Drug intelligence / Profile preview

gefapixant + omeprazole

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

Overview

**Gefapixant + omeprazole** is a combination of two pharmaceuticals used in clinical studies to assess pharmacokinetic and bioavailability effects. **Gefapixant** is a selective *P2X3 receptor antagonist* developed as an oral treatment for refractory or unexplained chronic cough. It acts primarily by blocking ATP-gated P2X3 ion channels on vagus nerve sensory fibers, thereby inhibiting cough reflex sensitization during inflammatory airway conditions. **Omeprazole** is a *proton pump inhibitor (PPI)* that suppresses gastric acid secretion by antagonizing the H+/K+ ATPase enzyme in gastric parietal cells. Clinical coadministration is used to assess the effect of gastric pH on gefapixant absorption. Data from multiple phase 1 crossover and bioequivalence studies indicate that omeprazole does not have a clinically meaningful effect on gefapixant pharmacokinetics or exposure for the commercial citrate salt formulation.

Other names
gefapixant citrateP2X3 receptor antagonistP-2X3 receptor antagonistP 2X3 receptor antagonist
02

Targets

ATP4A (Potassium–transporting ATPase alpha chain 1)P2RX1 (Purinergic receptor P2X 1)P2X3 (P2X purinoceptor 3)P2XR (P2X receptor family)

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