722959 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature