BELLUS Health's lead product candidate, BLU-5937, is a potent, highly selective, orally bioavailable small molecule antagonist of the P2X3 receptor, a clinically validated target for chronic cough. BLU-5937 has the potential to be an important treatment option for chronic cough and chronic pruritus patients.

In July 2019, the Company announced that the first patient had been enrolled in the Phase 2 study of BLU-5937 for the treatment of refractory chronic cough. The Phase 2 study will evaluate the efficacy of BLU-5937 and is expected to add to the Phase 1 evidence showing little to no impact on taste. Top-line results are expected in mid-2020. The Company also announced in July 2019 that it was expanding the BLU-5937 P2X3 antagonist platform to chronic pruritus. A Phase 2 study in chronic pruritus associated with atopic dermatitis ("AD"), also known as eczema, is expected to be initiated in 2020.

BLU-5937 has been shown to be highly selective (>1500 fold) for human P2X3 receptors versus P2X2/3 receptors. The P2X3 receptor in the cough reflex pathway is a rational target for treating refractory chronic cough, and it has been validated in multiple clinical studies. With a modestly-selective P2X3 antagonist therapy for chronic cough, an adverse effect on taste perception is a well-known and widely-documented tolerability issue. The Company believes that a highly selective P2X3 antagonist can reduce coughing in patients with chronic cough, while maintaining taste function by not inhibiting P2X2/3 receptors.

In addition to chronic cough and chronic pruritus, BLU-5937 may potentially have clinical benefit in other afferent hypersensitization-related disorders, such as visceral pain, hypertension, and migraine, among others. BELLUS Health is exploring how P2X3 activation can contribute to irritation and pain, and how inhibition of P2X3 receptors may be able to help treat these afferent hypersensitization-related disorders.


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