Ensifentrine

Highest phase reached
Approved
www.ebi.ac.uk
Drug type
Small molecule
www.ebi.ac.uk
First approval year
2024
www.ebi.ac.uk

First approval year
2024
www.ebi.ac.uk
Listing at source
Listed
Highest phase reached
Approved
www.ebi.ac.uk

Drug type
Small molecule
www.ebi.ac.uk
Drug name
Ensifentrine
www.ebi.ac.uk
Molecular weight
477.57
www.ebi.ac.uk
Structure (SMILES)
COc1cc2c(cc1OC)-c1c/c(=N\c3c(C)cc(C)cc3C)n(CCNC(N)=O)c(=O)n1CC2
www.ebi.ac.uk

  • ohtuvayre
  • Ohtuvayre

  • ensifentrina
  • Ensifentrina
  • ensifentrine
  • Ensifentrine
  • ensifentrine [INN]
  • Ensifentrine [MI]
  • ENSIFENTRINE [USAN]
  • Ensifentrine [WHO-DD]
  • Ensifentrine 1.5 mg
  • Ensifentrine 3 mg
  • Ensifentrine 3 mg (marketed formulation)
  • ensifentrine inn
  • ensifentrine mi
  • ensifentrine usan
  • ensifentrine who dd
  • ls 193 855
  • ls 193855
  • Ls-193,855
  • Ls-193855
  • rpl 554
  • RPL-554
  • rpl554
  • RPL554
  • RPL554 suspension
  • RPL554 Suspension

CAS registry numbers
  • 1884461-72-6
ChEMBL ID
CHEMBL4594287
www.ebi.ac.uk
InChIKey
CSOBIBXVIYAXFM-BYNJWEBRSA-N
www.ebi.ac.uk
PubChem compound IDs
  • 9934746
RxNorm IDs (RxCUI)
  • 2687215
FDA ingredient codes (UNII)
  • 3E3D8T1GIX

  • R03BX
  • R03BX02
Sources for recorded values
mor.nlm.nih.gov

Applicant
MSD
Approval date
26 Jun 2024
Application number
NDA217389

Status
application_withdrawn
Status date
30 Oct 2025
Approved indications
Maintenance treatment in symptomatic adult patients with chronic obstructive pulmonary disease (COPD).
Product number
EMEA/H/C/006742
Authorisation holder
Verona Pharma Ireland Limited
Priority medicines scheme
No
Generic
No
Biosimilar
No
Generic medicines
0
Biosimilar medicines
0
Advanced therapy
No
Conditional approval
No
Additional monitoring
No
Accelerated assessment
No
Exceptional circumstances
No

Therapeutic areas

  • Pulmonary Disease, Chronic Obstructive
European medicines record
www.ema.europa.eu

Patents
5
Designations
0
Earliest recorded loss of exclusivity
25 Jun 2044
First in class
No
Fast track
No
Breakthrough designation
No
Orphan designation
No
Priority review
No
Orphan exclusivity
No
Accelerated approval
No
Availability
Prescription only

Pharmacology name
ensifentrine
Type
Synthetic organic
Drug name stem
-fentrine
Approval recorded by Guide to Pharmacology
Yes

Administration routes

  • topical

  • Action
    Inhibition
    Action type
    Inhibitor
    Target
    phosphodiesterase 4A
    Gene symbol
    PDE4A
    Protein identifier
    P27815
    Median affinity
    5.83
    Affinity units
    pIC50
  • Action
    Inhibition
    Action type
    Inhibitor
    Target
    phosphodiesterase 3A
    Gene symbol
    PDE3A
    Protein identifier
    Q14432
    Median affinity
    9.4
    Affinity units
    pIC50
  • Mechanism
    Phosphodiesterase 3 inhibitor
    Action type
    Inhibitor
    Target
    Phosphodiesterase 3
    Protein identifier
    Q13370
  • Mechanism
    Phosphodiesterase 3 inhibitor
    Action type
    Inhibitor
    Target
    Phosphodiesterase 3
    Protein identifier
    Q14432
  • Mechanism
    Phosphodiesterase 4 inhibitor
    Action type
    Inhibitor
    Target
    Phosphodiesterase 4
    Protein identifier
    P27815
  • Mechanism
    Phosphodiesterase 4 inhibitor
    Action type
    Inhibitor
    Target
    Phosphodiesterase 4
    Protein identifier
    Q07343
  • Mechanism
    Phosphodiesterase 4 inhibitor
    Action type
    Inhibitor
    Target
    Phosphodiesterase 4
    Protein identifier
    Q08493
  • Mechanism
    Phosphodiesterase 4 inhibitor
    Action type
    Inhibitor
    Target
    Phosphodiesterase 4
    Protein identifier
    Q08499

  • Mechanism
    Phosphodiesterase 3 inhibitor
    Action type
    Inhibitor
    Target
    Phosphodiesterase 3
  • Mechanism
    Phosphodiesterase 4 inhibitor
    Action type
    Inhibitor
    Target
    Phosphodiesterase 4

  • Condition
    Pulmonary Disease, Chronic Obstructive
    Highest recorded phase
    4
    Condition identifier
    EFO:0000341
    Subject identifier
    D029424
  • Condition
    Asthma
    Highest recorded phase
    2
    Condition identifier
    MONDO:0004979
    Subject identifier
    D001249
  • Condition
    Pulmonary Disease, Chronic Obstructive
    Highest recorded phase
    4
    Condition identifier
    MONDO:0005002
    Subject identifier
    D029424
  • Condition
    Cystic Fibrosis
    Highest recorded phase
    2
    Condition identifier
    MONDO:0009061
    Subject identifier
    D003550
  • Condition
    Severe Acute Respiratory Syndrome
    Highest recorded phase
    2
    Condition identifier
    MONDO:0100096
    Subject identifier
    D045169

  • Condition identifier
    EFO_0000341
    Highest recorded phase
    3
  • Condition identifier
    EFO_0005854
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0004979
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005002
    Highest recorded phase
    4
  • Condition identifier
    MONDO_0009061
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0011786
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0100096
    Highest recorded phase
    2

Dose
3 mg
Route
Inhalation
How often
Twice daily

Conditions of use

  • Administer using a standard jet nebulizer with a mouthpiece

Hydrogen bond acceptors
7
Hydrogen bond donors
2
Polar surface area
112.87
Calculated partition coefficient (ALogP)
2.72
Calculated partition coefficient (XLogP)
2.7
Prodrug
No
Chirality
Achiral
Inorganic
No
Rule-of-five violations
0
Rotatable bonds
6
Heavy atoms
35
Molecular formula
C26H31N5O4
Monoisotopic mass
477.23760449
Natural product
No

  • 83034-003

Recorded assays
6
Active assays
5

Active assay types

  • Confirmatory

Related records

Trials (18)

Approved for (1)

In development for (4)

Targets (6)