Ensifentrine

Ensifentrine is a groundbreaking pharmaceutical active ingredient and research compound in respiratory medicine, functioning as the first-in-class inhaled dual PDE3/4 inhibitor for the treatment of chronic obstructive pulmonary disease . As the only dual PDE3/4 inhibitor to successfully complete Phase III clinical trials and receive regulatory approval, Ensifentrine addresses two key aspects of COPD pathology—bronchoconstriction and inflammation—through a single molecule with a novel mechanism of action . This unique profile means that Ensifentrine provides bronchodilation comparable to standard short-acting beta-agonists such as salbutamol (peak FEV1 increase >200 mL) while also delivering anti-inflammatory effects through PDE4 inhibition, all without the significant gastrointestinal side effects associated with oral PDE4 inhibitors like roflumilast . In clinical trials, Ensifentrine demonstrated a markedly improved tolerability profile, with diarrhea occurring in <1% of patients compared to 9-10% for roflumilast . The compound's unique pyrimido[6,1-a]isoquinolin-4-one core and dual PDE3/4 inhibitory activity make Ensifentrine an invaluable tool for respiratory research, as well as a reference standard for analytical method development and quality control applications .

Product Parameters

Medications for the treatment of COPD

Ensefentan, also known as ensafenetan, is a novel, first-in-class inhaled dual inhibitor of PDE3 and PDE4, exhibiting anti-inflammatory activity and bronchodilatory effects. Inhibition of PDE3 can induce smooth muscle relaxation by modulating cyclic adenosine monophosphate (cAMP) levels. In a parallel-controlled Phase III clinical trial, ensefentan administered via a standard nebulizer significantly improved lung function and alleviated dyspnea, though its impact on quality of life was inconsistent. Furthermore, the design of these studies did not aim to evaluate the effect of adding ensefentan to LABA+LAMA or LABA+LAMA+ICS regimens; therefore, it was challenging to fully characterize the drug's role within such treatment protocols. No safety or tolerability issues were observed in these studies. Ensefentan is currently only available in the United States.

Indication

This product is a dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4), indicated for the maintenance therapy of chronic obstructive pulmonary disease (COPD) in adult patients.

Effects

Ensifentrine is the first dual inhaled inhibitor of phosphodiesterase 3 (PDE3) and PDE4, with IC50 values of 0.4 nM and 1,479 nM, respectively. It exhibits bronchodilatory and anti-inflammatory properties and can be used in the study of chronic obstructive pulmonary disease (COPD).

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Respiratory research demands compounds that meet the highest standards of quality and documentation—and Cosperpharm delivers exactly that. Let us show you how we can support your work with Ensifentrine, the first-in-class dual PDE3/4 inhibitor that represents a new era in COPD therapy.