Drug intelligence / Profile preview

tenapanor + midazolam

Development stage
Phase 1
Lead developer
Ardelyx
Modality
Small Molecules
Administration
Oral
01

Overview

**tenapanor + midazolam** is a combination of tenapanor (also known as AZD1722 and RDX5791), a small molecule sodium/hydrogen exchanger 3 (NHE3) inhibitor developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and hyperphosphatemia in chronic kidney disease, with midazolam, an oral benzodiazepine commonly used as a probe substrate for CYP3A4 drug-drug interaction studies. Tenapanor works primarily by inhibiting intestinal NHE3, reducing sodium absorption, and increasing intestinal water content, improving stool frequency and abdominal symptoms in IBS-C. The combination is not a marketed product; it is used specifically in clinical pharmacology studies to evaluate the impact of tenapanor on CYP3A4 activity, using changes in midazolam pharmacokinetics to assess possible drug-drug interactions[3][5][1].

Brand names
Ibsrela + midazolam
Other names
sodium/hydrogen exchanger 3 inhibitor + midazolam
02

Targets

NHE3 (Sodium/hydrogen exchanger 3)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)

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