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Review
. 2023 Jul 28:18:1611-1622.
doi: 10.2147/COPD.S413436. eCollection 2023.

Ensifentrine as a Novel, Inhaled Treatment for Patients with COPD

James F Donohue  1 , Tara Rheault  2 , Margot MacDonald-Berko  2 , Thomas Bengtsson  3 , Kathleen Rickard  2
Affiliations
Review

Ensifentrine as a Novel, Inhaled Treatment for Patients with COPD

James F Donohue et al. Int J Chron Obstruct Pulmon Dis. .

Abstract

Ensifentrine is a novel, potent, and selective dual inhibitor of phosphodiesterase (PDE)3 and PDE4 designed for delivery by inhalation that combines effects on airway inflammation, bronchodilation and ciliary function in bronchial epithelia. In Phase 2 studies in subjects with COPD, ensifentrine demonstrated clinically meaningful bronchodilation and improvements in symptoms and health-related quality of life when administered alone or in combination with current standard of care therapies. Ensifentrine is currently in late-stage clinical development for the maintenance treatment of patients with COPD. This review summarizes non-clinical data as well as Phase 1 and Phase 2 efficacy and safety results of nebulized ensifentrine relevant to the maintenance treatment of patients with COPD.

Keywords: RPL554; chronic obstructive pulmonary disease; clinical efficacy; drug development; nebulized therapy.

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Conflict of interest statement

Margot MacDonald-Berko, Tara Rheault, PhD, and Kathleen Rickard, MD are employees and shareholders of Verona Pharma. Thomas Bengtsson is a paid statistical consultant for Verona Pharma. James F Donohue, MD has consultant and advisory board relationships with Verona Pharma. Dr Kathleen Rickard has a patent Various pending to unknown. The authors report no other conflicts of interest in this work.

Figures

Figure 1
Figure 1
Ensifentrine mechanism of action. Ensifentrine is a novel inhaled, single molecule that is a potent and selective inhibitor of PDE3 and PDE4 in late-stage clinical development for treatment of patients with COPD. PDE3 and PDE4 are expressed on airway smooth muscle, inflammatory cells and bronchial epithelial cells. The dual inhibition of PDE3 and PDE4 by ensifentrine produces additive or synergistic effects compared with inhibition of either PDE3 or PDE4 alone, which results in enhanced effects on bronchodilation, airway inflammation, and mucociliary clearance.
See this image and copyright information in PMC

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