Treatment of pain and respiratory indications
Osteoarthritis (OA) pain
Chronic refractory cough
Potent, selective, orally available P2X3 receptor antagonist that blocks ATP hypersensitivity in primary afferents
P2X3 receptors are ATP-gated Na/Ca channels expressed selectively in C- and Aδ primary afferent nerves, and are targets for novel therapies for pain and respiratory indications.
A P2X3 antagonist has shown Phase II efficacy in refractory chronic cough, IC/BPS, OA pain, and in an asthma challenge, but it also caused loss or alteration of taste, believed due to the drug’s inhibition of P2X2/3 receptors.
NEO5937 has high potency and selectivity at P2X3 and is orally efficacious in rat models of inflammatory pain and in a guinea pig cough model. Its higher selectivity for human P2X3 vs. P2X2/3 is expected to provide efficacy without the adverse effects on taste perception that were reported with the less selective P2X3 antagonist.