ticagrelor 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
platelet aggregation inhibitors	4184	274693-27-5

Description:

Molecule	Description
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: 3.35 LIPINSKI: 1 HAC: 10 HDO: 4 TPSA: 138.44 ALOGS: -3.92 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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: 3.35
LIPINSKI: 1
HAC: 10
HDO: 4
TPSA: 138.44
ALOGS: -3.92
ROTB: 10

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.18	g	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	6.80 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	3.38 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution)	1.25 L/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.01 mg/mL	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
July 20, 2011	FDA	ASTRAZENECA LP

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Vascular stent thrombosis	686.68	18.07	126	12901	851	63475144
Rhabdomyolysis	588.48	18.07	249	12778	43702	63432293
Myocardial infarction	343.43	18.07	228	12799	99665	63376330
Thrombosis in device	286.28	18.07	75	12952	2915	63473080
Drug interaction	281.44	18.07	287	12740	228844	63247151
Dyspnoea	269.35	18.07	482	12545	660831	62815164
Acute myocardial infarction	261.82	18.07	129	12898	31995	63444000
Gastrointestinal haemorrhage	179.58	18.07	142	12885	81034	63394961
Acute kidney injury	171.67	18.07	239	12788	263176	63212819
Haemorrhage	129.01	18.07	104	12923	60918	63415077

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Vascular stent thrombosis	1503.75	15.94	361	24512	2574	34929484
Thrombosis in device	721.83	15.94	207	24666	3118	34928940
Dyspnoea	460.06	15.94	895	23978	375887	34556171
Acute myocardial infarction	440.94	15.94	339	24534	53380	34878678
Myocardial infarction	333.74	15.94	420	24453	120665	34811393
Chest pain	241.21	15.94	368	24505	126394	34805664
Rhabdomyolysis	232.76	15.94	264	24609	67899	34864159
Angina pectoris	227.02	15.94	184	24689	31179	34900879
Chest discomfort	213.52	15.94	227	24646	54303	34877755
Gastrointestinal haemorrhage	210.85	15.94	286	24587	88191	34843867

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Vascular stent thrombosis	1679.83	14.54	375	33575	3335	79707103
Rhabdomyolysis	717.16	14.54	481	33469	102650	79607788
Acute myocardial infarction	663.03	14.54	411	33539	76625	79633813
Thrombosis in device	623.75	14.54	184	33766	5258	79705180
Myocardial infarction	550.91	14.54	523	33427	183606	79526832
Dyspnoea	497.03	14.54	1109	32841	855916	78854522
Drug interaction	448.42	14.54	703	33247	414480	79295958
Gastrointestinal haemorrhage	327.05	14.54	357	33593	147362	79563076
Chest pain	299.83	14.54	475	33475	281829	79428609
Angina pectoris	292.89	14.54	213	33737	51519	79658919

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	B01AC24	BLOOD AND BLOOD FORMING ORGANS ANTITHROMBOTIC AGENTS ANTITHROMBOTIC AGENTS Platelet aggregation inhibitors excl. heparin
CHEBI has role	CHEBI:50427	platelet aggregation inhibitors
CHEBI has role	CHEBI:68563	ADP receptor subtype P2Y12 antagonists
FDA EPC	N0000182142	P2Y12 Platelet Inhibitor
FDA MoA	N0000182141	Cytochrome P450 3A4 Inhibitors
FDA MoA	N0000182143	P2Y12 Receptor Antagonists
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000190115	Cytochrome P450 3A5 Inhibitors
FDA MoA	N0000190482	Phenylalanine Hydroxylase Activators
FDA PE	N0000008832	Decreased Platelet Aggregation

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.07	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
60MG	BRILINTA	ASTRAZENECA	N022433	Sept. 3, 2015	RX	TABLET	ORAL	RE46276	Oct. 30, 2024	REDUCTION OF THE RATE OF A FIRST MYOCARDIAL INFARCTION OR STROKE IN PATIENTS WITH CORONARY ARTERY DISEASE AT HIGH RISK FOR SUCH EVENTS
60MG	BRILINTA	ASTRAZENECA	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	N022433	Sept. 3, 2015	RX	TABLET	ORAL	RE46276	Oct. 30, 2024	REDUCTION OF THE RISK OF STROKE IN PATIENTS WITH ACUTE ISCHEMIC STROKE OR HIGH-RISK TRANSIENT ISCHEMIC ATTACK
60MG	BRILINTA	ASTRAZENECA	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	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	N022433	Sept. 3, 2015	RX	TABLET	ORAL	RE46276	Oct. 30, 2024	TREATMENT OF MYOCARDIAL INFARCTION OR STROKE IN PATIENTS WITH CORONARY ARTERY DISEASE AT HIGH RISK FOR SUCH EVENTS
60MG	BRILINTA	ASTRAZENECA	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
60MG	BRILINTA	ASTRAZENECA	N022433	Sept. 3, 2015	RX	TABLET	ORAL	10300065	Jan. 27, 2036	REDUCING THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE IN A PATIENT RECEIVING 75-100 MG ASPIRIN DAILY AND HAVING OR WHO HAD ACUTE CORONARY SYNDROME BY ADMINISTERING 60 MG TICAGRELOR TWICE DAILY
60MG	BRILINTA	ASTRAZENECA	N022433	Sept. 3, 2015	RX	TABLET	ORAL	10300065	Jan. 27, 2036	REDUCING THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION (MI), AND STROKE IN A PATIENT RECEIVING 75-100 MG ASPIRIN DAILY WITH A HISTORY OF MI BY ADMINISTERING 60 MG TICAGRELOR TWICE DAILY
90MG	BRILINTA	ASTRAZENECA	N022433	July 20, 2011	RX	TABLET	ORAL	RE46276	Oct. 30, 2024	REDUCTION OF THE RATE OF A FIRST MYOCARDIAL INFARCTION OR STROKE IN PATIENTS WITH CORONARY ARTERY DISEASE AT HIGH RISK FOR SUCH EVENTS

