Tirofiban

Highest phase reached
Drug type
Small molecule
First approval year

First approval year
Listing at source
Listed
Highest phase reached

Drug type
Small molecule
Drug name
Tirofiban
Molecular weight
Structure (SMILES)
CCCCS(=O)(=O)N[C@@H](Cc1ccc(OCCCCC2CCNCC2)cc1)C(=O)O

  • agrastat
  • Agrastat
  • tirofiban
  • Tirofiban
  • TIROFIBAN [HSDB]
  • tirofiban [INN]
  • TIROFIBAN [MI]
  • TIROFIBAN [VANDF]
  • Tirofiban [WHO-DD]
  • tirofiban hsdb
  • tirofiban inn
  • tirofiban mi
  • tirofiban vandf
  • tirofiban who dd

ATC classification codes
  • B01AC17
Sources for recorded values
CAS registry numbers
  • 144494-65-5
ChEMBL ID
CHEMBL916
InChIKey
COKMIXFXJJXBQG-NRFANRHFSA-N
FDA ingredient codes (UNII)
  • GGX234SI5H

  • 60947
  • 40466968

  • 73137
  • 253202

Applicant
MEDICURE
Approval date
14 May 1998
Application number
NDA020912

First in class
No
Orphan designation
No
Availability
Prescription only

United States (FDA)
Approved

Pharmacology name
tirofiban
Type
Synthetic organic
Drug name stem
-fiban
Approval recorded by Guide to Pharmacology
Yes

Administration routes

  • Parenteral

  • Action
    Inhibition
    Action type
    Inhibitor
    Target
    integrin αIIbβ3
    Gene symbol
    ITGA2B
    Protein identifier
    P05106
    Median affinity
    9.43
    Affinity units
    pIC50
    Primary target
    Yes
  • Action
    Inhibition
    Action type
    Inhibitor
    Target
    integrin αIIbβ3
    Gene symbol
    ITGB3
    Protein identifier
    P08514
    Median affinity
    9.43
    Affinity units
    pIC50
    Primary target
    Yes

Open Targets mechanisms

  • Mechanism
    Integrin alpha-IIb/beta-3 inhibitor
    Action type
    Inhibitor
    Target
    Integrin alpha-IIb/beta-3

DrugCentral mechanisms

  • Action type
    Inhibitor
    Gene symbol
    ITGB3|ITGA2B
    Protein identifier
    P05106|P08514
    Organism
    Homo sapiens
    Target development level
    Clinical

  • Condition
    Myocardial Infarction
    Highest recorded phase
    3
    Condition identifier
    EFO:0000612
    Subject identifier
    D009203
  • Condition
    Stroke
    Highest recorded phase
    2
    Condition identifier
    EFO:0000712
    Subject identifier
    D020521
  • Condition
    Coronary Disease
    Highest recorded phase
    3
    Condition identifier
    EFO:0001645
    Subject identifier
    D003327
  • Condition
    Atherosclerosis
    Highest recorded phase
    3
    Condition identifier
    EFO:0003914
    Subject identifier
    D050197
  • Condition
    Venous Thromboembolism
    Highest recorded phase
    2
    Condition identifier
    EFO:0004286
    Subject identifier
    D054556
  • Condition
    Acute Coronary Syndrome
    Highest recorded phase
    3
    Condition identifier
    EFO:0005672
    Subject identifier
    D054058
  • Condition
    Pneumonia, Viral
    Highest recorded phase
    2
    Condition identifier
    EFO:0007541
    Subject identifier
    D011024
  • Condition
    Myocardial Infarction
    Highest recorded phase
    3
    Condition identifier
    EFO:0008583
    Subject identifier
    D009203
  • Condition
    Respiratory Insufficiency
    Highest recorded phase
    2
    Condition identifier
    EFO:0009686
    Subject identifier
    D012131
  • Condition
    Renal Insufficiency
    Highest recorded phase
    1
    Condition identifier
    HP:0000083
    Subject identifier
    D051437
  • Condition
    Ischemic Stroke
    Highest recorded phase
    2
    Condition identifier
    HP:0002140
    Subject identifier
    D000083242
  • Condition
    Thrombosis
    Highest recorded phase
    4
    Condition identifier
    HP:0004419
    Subject identifier
    D013927
  • Condition
    Severe Acute Respiratory Syndrome
    Highest recorded phase
    2
    Condition identifier
    MONDO:0100096
    Subject identifier
    D045169

