General
Preferred name
ENSIFENTRINE
Synonyms
Ensifentrina ()
Ensifentrinum ()
RPL-554 ()
Ls-193,855 ()
Ls-193855 ()
Ohtuvayre ()
RPL554 ()
P&D ID
PD143717
CAS
298680-25-8
1884461-72-6
Tags
available
drug
Drug indication
Allergic rhinitis
Chronic obstructive pulmonary disease
Drug Status
approved
investigational
Max Phase
4.0
First approval
2024
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PRICE 157
DESCRIPTION Ensifentrine (RPL-554) is an inhibitor of phosphodiesterases 3 and 4 (PDE3 and PDE4) . It has bronchodilatory action that is mediated by inhibition of PDE3 in airway smooth muscle that is associated with short-term improvement in lung function . Ensifentrine was developed for therapeutic potential in asthma and chronic obstructive pulmonary disease (COPD) . It also also has anti-inflammatory effects in vitro (e.g. reducing TNFα release from human monocytes) and in vivo, likely through inhibtion of PDE4 expressed by inflammatory cells in the lungs . Ensifentrine is active when delivered orally or by inhalation (nebulised) .

COVID-19: A pilot study of ensifentrine in hospitalised COVID-19 patients was initiated in mid-late 2020, but by 2024 no results had been published.

FDA approval of ensifentrine in 2024 made this the first COPD inhalation drug with a new mechanism of action to reach the clinic in more than 20 years. (GtoPdb)
DESCRIPTION Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research[1][2].
DESCRIPTION Ensifentrine (Ensifentrinum) is a PDE3/4 inhibitor, although its affinity for PDE3(IC50: 0.4 nM) is 3,440 times higher than that for PDE4(IC50: 1479 nM), that is under clinical development for the treatment of asthma and COPD and, potentially, cystic fibrosis. (TargetMol Bioactive Compound Library)
Compound Sets
9
Cayman Chemical Bioactives
38761
ChEMBL Approved Drugs
CHEMBL4594287
ChEMBL Drugs
CHEMBL4594287
DrugBank
DB16157
DrugBank Approved Drugs
DB16157
DrugMAP
DMLD4VQ
Guide to Pharmacology
11865
MedChem Express Bioactive Compound Library
HY-119708
TargetMol Bioactive Compound Library
T25376
External IDs
17
Properties
(calculated by RDKit )
Molecular Weight
477.24
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
3
cLogP
2.72
TPSA
112.87
Fraction CSP3
0.35
Chiral centers
0.0
Largest ring
6.0
QED
0.57
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
Phosphodiesterase (PDE)
PDE3
PDE4
Pathway
Metabolism
Metabolic Enzyme/Protease
Source data