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
60MG	BRILINTA	ASTRAZENECA	N022433	Sept. 3, 2015	RX	TABLET	ORAL	May 28, 2023	TO REDUCE THE RISK OF A FIRST MYOCARDIAL INFARCTION (MI) OR STROKE IN PATIENTS WITH CORONARY ARTERY DISEASE (CAD) AT HIGH RISK FOR SUCH EVENTS
60MG	BRILINTA	ASTRAZENECA	N022433	Sept. 3, 2015	RX	TABLET	ORAL	Nov. 5, 2023	REDUCE THE RISK OF STROKE IN PATIENTS WITH ACUTE ISCHEMIC STROKE (NIH STROKE SCALE SCORE <=5) OR HIGH-RISK TRANSIENT ISCHEMIC ATTACK (TIA)
60MG	BRILINTA	ASTRAZENECA	N022433	Sept. 3, 2015	RX	TABLET	ORAL	Nov. 28, 2023	PEDIATRIC EXCLUSIVITY
60MG	BRILINTA	ASTRAZENECA	N022433	Sept. 3, 2015	RX	TABLET	ORAL	May 5, 2024	PEDIATRIC EXCLUSIVITY
60MG	BRILINTA	ASTRAZENECA	N022433	Sept. 3, 2015	RX	TABLET	ORAL	May 9, 2025	INFORMATION ADDED TO SECTION 8.4 OF THE LABELING TO INCLUDE THE RESULT OF STUDY HESTIA3
60MG	BRILINTA	ASTRAZENECA	N022433	Sept. 3, 2015	RX	TABLET	ORAL	Nov. 9, 2025	PEDIATRIC EXCLUSIVITY
90MG	BRILINTA	ASTRAZENECA	N022433	July 20, 2011	RX	TABLET	ORAL	May 28, 2023	TO REDUCE THE RISK OF A FIRST MYOCARDIAL INFARCTION (MI) OR STROKE IN PATIENTS WITH CORONARY ARTERY DISEASE (CAD) AT HIGH RISK FOR SUCH EVENTS
90MG	BRILINTA	ASTRAZENECA	N022433	July 20, 2011	RX	TABLET	ORAL	Nov. 5, 2023	REDUCE THE RISK OF STROKE IN PATIENTS WITH ACUTE ISCHEMIC STROKE (NIH STROKE SCALE SCORE <=5) OR HIGH-RISK TRANSIENT ISCHEMIC ATTACK (TIA)
90MG	BRILINTA	ASTRAZENECA	N022433	July 20, 2011	RX	TABLET	ORAL	Nov. 28, 2023	PEDIATRIC EXCLUSIVITY
90MG	BRILINTA	ASTRAZENECA	N022433	July 20, 2011	RX	TABLET	ORAL	May 5, 2024	PEDIATRIC EXCLUSIVITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
P2Y purinoceptor 12	GPCR	Q9H244	P2Y12_HUMAN	NEGATIVE ALLOSTERIC MODULATOR	Ki	7.85	CHEMBL	CHEMBL
Equilibrative nucleoside transporter 1	Transporter	Q99808	S29A1_HUMAN	INHIBITOR	Ki	7.30	IUPHAR
P2Y purinoceptor 12	GPCR		P2Y12_RAT		IC50	5.38	CHEMBL

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External reference:

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ID	Source
TIQ	PDB_CHEM_ID
013611	NDDF
1116632	RXNORM
1765	IUPHAR_LIGAND_ID
182026	MMSL
235692	MMSL
27677	MMSL
4030908	VUID
4030908	VANDF
698805004	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
BRILINTA	HUMAN PRESCRIPTION DRUG LABEL	1	0186-0776	TABLET	60 mg	ORAL	NDA	31 sections
BRILINTA	HUMAN PRESCRIPTION DRUG LABEL	1	0186-0776	TABLET	60 mg	ORAL	NDA	31 sections
BRILINTA	HUMAN PRESCRIPTION DRUG LABEL	1	0186-0777	TABLET	90 mg	ORAL	NDA	31 sections
BRILINTA	HUMAN PRESCRIPTION DRUG LABEL	1	0186-0777	TABLET	90 mg	ORAL	NDA	31 sections
BRILINTA	HUMAN PRESCRIPTION DRUG LABEL	1	55154-9618	TABLET	90 mg	ORAL	NDA	31 sections
BRILINTA	HUMAN PRESCRIPTION DRUG LABEL	1	55154-9618	TABLET	90 mg	ORAL	NDA	31 sections
BRILINTA	HUMAN PRESCRIPTION DRUG LABEL	1	55154-9618	TABLET	90 mg	ORAL	NDA	31 sections
ticagrelor	HUMAN PRESCRIPTION DRUG LABEL	1	69238-1134	TABLET	90 mg	ORAL	ANDA	28 sections
ticagrelor	HUMAN PRESCRIPTION DRUG LABEL	1	69238-1134	TABLET	90 mg	ORAL	ANDA	28 sections

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