  • Condition identifier
    EFO_0000612
    Highest recorded phase
    3
  • Condition identifier
    EFO_0000712
  • Condition identifier
    EFO_0001645
    Highest recorded phase
    3
  • Condition identifier
    EFO_0005672
  • Condition identifier
    EFO_0008583
    Highest recorded phase
    3
  • Condition identifier
    HP_0000083
    Highest recorded phase
    1
  • Condition identifier
    HP_0001297
    Highest recorded phase
    3
  • Condition identifier
    HP_0002140
    Highest recorded phase
    3
  • Condition identifier
    HP_0004419
  • Condition identifier
    HP_0004419
    Highest recorded phase
    4
  • Condition identifier
    MONDO_0001106
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0004781
  • Condition identifier
    MONDO_0005010
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005068
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0005098
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005098
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0005099
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005542
    Highest recorded phase
    4
  • Condition identifier
    MONDO_1060198
    Highest recorded phase
    3

  • Event
    abdominal discomfort
    Reports
    1
    Reporting signal score
    8.2813
  • Event
    abdominal pain
    Reports
    5
    Reporting signal score
    12.8396
  • Event
    abdominal pain upper
    Reports
    1
    Reporting signal score
    12.1071
  • Event
    acute kidney injury
    Reports
    1
    Reporting signal score
    14.6134
  • Event
    acute myocardial infarction
    Reports
    14
    Reporting signal score
    7.77274
  • Event
    angina pectoris
    Reports
    129
    Reporting signal score
    335.801
  • Event
    anxiety
    Reports
    1
    Reporting signal score
    15.718
  • Event
    arrhythmia
    Reports
    28
    Reporting signal score
    29.0962
  • Event
    asthenia
    Reports
    1
    Reporting signal score
    30.4318
  • Event
    atrial fibrillation
    Reports
    1
    Reporting signal score
    7.52315
  • Event
    back pain
    Reports
    3
    Reporting signal score
    11.2835
  • Event
    blood pressure increased
    Reports
    1
    Reporting signal score
    8.46476
  • Event
    capsular warning syndrome
    Reports
    4
    Reporting signal score
    26.1662
  • Event
    cardiac failure
    Reports
    62
    Reporting signal score
    79.5914
  • Event
    cardiac failure acute
    Reports
    11
    Reporting signal score
    20.6309
  • Event
    cerebral haemorrhage
    Reports
    86
    Reporting signal score
    211.949
  • Event
    condition aggravated
    Reports
    1
    Reporting signal score
    24.4328
  • Event
    coronary artery restenosis
    Reports
    4
    Reporting signal score
    9.49702
  • Event
    coronary artery stenosis
    Reports
    10
    Reporting signal score
    15.4602
  • Event
    coronary revascularisation
    Reports
    18
    Reporting signal score
    104.379
  • Event
    device embolisation
    Reports
    4
    Reporting signal score
    15.8812
  • Event
    diarrhoea
    Reports
    3
    Reporting signal score
    51.0923
  • Event
    dizziness
    Reports
    3
    Reporting signal score
    35.7149
  • Event
    drug hypersensitivity
    Reports
    5
    Reporting signal score
    16.2231
  • Event
    drug interaction
    Reports
    7
    Reporting signal score
    8.61224

And 60 more, listed on the interactive page.

Dose
25 mcg/kg
Route
Intravenous
How often
Up to 18 hours

  • Administer within 5 minutes
  • Use premixed bag for bolus and infusion

Hydrogen bond acceptors
5
Hydrogen bond donors
3
Polar surface area
104.73
Calculated partition coefficient (ALogP)
2.95
Calculated partition coefficient (XLogP)
1.4
Prodrug
No
Chirality
Single enantiomer
Inorganic
No
Rule-of-five violations
0
Rotatable bonds
14
Heavy atoms
30
Molecular formula
C22H36N2O5S
Monoisotopic mass
440.23449343
Natural product
Yes

Recorded assays
316
Active assays
81

Active assay types

  • Confirmatory

Related records

Trials (55)

Approved for (1)

In development for (13)

Targets (2)