General
Preferred name
ENSIFENTRINE
Synonyms
RPL-554 ()
Ensifentrina ()
RPL554 ()
Ls-193855 ()
Ls-193,855 ()
P&D ID
PD143717
CAS
298680-25-8
1884461-72-6
Tags
available
drug
drug candidate
Drug indication
Allergic rhinitis
Drug Status
approved
investigational
Max Phase
3.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
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)
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)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
6
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
16
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
Related compounds
Custom attributes
(extracted from source data)
Pathway
Metabolic Enzyme/Protease
Target
Phosphodiesterase (PDE)
Source data
