NEO5937

P2X3 RECEPTOR ANTAGONIST

Treatment of pain and respiratory indications

Indications

Osteoarthritis (OA) pain
Visceral pain
Chronic refractory cough

Mode Of Action

Potent, selective, orally available P2X3 receptor antagonist that blocks ATP hypersensitivity in primary afferents

Main Advantages

  • Selective P2X3 antagonist
  • Unique pharmacological profile

Partnered with



Bellus Health


Testimonials

Disease Facts / Medical Need

  • OA pain affects 25% of the adult population; there is a need for analgesics with better long-term tolerability and/or safety than NSAIDs and weak opioids.
  • Interstitial cystitis/bladder pain syndrome (IC/BPS) affects 2.7% of women and 1.3% of men in the US alone; there is a need for effective treatments of the debilitating visceral pain and frequent perception of pressure and urinary urgency.
  • Effective, safe, and well-tolerated antitussives are another important medical need, as 7% of people suffer from chronic cough (>8 weeks); a significant portion of these is refractory to the treatment of associated conditions.

How This Target Works

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.

For more information

Kem Payza

Project Director

514-260-1079 kpayza@neomed.ca
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