Ensifentrine is a phosphodiesterase inhibitor used for the maintenance treatment of chronic obstructive pulmonary disease (COPD) in adults. Ensifentrine is a first-in-class, selective dual inhibitor of the phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4) enzymes.
- Mechanism
- Curator reviewed · 10 references
COPD is characterized by progressive airflow obstruction and chronic inflammation of the respiratory tract. Because PDE3 and PDE4 are expressed in airway smooth muscle, inflammatory cells, and bronchial epithelial cells to drive inflammation and bronchial muscle tone, these two PDE isoforms have been identified as therapeutic targets in the treatment of COPD. PDE3 primarily hydrolyzes the second-messenger molecule cyclic adenosine monophosphate (cAMP) in airway smooth muscle, mediating muscle tone. PDE3 can also hydrolyze cyclic guanosine monophosphate (cGMP). PDE4 regulates cAMP only and is involved in inflammatory cell activation and migration, as well as Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) stimulation in bronchial epithelial cells.
Ensifentrine is a drug that selectively inhibits the PDE3 and PDE4 enzymes. Dual inhibition of PDE3 and PDE4 results in the accumulation of intracellular levels of cAMP and/or cGMP, causing a synergistic effect in contracting airway smooth muscle and suppressing inflammatory response.
- Primary indication
- Ensifentrine is indicated for the maintenance treatment of chronic obstructive pulmonary disease (COPD) in adult patients.Curator reviewed · 1 structured indication
- Formula / weight
- C26H31N5O4 · 477.565 g/mol (avg)
- First approval
- United States, 2024
- Also known as
- 2-(9,10-DIMETHOXY-4-OXO-2-(2,4,6-TRIMETHYLPHENYL)IMINO-6,7-DIHYDROPYRIMIDO(6,1-A)ISOQUINOLIN-3-YL)ETHYLUREA · N-(2-((2E)-9,10-DIMETOXI-4-OXO-2-((2,4,6-TRIMETILFENIL)IMINO)-6,7-DIHIDRO-2H-PIRIMIDO(6,1-A)ISOQUINOLEIN-3(4H)-IL)ETIL)UREA · UREA, N-(2-(6,7-DIHYDRO-9,10-DIMETHOXY-4-OXO-2-((2,4,6-TRIMETHYLPHENYL)IMINO)-2H-PYRIMIDO(6,1-A)ISOQUINOLIN-3(4H)-YL)ETHYL)-
- Code names
- LS-193,855 · RPL-554
- Brand names
Resolves to
CSOBIBXVIYAXFM-BYNJWEBRSA-NSMILESCOC1=C(OC)C=C2C(CCN3C(=O)N(CCNC(N)=O)\C(C=C23)=N\C2=C(C)C=C(C)C=C2C)=C1What you can answer from here — as of August 08, 2024
Which other approved drugs treat the same conditions as Ensifentrine, and which companies have late-stage candidates in those indications?
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