ticagrelor indications/contra

Stem definitionDrug idCAS RN
platelet aggregation inhibitors 4184 274693-27-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ticagrelor
  • brilinta
  • AZD 6140
  • possia
  • brilique
a cyclopentyltriazolopyrimidine, inhibitor of platelet activation and aggregation mediated by the P2Y12 ADP-receptor indicated to reduce the rate of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome or a history of myocardial infarction
  • Molecular weight: 522.57
  • Formula: C23H28F2N6O4S
  • CLOGP: 2.55
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 4
  • TPSA: 138.44
  • ALOGS: -3.92
  • ROTB: 10

Drug dosage:

DoseUnitRoute
0.18 g O

Approvals:

DateAgencyCompanyOrphan
July 20, 2011 FDA ASTRAZENECA LP

FDA Adverse Event Reporting System

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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
Thrombosis in device 2046.72 46.45 359 5534 1399 3378567
Dyspnoea 1660.39 46.45 702 5191 102232 3277734
Vascular stent thrombosis 1290.75 46.45 201 5692 271 3379695
Gastrointestinal haemorrhage 748.47 46.45 268 5625 24106 3355860
Acute myocardial infarction 740.96 46.45 225 5668 12026 3367940
Myocardial infarction 460.56 46.45 225 5668 43908 3336058
Cerebral haemorrhage 428.69 46.45 141 5752 9713 3370253
Haemorrhage 417.39 46.45 166 5727 19755 3360211
Anaemia 369.29 46.45 208 5685 54125 3325841
Haemorrhage intracranial 351.81 46.45 105 5788 5234 3374732
Chest pain 345.36 46.45 180 5713 40095 3339871
Intentional product misuse 330.45 46.45 124 5769 12577 3367389
Melaena 287.36 46.45 97 5796 7215 3372751
Bradycardia 280.97 46.45 119 5774 16550 3363416
Drug dose omission 273.85 46.45 152 5741 38280 3341686
Epistaxis 239.57 46.45 102 5791 14349 3365617
Haemoglobin decreased 227.13 46.45 124 5769 30170 3349796
Angina unstable 220.81 46.45 66 5827 3296 3376670
Atrioventricular block complete 218.83 46.45 61 5832 2371 3377595
Device occlusion 216.86 46.45 55 5838 1476 3378490
Angina pectoris 213.85 46.45 79 5814 7642 3372324
Drug interaction 193.97 46.45 131 5762 46681 3333285
Coronary artery restenosis 189.01 46.45 38 5855 337 3379629
Cardiac arrest 188.71 46.45 106 5787 27213 3352753
Subdural haematoma 181.09 46.45 61 5832 4494 3375472
Rectal haemorrhage 174.93 46.45 72 5821 9286 3370680
Death 167.78 46.45 201 5692 152123 3227843
Acute coronary syndrome 166.27 46.45 53 5840 3279 3376687
Sinus arrest 162.15 46.45 36 5857 533 3379433
Off label use 161.53 46.45 124 5769 53853 3326113

Pharmacologic Action:

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SourceCodeDescription
ATC B01AC24 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Platelet aggregation inhibitors excl. heparin
FDA EPC N0000182142 P2Y12 Platelet Inhibitor
FDA MoA N0000190482 Phenylalanine Hydroxylase Activators
FDA PE N0000008832 Decreased Platelet Aggregation
FDA MoA N0000182143 P2Y12 Receptor Antagonists
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000190115 Cytochrome P450 3A5 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D058905 Purinergic Agents
MeSH PA D058914 Purinergic Antagonists
MeSH PA D058919 Purinergic P2 Receptor Antagonists
MeSH PA D058921 Purinergic P2Y Receptor Antagonists
CHEBI has role CHEBI:50427 platelet aggregation inhibitor

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Acute coronary syndrome indication 394659003
Peripheral vascular disease indication 400047006
Percutaneous coronary intervention indication 415070008
Myocardial Reinfarction Prevention indication
Intracranial hemorrhage contraindication 1386000
Hepatic failure contraindication 59927004
Disease of liver contraindication 235856003 DOID:409
Surgical procedure contraindication 387713003
Significant Bleeding contraindication

