Drug intelligence / Profile preview

SHR2554 + omeprazole

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

This entry represents the **combination of SHR2554, a small molecule inhibitor of enhancer of zeste 2 (EZH2) polycomb repressive complex 2 subunit, and omeprazole, a proton pump inhibitor**. SHR2554 (also known as zeprumetostat) is under development mainly for hematologic malignancies, acting by inhibiting the methyltransferase activity of EZH2, leading to decreased H3K27 trimethylation, ultimately affecting gene expression and impeding tumor cell growth and survival[1][2]. Omeprazole is included here based on its use in a clinical drug-drug interaction study to evaluate the effect of the gastric pH-altering agent on SHR2554 pharmacokinetics; omeprazole itself is a well-established inhibitor of the H+/K+-ATPase in gastric parietal cells and is not an anti-cancer therapy. There are no indications this specific combination is being clinically developed as a fixed-dose or therapeutic combo beyond pharmacokinetic/drug-interaction evaluation.

Other names
omeprazole
02

Targets

EZH2 (Histone-lysine N-methyltransferase EZH2)ATP4A (Potassium–transporting ATPase alpha chain 1)

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