Drug intelligence / Profile preview

imlunestrant + omeprazole

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Imlunestrant (LY3484356) is an investigational, orally bioavailable selective estrogen receptor degrader (SERD) being developed by Eli Lilly for the treatment of estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. It functions by binding to the estrogen receptor alpha, inducing its degradation and inhibiting estrogen-dependent signaling pathways that drive tumor growth. Omeprazole is a proton pump inhibitor (PPI) that reduces gastric acid secretion by irreversibly inhibiting the H+/K+-ATPase enzyme in gastric parietal cells. The co-administration of imlunestrant and omeprazole is primarily studied in clinical pharmacology trials to evaluate the effect of increased gastric pH on the absorption and systemic exposure of imlunestrant. Such drug-drug interaction studies are critical for determining whether acid-reducing medications, commonly used by cancer patients, impact the efficacy or safety profile of the therapeutic agent.

Other names
LY3484356 + omeprazole
02

Targets

AHR (Aryl hydrocarbon receptor)ATP4A (Potassium–transporting ATPase alpha chain 1)ER (Estrogen receptor)

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