ticlopidine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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: OFP

  • 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 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 80 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

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
Anaemia 203.87 51.10 57 263 34735 2323030
Rectal haemorrhage 64.25 51.10 16 304 5840 2351925
Melaena 59.26 51.10 14 306 4092 2353673
Aplastic anaemia 54.00 51.10 10 310 894 2356871

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
Anaemia 112.34 56.48 43 397 29414 1716927
Agranulocytosis 83.13 56.48 21 419 3555 1742786
Melaena 75.30 56.48 21 419 5189 1741152
Liver disorder 73.66 56.48 21 419 5615 1740726
Thrombotic microangiopathy 58.28 56.48 13 427 1282 1745059

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
CHEBI has role CHEBI:48676 fibrin modulating drug
CHEBI has role CHEBI:50248 hematologic agent
CHEBI has role CHEBI:50427 platelet aggregation inhibitor
CHEBI has role CHEBI:50249 anticoagulant
MeSH PA D002317 Cardiovascular Agents
MeSH PA D065689 Cytochrome P-450 CYP2C19 Inhibitors
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D005343 Fibrinolytic Agents
MeSH PA D006401 Hematologic Agents
MeSH PA D065606 Metabolic Side Effects of Drugs and Substances
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D010975 Platelet Aggregation Inhibitors
MeSH PA D058914 Purinergic Antagonists
MeSH PA D058919 Purinergic P2 Receptor Antagonists
MeSH PA D058921 Purinergic P2Y Receptor Antagonists

Drug Use (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

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
Alpha-2A adrenergic receptor GPCR Ki 6.84 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 2C19 Enzyme IC50 6.18 DRUG MATRIX
Cytochrome P450 2A6 Enzyme Ki 6.70 WOMBAT-PK
Prostaglandin G/H synthase 1 Enzyme IC50 4.28 WOMBAT-PK
Prostaglandin G/H synthase 2 Enzyme IC50 4.33 WOMBAT-PK
Bile salt export pump Transporter IC50 4.13 CHEMBL
Cytochrome P450 2B6 Enzyme INHIBITOR IC50 6.70 IUPHAR
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 5.70 DRUG MATRIX
Bile salt export pump Unclassified IC50 4.31 CHEMBL

External reference:

IDSource
4020513 VUID
N0000148235 NUI
C0040207 UMLSCUI
D01028 KEGG_DRUG
108971003 SNOMEDCT_US
4020513 VANDF
10594 RXNORM
386950000 SNOMEDCT_US
d00514 MMSL
003610 NDDF
A1L4914FMF UNII
53885-35-1 SECONDARY_CAS_RN
CHEBI:9588 CHEBI
CHEMBL833 ChEMBL_ID
DB00208 DRUGBANK_ID
CHEMBL1717 ChEMBL_ID
3908 INN_ID
TIC PDB_CHEM_ID
5472 PUBCHEM_CID
D013988 MESH_DESCRIPTOR_UI
7307 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Ticlopidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68151-0079 TABLET, FILM COATED 250 mg ORAL ANDA 14 sections