Gefapixant is a P2X3 receptor antagonist that reduces the cough reflex in patients with refractory or unexplained chronic cough. It has been estimated that 5-10% of adults globally suffer from chronic cough, which is defined as a cough lasting longer than eight weeks.
- Mechanism
- Curator reviewed · 3 references
Gefapixant is a selective antagonist of P2X3 receptors, with some activity against the P2X2/3 receptor subtype.
P2X3 receptors are ATP-gated ion channels found on sensory C fibers of the vagus nerve in the airways. Under inflammatory conditions, ATP is released from airway mucosal cells where it can subsequently bind to P2X3 receptors on C fibers. The activation of vagal C fibers is perceived as an urge to cough and initiates a cough reflex. Gefapixant inhibits the binding of ATP to P2X3 receptors, thereby reducing excessive C fiber activation by extracellular ATP and dampening the subsequent cough reflex.
- Primary indication
- Gefapixant is indicated in adult patients for the treatment of refractory or unexplained chronic cough.Curator reviewed · 2 structured indications
- Formula / weight
- C14H19N5O4S · 353.4 g/mol (avg)
- First approval
- European Union, 2023
- Code names
- AF-219 · R-1646 · RG-1646 · RO-4926219
- Brand names
Resolves to
HLWURFKMDLAKOD-UHFFFAOYSA-NSMILESCOC1=C(C=C(OC2=CN=C(N)N=C2N)C(=C1)C(C)C)S(N)(=O)=OWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Gefapixant, and which of those have an active Phase 3 trial?
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