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

Stem definitionDrug idCAS RN
2161 32828-81-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • picotamide
  • picotamide monohydrate
  • picotamide hydrate
Picotamide is an antiplatelet drug with dual mechanism of action it inhibits thromboxane A2 synthase and antagonizes the pharmacological responses mediated by thromboxane A2 receptor.
  • Molecular weight: 376.42
  • Formula: C21H20N4O3
  • CLOGP: 1.10
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 93.21
  • ALOGS: -4.35
  • ROTB: 7

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 50 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.449 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 21.677 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 8.337 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 3.221 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 53.850 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 59.440 % High 1
herg hERG pIC50 4.217 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.315 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 31.261 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 48.270 % High 1
kinase-safety-class ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK1,GRK2,GRK3,ITK,MAP2K6,MAP3K21,MAP3K7,MAPK1,MAPK7,MAPK9,MARK4,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK 38
kinase-selectivity-class AXL,BRAF,EIF2AK3,EPHB4,GRK2,GRK3,MAPK1,PDK1,ROCK1,SIK2 10
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 9.419 High 1
mh-clint Mouse hepatocyte intrinsic clearance 26.669 High 1
mppb Mouse plasma protein binding (% unbound) 58.830 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 19.724 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 68.530 % High 1
rh-clint Rat hepatocyte intrinsic clearance 13.335 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 89.070 % High 1
rppb Rat plasma protein binding (% unbound) 54.080 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 909.913 uM High 1

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B01AC03 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Platelet aggregation inhibitors excl. heparin
MeSH PA D006401 Hematologic Agents
MeSH PA D010975 Platelet Aggregation Inhibitors

Related Drugs by ATC class:

B01AC Platelet aggregation inhibitors excl. heparin 24 drugs
abciximabacetylsalicylic acidaloxiprinberaprostcangrelorcarbasalate calciumcilostazolclopidogrelcloricromendipyridamoleditazoleepoprostenol show all 24 →

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

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.73 acidic
pKa2 12.39 acidic
pKa3 5.2 Basic
pKa4 4.59 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D07140 KEGG_DRUG
C0071043 UMLSCUI
CHEBI:93175 CHEBI
CHEMBL1257015 ChEMBL_ID
DB13327 DRUGBANK_ID
C011581 MESH_SUPPLEMENTAL_RECORD_UI
4814 PUBCHEM_CID
11379 IUPHAR_LIGAND_ID
80530-63-8 SECONDARY_CAS_RN
654G2VCI4Q UNII
654G2VCI4Q INXIGHT DRUGS

Pharmaceutical products:

None