All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

ensifentrine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
inhibitors of phosphodiesterases	5826	497223-25-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ensifentrine ohtuvayre RPL554 RVT-1601 VMX554 VRP554	Ensifentrine is a first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4). Inhibition of PDE3 and PDE4 increases intracellular cyclic adenosine monophosphate (cAMP) levels. Molecular weight: 564.64 Formula: C33H32N4O5 CLOGP: 4.34 LIPINSKI: 2 HAC: 9 HDO: 0 TPSA: 91.75 ALOGS: ROTB: 6 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

Date	Agency	Company	Orphan
June 26, 2024	FDA	Verona Pharma, Inc.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Dyspnoea	70.05	42.56	44	344	880911	89747148
Chronic obstructive pulmonary disease	47.43	42.56	16	372	73813	90554246

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Dyspnoea	81.34	52.49	44	238	442577	42178476

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Dyspnoea	90.53	38.07	59	478	1106813	109481949
Chronic obstructive pulmonary disease	57.19	38.07	21	516	109137	110479625

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	R03BX02	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS Other drugs for obstructive airway diseases, inhalants
FDA MoA	N0000175086	Phosphodiesterase 3 Inhibitors
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D010726	Phosphodiesterase Inhibitors
MeSH PA	D058987	Phosphodiesterase 3 Inhibitors
MeSH PA	D058988	Phosphodiesterase 4 Inhibitors
FDA EPC	N0000175598	Phosphodiesterase 3 Inhibitor
FDA MoA	N0000182960	Phosphodiesterase 4 Inhibitors
FDA EPC	N0000182961	Phosphodiesterase 4 Inhibitor
CHEBI has role	CHEBI:22587	antiviral agent
CHEBI has role	CHEBI:65023	anti-asthmatic agent

Related Drugs by ATC class:

R03BX Other drugs for obstructive airway diseases, inhalants 1 drug

fenspiride

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Chronic obstructive lung disease	indication	13645005	DOID:3083

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
3MG/2.5ML	OHTUVAYRE	MSD	N217389	June 26, 2024	RX	SUSPENSION	INHALATION	9062047	Aug. 21, 2031	FOR THE MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) IN ADULT PATIENTS
3MG/2.5ML	OHTUVAYRE	MSD	N217389	June 26, 2024	RX	SUSPENSION	INHALATION	9956171	Sept. 15, 2035	FOR THE MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) IN ADULT PATIENTS

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
3MG/2.5ML	OHTUVAYRE	MSD	N217389	June 26, 2024	RX	SUSPENSION	INHALATION	June 26, 2029	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Enzyme	Q14432	PDE3A_HUMAN	INHIBITOR	IC50	9.60		SCIENTIFIC LITERATURE	DRUG LABEL
cAMP-specific 3',5'-cyclic phosphodiesterase 4B	Enzyme	Q07343	PDE4B_HUMAN	INHIBITOR	IC50	6.75		SCIENTIFIC LITERATURE	DRUG LABEL
cAMP-specific 3',5'-cyclic phosphodiesterase 4D	Enzyme	Q08499	PDE4D_HUMAN	INHIBITOR	IC50	7.33		SCIENTIFIC LITERATURE	DRUG LABEL
cGMP-inhibited 3',5'-cyclic phosphodiesterase B	Enzyme	Q13370	PDE3B_HUMAN	INHIBITOR	IC50	9.54		SCIENTIFIC LITERATURE	DRUG LABEL
cAMP-specific 3',5'-cyclic phosphodiesterase 4A	Enzyme	P27815	PDE4A_HUMAN	INHIBITOR	IC50	5.83		IUPHAR

External reference:

ID	Source
1884461-72-6	SECONDARY_CAS_RN
CHEMBL4594287	ChEMBL_ID
C512996	MESH_SUPPLEMENTAL_RECORD_UI
DB16157	DRUGBANK_ID
4043256	VANDF
C1744503	UMLSCUI
CHEBI:757790	CHEBI
10726	INN_ID
9934746	PUBCHEM_CID
386947	MMSL
42949	MMSL
d10199	MMSL
019797	NDDF
11865	IUPHAR_LIGAND_ID
3E3D8T1GIX	UNII
2687215	RXNORM
D11743	KEGG_DRUG

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ohtuvayre	HUMAN PRESCRIPTION DRUG LABEL	1	83034-003	SUSPENSION	3 mg	RESPIRATORY (INHALATION)	NDA	30 sections