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

Stem definitionDrug idCAS RN
2657 55142-85-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ticlopidine
  • ticlop
  • ticlid
  • tiklyd
  • ticlopidine hydrochloride
  • ticlopidine HCl
An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.
  • Molecular weight: 263.78
  • Formula: C14H14ClNS
  • CLOGP: 4.39
  • LIPINSKI: 0
  • HAC: 1
  • HDO: 0
  • TPSA: 3.24
  • ALOGS: -4.08
  • ROTB: 2
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.50 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 15.81 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 80 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.396 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.305 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 24.434 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 76.384 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 0.260 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 1.190 % High 1
herg hERG pIC50 5.266 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 51.761 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 194.536 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.330 % High 1
kinase-safety-class ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK 44
kinase-selectivity-class AKT3,AXL,BRAF,CDK9,EPHB4,GRK2,PDK4,SIK2,TEK 9
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.015 High 1
mh-clint Mouse hepatocyte intrinsic clearance 271.019 High 1
mppb Mouse plasma protein binding (% unbound) 0.660 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.032 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 1.870 % High 1
rh-clint Rat hepatocyte intrinsic clearance 325.087 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 8.390 % High 1
rppb Rat plasma protein binding (% unbound) 0.370 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 1.084 uM High 1

Approvals:

DateAgencyCompanyOrphan
Oct. 31, 1991 FDA

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
Drug interaction 81.80 32.80 52 1385 276401 90350609
Sopor 79.57 32.80 25 1412 24619 90602391
Hyponatraemic syndrome 46.26 32.80 8 1429 566 90626444
Hyperkalaemia 43.48 32.80 21 1416 64943 90562067
Apraxia 40.79 32.80 9 1428 2253 90624757
Hypochloraemia 39.47 32.80 9 1428 2613 90624397
Cerebral haemorrhage 38.63 32.80 16 1421 34506 90592504
Hypercreatininaemia 37.65 32.80 7 1430 746 90626264
Melaena 35.17 32.80 15 1422 34782 90592228

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
Drug interaction 54.06 28.14 58 1559 266941 42352777
Sopor 50.69 28.14 19 1598 13183 42606535
Slow speech 45.07 28.14 11 1606 1779 42617939
Alcohol interaction 43.14 28.14 11 1606 2124 42617594
Electrocardiogram QT prolonged 42.50 28.14 25 1592 47920 42571798
Intentional self-injury 41.18 28.14 17 1600 15185 42604533
Melaena 39.13 28.14 22 1595 38724 42580994
Carotid arteriosclerosis 32.71 28.14 9 1608 2323 42617395
Mechanical urticaria 29.94 28.14 5 1612 117 42619601
Anaemia 29.47 28.14 44 1573 280234 42339484

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
Drug interaction 125.24 26.24 109 3149 500074 110085967
Sopor 120.62 26.24 44 3214 36502 110549539
Melaena 72.70 26.24 37 3221 68720 110517321
Anaemia 58.54 26.24 76 3182 547010 110039031
Intentional self-injury 57.37 26.24 26 3232 37403 110548638
Cerebral haemorrhage 54.60 26.24 30 3228 64938 110521103
Hyponatraemic syndrome 50.58 26.24 10 3248 787 110585254
Hyponatraemia 47.37 26.24 44 3214 217609 110368432
Hyperkalaemia 47.25 26.24 36 3222 135760 110450281
Electrocardiogram QT prolonged 42.63 26.24 31 3227 108929 110477112
Drug abuse 40.80 26.24 37 3221 177374 110408667
Slow speech 40.65 26.24 11 3247 3437 110582604
Alcohol interaction 39.90 26.24 11 3247 3683 110582358
Hypertensive crisis 34.42 26.24 16 3242 24356 110561685
Hypoglycaemia 34.38 26.24 28 3230 116076 110469965
Apraxia 31.24 26.24 9 3249 3531 110582510
Subdural haematoma 31.07 26.24 17 3241 36437 110549604
Hypochloraemia 31.04 26.24 9 3249 3609 110582432
Labelled drug-drug interaction medication error 28.72 26.24 15 3243 29287 110556754

