From the FDA Drug Label
OHTUVAYRE (ensifentrine) is a sterile, yellow to pale yellow aqueous inhalation suspension of ensifentrine for oral inhalation. Ensifentrine, the active component of OHTUVAYRE, is an inhibitor of phosphodiesterases 3 and 4 (PDE3 and PDE4) The chemical name for ensifentrine is N-(2-{(2E)-9,10-dimethoxy-4-oxo-2-[(2,4,6-trimethylphenyl)imino]-6,7-dihydro-2H-pyrimido[6,1-a]isoquinolin-3(4H)-yl}ethyl)urea; its structural formula is: Ensifentrine has a molecular weight of 477. 56 and its empirical formula is C26H31N5O4.
Ensifentrine is a small molecule that is an inhibitor of the PDE3 and PDE4 enzymes. It is the active component of OHTUVAYRE, a sterile, yellow to pale yellow aqueous inhalation suspension for oral inhalation. Ensifentrine has a molecular weight of 477.56 and an empirical formula of C26H31N5O4. 1 1
From the Research
Ensifentrine is a dual inhibitor medication that targets both phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4) enzymes, primarily used to treat chronic obstructive pulmonary disease (COPD).
Overview of Ensifentrine
Ensifentrine works by simultaneously relaxing airway smooth muscles and reducing inflammation in the lungs, which helps improve breathing in COPD patients. The typical dosage is administered via a nebulizer twice daily.
Mechanism and Benefits
Unlike many other COPD medications, ensifentrine's dual mechanism provides both bronchodilation and anti-inflammatory effects in a single treatment, potentially reducing the need for multiple medications.
Recent Clinical Trials
As shown in the ENHANCE trials 2, ensifentrine significantly improved lung function, reduced the rate of moderate or severe exacerbations, and increased time to first exacerbation in patients with COPD.
Side Effects and Tolerability
Side effects may include cough, headache, and upper respiratory tract infections. Ensifentrine is generally well tolerated, as reported in the phase III ENHANCE clinical trials 2.
Future Role in COPD Treatment
Data from recent clinical trials suggest that ensifentrine can provide additional benefit to existing treatments in patients with COPD and represents a 'first-in-class' drug having bifunctional bronchodilator and anti-inflammatory activity in a single molecule 3.
Key Points
- Ensifentrine is a dual PDE3 and PDE4 inhibitor for the treatment of COPD.
- It provides both bronchodilation and anti-inflammatory effects in a single treatment.
- Ensifentrine is generally well tolerated and can be used in addition to other COPD medications.
- Recent clinical trials have demonstrated its efficacy in improving lung function and reducing exacerbations in patients with COPD.