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

Stem definitionDrug idCAS RN
fibrinogen receptor antagonists (glycoprotein IIb/IIIa receptor antagonists) 2680 144494-65-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tirofiban
  • aggrestat
  • tirofiban hydrochloride
  • tirofiban HCl
  • tirofiban hydrochloride monohydrate
  • L-700,462
  • aggrastat
a reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation, when administered intravenously inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner
  • Molecular weight: 440.60
  • Formula: C22H36N2O5S
  • CLOGP: 2
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 104.73
  • ALOGS: -5.14
  • ROTB: 13
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
10 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 65 % Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability) 0 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.34 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.36 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.60 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK,TGFBR1,ZAP70 23
kinase-selectivity-class AXL,CDK4,EIF2AK3,GRK2,TEK 5
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
May 14, 1998 FDA MEDICURE

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
Thrombocytopenia 147.12 89.70 56 636 208669 90419086
Angina pectoris 95.41 89.70 27 665 39133 90588622
Vascular stent thrombosis 89.81 89.70 14 678 1102 90626653

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
Thrombocytopenia 289.76 56.87 127 1046 190152 42430010
Cerebral haemorrhage 78.15 56.87 32 1141 38934 42581228
Vascular stent thrombosis 56.95 56.87 14 1159 3228 42616934

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
Thrombocytopenia 387.14 59.31 159 1598 348726 110238816
Vascular stent thrombosis 135.61 59.31 27 1730 4134 110583408
Pulmonary alveolar haemorrhage 93.27 59.31 27 1730 20123 110567419
Cerebral haemorrhage 93.25 59.31 36 1721 64932 110522610
Coronary artery stenosis 84.46 59.31 23 1734 13735 110573807
Myocardial infarction 79.65 59.31 45 1712 192038 110395504
Cardiogenic shock 75.99 59.31 30 1727 57308 110530234
Acute myocardial infarction 68.17 59.31 31 1726 83746 110503796

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B01AC17 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 D005343 Fibrinolytic Agents
MeSH PA D006401 Hematologic Agents
MeSH PA D010975 Platelet Aggregation Inhibitors
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:48676 fibrin modulating drug
CHEBI has role CHEBI:50249 anticoagulant
CHEBI has role CHEBI:50433 platelet glycoprotein-IIb/IIIa receptor antagonist
CHEBI has role CHEBI:145947 antiatherosclerotic agent

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
Non-Q wave myocardial infarction indication 314207007
Acute coronary syndrome indication 394659003
Percutaneous coronary intervention indication 415070008
Intracranial hemorrhage contraindication 1386000
Acute pericarditis contraindication 15555002
Arteriovenous malformation contraindication 24551003
Acute nephropathy contraindication 58574008
Blood coagulation disorder contraindication 64779008 DOID:1247
Neoplasm of brain contraindication 126952004 DOID:1319
Bleeding contraindication 131148009
Lithotripsy contraindication 133864008
Cerebrovascular accident contraindication 230690007
Arterial aneurysm contraindication 233981004
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Dissection of aorta contraindication 308546005
Surgical procedure contraindication 387713003
Traumatic injury contraindication 417746004
Hypertensive urgency contraindication 443482000
Hemorrhagic Diabetic Retinopathy contraindication
Hemodialysis with High-Flux Membrane contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.02 acidic
pKa2 13.5 acidic
pKa3 10.31 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
Integrin alpha-IIb/beta-3 Adhesion INHIBITOR IC50 7.96 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
4024116 VUID
N0000022121 NUI
D01029 KEGG_DRUG
150915-40-5 SECONDARY_CAS_RN
4021109 VANDF
4024116 VANDF
C0247025 UMLSCUI
CHEBI:9605 CHEBI
AGG PDB_CHEM_ID
CHEMBL916 ChEMBL_ID
CHEMBL3189072 ChEMBL_ID
D000077466 MESH_DESCRIPTOR_UI
DB00775 DRUGBANK_ID
6586 IUPHAR_LIGAND_ID
7345 INN_ID
GGX234SI5H UNII
60947 PUBCHEM_CID
187024 RXNORM
11701 MMSL
252483 MMSL
5588 MMSL
d04315 MMSL
007531 NDDF
007532 NDDF
108981004 SNOMEDCT_US
1269173006 SNOMEDCT_US
386953003 SNOMEDCT_US
412321006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tirofiban Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 14789-101 INJECTION 50 ug INTRAVENOUS ANDA 25 sections
Tirofiban Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 14789-102 INJECTION 50 ug INTRAVENOUS ANDA 25 sections
Tirofiban Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 25021-417 INJECTION, SOLUTION 50 ug INTRAVENOUS ANDA 28 sections
AGGRASTAT HUMAN PRESCRIPTION DRUG LABEL 1 25208-001 INJECTION, SOLUTION 3.75 mg INTRAVENOUS NDA 25 sections
AGGRASTAT HUMAN PRESCRIPTION DRUG LABEL 1 25208-002 INJECTION, SOLUTION 5 mg INTRAVENOUS NDA 25 sections
AGGRASTAT HUMAN PRESCRIPTION DRUG LABEL 1 25208-901 INJECTION, SOLUTION 3.75 mg INTRAVENOUS NDA 25 sections
AGGRASTAT HUMAN PRESCRIPTION DRUG LABEL 1 25208-902 INJECTION, SOLUTION 5 mg INTRAVENOUS NDA 25 sections
Tirofiban Human Prescription Drug Label 1 55150-429 INJECTION, SOLUTION 5 mg INTRAVENOUS ANDA 25 sections
Tirofiban Human Prescription Drug Label 1 55150-430 INJECTION, SOLUTION 12.50 mg INTRAVENOUS ANDA 25 sections
Tirofiban hydrochloride Human Prescription Drug Label 1 68083-145 INJECTION, SOLUTION 12.50 mg INTRAVENOUS ANDA 25 sections