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B01AC05 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Platelet aggregation inhibitors excl. heparin
FDA PE N0000008832 Decreased Platelet Aggregation
FDA EPC N0000175578 Platelet Aggregation Inhibitor
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D005343 Fibrinolytic Agents
MeSH PA D006401 Hematologic Agents
MeSH PA D010975 Platelet Aggregation Inhibitors
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D058921 Purinergic P2Y Receptor Antagonists
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D065689 Cytochrome P-450 CYP2C19 Inhibitors
CHEBI has role CHEBI:48676 fibrin modulating drug
CHEBI has role CHEBI:50248 hematologic agent
CHEBI has role CHEBI:50249 anticoagulant
CHEBI has role CHEBI:50427 platelet aggregation inhibitor
CHEBI has role CHEBI:68563 P2Y<small><sub>12</sub></small> receptor antagonist

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|

DiseaseRelationSNOMED_IDDOID
Percutaneous coronary intervention indication 415070008
Cerebrovascular Occlusion indication
Subacute Stent Thrombosis Prevention indication
Prevention of Cerebral Thrombosis indication
Obstruction of bile duct contraindication 30144000
Gastrointestinal ulcer contraindication 40845000
Hyperlipidemia contraindication 55822004 DOID:1168
Acute nephropathy contraindication 58574008
Blood coagulation disorder contraindication 64779008 DOID:1247
Gastrointestinal hemorrhage contraindication 74474003
Ascorbic acid deficiency contraindication 76169001
Thrombotic thrombocytopenic purpura contraindication 78129009 DOID:10772
Congenital hypoplastic anemia contraindication 88854002 DOID:1339
Leukemia, disease contraindication 93143009 DOID:1240
Procedure on central nervous system contraindication 118679007
Bleeding contraindication 131148009
Arterial aneurysm contraindication 233981004
Cerebral hemorrhage contraindication 274100004
Lumbar puncture contraindication 277762005
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Surgical procedure contraindication 387713003




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.18 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
P2Y purinoceptor 12 GPCR ANTAGONIST WOMBAT-PK CHEMBL
Cytochrome P450 2B6 Enzyme INHIBITOR IC50 6.70 IUPHAR
Prostaglandin G/H synthase 2 Enzyme IC50 4.33 WOMBAT-PK
Prostaglandin G/H synthase 1 Enzyme IC50 4.28 WOMBAT-PK
Alpha-2A adrenergic receptor GPCR Ki 6.85 DRUG MATRIX
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.75 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.86 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 6.77 DRUG MATRIX
Cytochrome P450 2D6 Enzyme IC50 5.20 DRUG MATRIX
Cytochrome P450 2A6 Enzyme Ki 6.70 WOMBAT-PK
Bile salt export pump Transporter IC50 4.13 CHEMBL
Cytochrome P450 2C19 Enzyme IC50 6.18 DRUG MATRIX
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 5.70 DRUG MATRIX
Bile salt export pump Transporter IC50 4.31 CHEMBL

External reference:

IDSource
4020513 VUID
N0000148235 NUI
D01028 KEGG_DRUG
53885-35-1 SECONDARY_CAS_RN
4020458 VANDF
4020513 VANDF
C0040207 UMLSCUI
CHEBI:9588 CHEBI
TIC PDB_CHEM_ID
CHEMBL833 ChEMBL_ID
CHEMBL1717 ChEMBL_ID
DB00208 DRUGBANK_ID
D013988 MESH_DESCRIPTOR_UI
5472 PUBCHEM_CID
7307 IUPHAR_LIGAND_ID
3908 INN_ID
OM90ZUW7M1 UNII
10594 RXNORM
2177 MMSL
31069 MMSL
5582 MMSL
d00514 MMSL
003610 NDDF
003611 NDDF
108971003 SNOMEDCT_US
386950000 SNOMEDCT_US
395904008 SNOMEDCT_US
OM90ZUW7M1 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Ticlopidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68151-0079 TABLET, FILM COATED 250 mg ORAL ANDA 25 sections