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.07 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 6525060 Dec. 2, 2019 REDUCTION OF THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 6525060 Dec. 2, 2019 REDUCTION OF THE RATE OF THROMBOTIC EVENTS IN PATIENTS WITH ACUTE CORONARY SYNDROME
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 6525060 Dec. 2, 2019 TREATMENT OF POST-MYOCARDIAL INFARCTION
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 6525060 Dec. 2, 2019 TREATMENT OF STROKE
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 7250419 Dec. 2, 2019 METHOD OF INHIBITING PLATELET AGGREGATION
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 7250419 Dec. 2, 2019 REDUCTION OF THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 7250419 Dec. 2, 2019 REDUCTION OF THE RATE OF THROMBOTIC EVENTS IN PATIENTS WITH ACUTE CORONARY SYNDROME
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 7250419 Dec. 2, 2019 TREATMENT OF MYOCARDIAL INFARCTION
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 7250419 Dec. 2, 2019 TREATMENT OF STABLE AND UNSTABLE ANGINA
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 7250419 Dec. 2, 2019 TREATMENT OF THROMBOTIC STROKE
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 6525060 Dec. 2, 2019 REDUCTION OF THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 6525060 Dec. 2, 2019 REDUCTION OF THE RATE OF THROMBOTIC EVENTS IN PATIENTS WITH ACUTE CORONARY SYNDROME
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 6525060 Dec. 2, 2019 TREATMENT OF POST-MYOCARDIAL INFARCTION
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 6525060 Dec. 2, 2019 TREATMENT OF STROKE
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 7250419 Dec. 2, 2019 METHOD OF INHIBITING PLATELET AGGREGATION
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 7250419 Dec. 2, 2019 REDUCTION OF THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 7250419 Dec. 2, 2019 REDUCTION OF THE RATE OF THROMBOTIC EVENTS IN PATIENTS WITH ACUTE CORONARY SYNDROME
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 7250419 Dec. 2, 2019 TREATMENT OF MYOCARDIAL INFARCTION
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 7250419 Dec. 2, 2019 TREATMENT OF STABLE AND UNSTABLE ANGINA
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 7250419 Dec. 2, 2019 TREATMENT OF THROMBOTIC STROKE
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 7265124 July 9, 2021 REDUCTION OF THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 7265124 July 9, 2021 REDUCTION OF THE RATE OF THROMBOTIC EVENTS IN PATIENTS WITH ACUTE CORONARY SYNDROME
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 7265124 July 9, 2021 TREATMENT OF AN ARTERIAL THROMBOTIC COMPLICATION IN A PATIENT WITH CORONARY ARTERY, CEREBROVASCULAR OR PERIPHERAL VASCULAR DISEASE
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL 7265124 July 9, 2021 TREATMENT OF ARTERIAL THROMBOTIC COMPLICATIONS SELECTED FROM THE GROUP CONSISTING OF UNSTABLE ANGINA, THROMBOTIC OR EMBOLIC STROKE, TRANSIENT ISCHAEMIC ATTACKS, PERIPHERAL VASCULAR DISEASE AND MYOCARDIAL INFARCTION
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 7265124 July 9, 2021 REDUCTION OF THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 7265124 July 9, 2021 REDUCTION OF THE RATE OF THROMBOTIC EVENTS IN PATIENTS WITH ACUTE CORONARY SYNDROME
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 7265124 July 9, 2021 TREATMENT OF AN ARTERIAL THROMBOTIC COMPLICATION IN A PATIENT WITH CORONARY ARTERY, CEREBROVASCULAR OR PERIPHERAL VASCULAR DISEASE
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL 7265124 July 9, 2021 TREATMENT OF ARTERIAL THROMBOTIC COMPLICATIONS SELECTED FROM THE GROUP CONSISTING OF UNSTABLE ANGINA, THROMBOTIC OR EMBOLIC STROKE, TRANSIENT ISCHAEMIC ATTACKS, PERIPHERAL VASCULAR DISEASE AND MYOCARDIAL INFARCTION
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL RE46276 Oct. 30, 2024 REDUCTION OF THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE IN PATIENTS WITH A HISTORY OF MYOCARDIAL INFARCTION
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL RE46276 Oct. 30, 2024 TREATMENT OF MYOCARDIAL INFARCTION AND STROKE IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL RE46276 Oct. 30, 2024 TREATMENT OF MYOCARDIAL INFARCTION IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL RE46276 Oct. 30, 2024 TREATMENT OF STROKE IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL RE46276 Oct. 30, 2024 REDUCTION OF THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE IN PATIENTS WITH A HISTORY OF MYOCARDIAL INFARCTION
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL RE46276 Oct. 30, 2024 TREATMENT OF MYOCARDIAL INFARCTION AND STROKE IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL RE46276 Oct. 30, 2024 TREATMENT OF MYOCARDIAL INFARCTION IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL RE46276 Oct. 30, 2024 TREATMENT OF STROKE IN PATIENTS WITH ACUTE CORONARY SYNDROME OR A HISTORY OF MYOCARDIAL INFARCTION

Orange Book exclusivity data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
60MG BRILINTA ASTRAZENECA PHARMS N022433 Sept. 3, 2015 RX TABLET ORAL Sept. 3, 2018 NEW STRENGTH
90MG BRILINTA ASTRAZENECA PHARMS N022433 July 20, 2011 RX TABLET ORAL Sept. 3, 2018 EXTENDS THE 2011 APPROVAL OF BRILINTA FOR USE BEGINNING WITH ACS TO USE BEGINNING MORE REMOTE FROM MYOCARDIAL INFRACTION

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
P2Y purinoceptor 12 GPCR NEGATIVE ALLOSTERIC MODULATOR Ki 7.85 CHEMBL CHEMBL
Equilibrative nucleoside transporter 1 Transporter INHIBITOR Ki 7.30 IUPHAR
P2Y purinoceptor 12 Unclassified IC50 5.38 CHEMBL

External reference:

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IDSource
1765 IUPHAR_LIGAND_ID
4030908 VUID
N0000182973 NUI
C1999375 UMLSCUI
D09017 KEGG_DRUG
013611 NDDF
CHEMBL398435 ChEMBL_ID
C503700 MESH_SUPPLEMENTAL_RECORD_UI
DB08816 DRUGBANK_ID
1116632 RXNORM
4030908 VANDF
27677 MMSL
d07721 MMSL
N0000182973 NDFRT
698805004 SNOMEDCT_US
704464003 SNOMEDCT_US
9871419 PUBCHEM_CID
GLH0314RVC UNII
8772 INN_ID
CHEBI:68558 CHEBI
TIQ PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
BRILINTA HUMAN PRESCRIPTION DRUG LABEL 1 0186-0776 TABLET 60 mg ORAL NDA 19 sections
BRILINTA HUMAN PRESCRIPTION DRUG LABEL 1 0186-0777 TABLET 90 mg ORAL NDA 19 sections
BRILINTA HUMAN PRESCRIPTION DRUG LABEL 1 55154-9618 TABLET 90 mg ORAL NDA 19 sections
BRILINTA HUMAN PRESCRIPTION DRUG LABEL 1 63629-5292 TABLET 90 mg ORAL NDA 18 sections