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

Stem definitionDrug idCAS RN
cardiac stimulants, pimobendan derivatives 2171 74150-27-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • UD-CG 115 BS
  • UDCG 115
  • pimobendan
  • acardi
produces arterial & venous dilatation in dogs; structure given in first source
  • Molecular weight: 334.38
  • Formula: C19H18N4O2
  • CLOGP: 2.90
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 79.37
  • ALOGS: -4.36
  • ROTB: 3

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 2 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 14 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.02 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.80 hours Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 62.50 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.992 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 11.776 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 40.832 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 12.474 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 7.740 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 20.340 % High 1
herg hERG pIC50 4.677 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 10.116 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 38.637 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 4.930 % High 1
kinase-safety-class ACVR2B,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,ITK,MAP3K21,MAPK10,MAPK7,MARK4,PDK1,PDK2,PDK4,PIK3CG,PRKDC,TTK 21
kinase-selectivity-class ACVR2A,ACVR2B,BRAF,CAMK2D,DYRK1B,MAP2K6,MAP3K11,MAP3K21,MAPK7,SIK2,SIK3,STK33,TTK,ULK1 14
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 28.314 High 1
mh-clint Mouse hepatocyte intrinsic clearance 33.497 High 1
mppb Mouse plasma protein binding (% unbound) 8.630 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 19.275 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 11.580 % High 1
rh-clint Rat hepatocyte intrinsic clearance 36.392 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 52.930 % High 1
rppb Rat plasma protein binding (% unbound) 3.530 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 10.093 uM High 1

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1994 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cardiac failure 148.05 53.77 43 402 109453 90518549

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cardiac failure 161.32 43.71 62 662 106794 42513817
Cardiac failure chronic 81.48 43.71 21 703 9580 42611031
Low cardiac output syndrome 58.11 43.71 10 714 644 42619967
Renal impairment 44.68 43.71 26 698 110202 42510409

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cardiac failure 264.21 41.79 93 1156 187533 110400517
Renal impairment 89.06 41.79 43 1206 188402 110399648
Cardiac failure chronic 87.23 41.79 22 1227 13789 110574261
Low cardiac output syndrome 70.48 41.79 12 1237 1094 110586956
Blood pressure decreased 53.44 41.79 26 1223 115065 110472985
Concomitant disease aggravated 46.85 41.79 14 1235 16350 110571700
Pulmonary congestion 41.82 41.79 15 1234 30951 110557099

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D010726 Phosphodiesterase Inhibitors
MeSH PA D014665 Vasodilator Agents
MeSH PA D020011 Protective Agents
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:38147 cardiotonic drug
CHEBI has role CHEBI:50218 EC 3.1.4.* (phosphoric diester hydrolase) inhibitor

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

None




🐶 Veterinary Drug Use

SpeciesUseRelation
Dogs Congestive heart failure caused by atrioventricular valvular insufficiency or dilated cardiomyopathy Indication
Dogs Use with concurrent therapy for congestive heart failure Indication

🐶 Veterinary products

ProductApplicantIngredients
Vetmedin Boehringer lngelheim Animal Health USA Inc. 1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.86 acidic
pKa2 11.61 acidic
pKa3 4.76 Basic
pKa4 4.16 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Phosphodiesterase 3 Enzyme INHIBITOR IC50 6.39 CHEMBL SCIENTIFIC LITERATURE
Type-1 angiotensin II receptor GPCR IC50 4.77 CHEMBL

External reference:

IDSource
D01133 KEGG_DRUG
C0071071 UMLSCUI
CHEBI:32003 CHEBI
CHEMBL24646 ChEMBL_ID
DB11450 DRUGBANK_ID
C041648 MESH_SUPPLEMENTAL_RECORD_UI
4823 PUBCHEM_CID
5090 INN_ID
34AP3BBP9T UNII
1110783 RXNORM
017800 NDDF

Pharmaceutical products:

None