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

Stem definition	Drug id	CAS RN
platelet aggregation inhibitors	4113	150322-43-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: prasugrel prasugrel hydrochloride effient efient prasugrel HCl CS-747 LY640315	A piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS. Molecular weight: 373.44 Formula: C20H20FNO3S CLOGP: 3.46 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 46.61 ALOGS: -5.20 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

prasugrel
prasugrel hydrochloride
effient
efient
prasugrel HCl
CS-747
LY640315

A piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.

Molecular weight: 373.44
Formula: C20H20FNO3S
CLOGP: 3.46
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 46.61
ALOGS: -5.20
ROTB: 6

Status: OFP

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

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

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Date	Agency	Company
Feb. 24, 2009	EMA	DAIICHI SANKYO EUROPE GMBH
July 10, 2009	FDA	ELI LILLY AND CO
March 24, 2014	PMDA	DAIICHI SANKYO COMPANY, LIMITED

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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
Myocardial infarction	163.20	20.90	94	4101	99799	63385028
Thrombosis in device	136.23	20.90	33	4162	2957	63481870
Acute myocardial infarction	113.55	20.90	51	4144	32073	63452754
Vascular pseudoaneurysm	107.38	20.90	24	4171	1510	63483317
Vascular stent stenosis	93.67	20.90	18	4177	535	63484292
Gastrointestinal haemorrhage	81.03	20.90	56	4139	81120	63403707
Coronary artery restenosis	68.15	20.90	13	4182	371	63484456
Haemorrhage	62.99	20.90	43	4152	60979	63423848
Coronary artery occlusion	60.11	20.90	22	4173	8169	63476658
Angina pectoris	59.02	20.90	32	4163	30046	63454781

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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
Thrombosis in device	349.29	17.74	91	7592	3234	34946014
Vascular stent thrombosis	292.26	17.74	77	7606	2858	34946390
Vascular stent stenosis	202.97	17.74	48	7635	1133	34948115
Acute myocardial infarction	173.17	17.74	121	7562	53598	34895650
Myocardial infarction	154.79	17.74	160	7523	120925	34828323
Chest pain	116.34	17.74	141	7542	126621	34822627
Angina pectoris	108.83	17.74	74	7609	31289	34917959
Coronary artery restenosis	83.46	17.74	23	7660	1011	34948237
Haemorrhage	72.93	17.74	72	7611	51298	34897950
Angina unstable	72.59	17.74	40	7643	11613	34937635

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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	328.52	16.09	79	9782	3631	79730896
Thrombosis in device	270.06	16.09	73	9788	5369	79729158
Acute myocardial infarction	238.59	16.09	137	9724	76899	79657628
Myocardial infarction	233.04	16.09	188	9673	183941	79550586
Gastrointestinal haemorrhage	124.68	16.09	120	9741	147599	79586928
Vascular stent stenosis	122.28	16.09	30	9831	1497	79733030
Vascular pseudoaneurysm	114.77	16.09	34	9827	3476	79731051
Haemorrhage	106.51	16.09	89	9772	91029	79643498
Coronary artery stenosis	95.08	16.09	41	9820	12443	79722084
Chest pain	94.15	16.09	143	9718	282161	79452366

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	B01AC22	BLOOD AND BLOOD FORMING ORGANS ANTITHROMBOTIC AGENTS ANTITHROMBOTIC AGENTS Platelet aggregation inhibitors excl. heparin
CHEBI has role	CHEBI:35554	cardiovascular agent
CHEBI has role	CHEBI:50433	platelet glycoprotein-IIb/IIIa receptor antagonists
CHEBI has role	CHEBI:68563	ADP receptor subtype P2Y12 antagonists
CHEBI has role	CHEBI:50266	Prodrugs
FDA EPC	N0000182142	P2Y12 Platelet Inhibitor
FDA MoA	N0000182143	P2Y12 Receptor Antagonists
FDA PE	N0000008832	Decreased Platelet Aggregation
MeSH PA	D006401	Hematologic Agents
MeSH PA	D010975	Platelet Aggregation Inhibitors

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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
Prevention of recurrence of ischemic cerebrovascular disease	indication	62914000	DOID:6713
Acute coronary syndrome	indication	394659003
Percutaneous coronary intervention	indication	415070008
Myocardial Reinfarction Prevention	indication
Intracranial hemorrhage	contraindication	1386000
Acute hemorrhage	contraindication	8573003
Acute peptic ulcer with hemorrhage	contraindication	12274003
Low blood pressure	contraindication	45007003
Hepatic failure	contraindication	59927004
Blood coagulation disorder	contraindication	64779008	DOID:1247

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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	5.53	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
P2Y purinoceptor 12	GPCR	Q9H244	P2Y12_HUMAN	ANTAGONIST				UNKNOWN	CHEMBL

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External reference:

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ID	Source
012994	NDDF
012995	NDDF
166281	MMSL
261080	MMSL
26287	MMSL
34K66TBT99	UNII
389574-19-0	SECONDARY_CAS_RN
39620	MMSL
4029056	VUID
4029056	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Effient	HUMAN PRESCRIPTION DRUG LABEL	1	0002-5121	TABLET, FILM COATED	5 mg	ORAL	NDA	32 sections
Effient	HUMAN PRESCRIPTION DRUG LABEL	1	0002-5123	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Effient	HUMAN PRESCRIPTION DRUG LABEL	1	0713-0881	TABLET, COATED	5 mg	ORAL	NDA	33 sections
Effient	HUMAN PRESCRIPTION DRUG LABEL	1	0713-0882	TABLET, COATED	10 mg	ORAL	NDA	33 sections
Effient	HUMAN PRESCRIPTION DRUG LABEL	1	54868-6238	TABLET, FILM COATED	10 mg	ORAL	NDA	28 sections
Prasugrel	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5185	TABLET, FILM COATED	5 mg	ORAL	ANDA	29 sections
Prasugrel	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5185	TABLET, FILM COATED	5 mg	ORAL	ANDA	29 sections
Prasugrel	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5186	TABLET, FILM COATED	10 mg	ORAL	ANDA	29 sections
Prasugrel	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5186	TABLET, FILM COATED	10 mg	ORAL	ANDA	29 sections
PRASUGREL	HUMAN PRESCRIPTION DRUG LABEL	1	0440-0604	TABLET, FILM COATED	5 mg	ORAL	ANDA	29 sections

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