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

Stem definition	Drug id	CAS RN
blood coagulation factor XA inhibitors, antithrombotics	4182	366789-02-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: xarelto rivaroxaban BAY 59-7939	A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME. Molecular weight: 435.88 Formula: C19H18ClN3O5S CLOGP: 2.39 LIPINSKI: 0 HAC: 8 HDO: 1 TPSA: 88.18 ALOGS: -4.64 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

xarelto
rivaroxaban
BAY 59-7939

A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME.

Molecular weight: 435.88
Formula: C19H18ClN3O5S
CLOGP: 2.39
LIPINSKI: 0
HAC: 8
HDO: 1
TPSA: 88.18
ALOGS: -4.64
ROTB: 5

Status: ONP

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

Drug dosage:

Dose	Unit	Route
20	mg	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	7 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
Vd (Volume of distribution)	0.70 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.06 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.01 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

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Date	Agency	Company
Jan. 18, 2012	PMDA	Bayer Yakuhin, Ltd.
July 1, 2011	FDA	JANSSEN PHARMS
Sept. 30, 2008	EMA	BAYER PHARMA AG

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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
Gastrointestinal haemorrhage	6000.42	10.90	3039	126521	78137	63281325
Pulmonary embolism	2189.00	10.90	1849	127711	114835	63244627
Ischaemic stroke	1350.27	10.90	682	128878	17275	63342187
Haemorrhage	1290.88	10.90	1038	128522	59984	63299478
Cerebral haemorrhage	1185.69	10.90	754	128806	29975	63329487
Cerebrovascular accident	1164.61	10.90	1262	128298	106762	63252700
Deep vein thrombosis	1105.06	10.90	1091	128469	82709	63276753
Epistaxis	1068.59	10.90	1005	128555	71720	63287742
Upper gastrointestinal haemorrhage	865.60	10.90	517	129043	18335	63341127
Haemorrhage intracranial	846.18	10.90	453	129107	12966	63346496

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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
Gastrointestinal haemorrhage	4780.99	11.50	3268	118985	85209	34749469
Haemorrhage	1513.60	11.50	1328	120925	50042	34784636
Haematuria	1402.64	11.50	1258	120995	48808	34785870
Epistaxis	1160.83	11.50	1214	121039	57037	34777641
Cerebral haemorrhage	1144.02	11.50	960	121293	33977	34800701
Pulmonary embolism	1031.71	11.50	1413	120840	88333	34746345
Haemorrhage intracranial	991.19	11.50	645	121608	15301	34819377
Ischaemic stroke	935.42	11.50	655	121598	17595	34817083
Cerebrovascular accident	887.81	11.50	1277	120976	83534	34751144
Upper gastrointestinal haemorrhage	851.22	11.50	709	121544	24809	34809869

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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
Gastrointestinal haemorrhage	9022.53	10.48	5334	207072	142385	79389597
Cerebral haemorrhage	2121.87	10.48	1520	210886	56153	79475829
Pulmonary embolism	2003.97	10.48	2375	210031	169279	79362703
Ischaemic stroke	1950.19	10.48	1172	211234	31959	79500023
Haematuria	1925.03	10.48	1540	210866	67296	79464686
Haemorrhage	1860.77	10.48	1702	210704	89416	79442566
Epistaxis	1725.58	10.48	1789	210617	109726	79422256
Upper gastrointestinal haemorrhage	1673.69	10.48	1156	211250	40224	79491758
Haemorrhage intracranial	1396.57	10.48	870	211536	25323	79506659
Cerebral infarction	1278.80	10.48	1023	211383	44653	79487329

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	B01AF01	BLOOD AND BLOOD FORMING ORGANS ANTITHROMBOTIC AGENTS ANTITHROMBOTIC AGENTS Direct factor Xa inhibitors
CHEBI has role	CHEBI:50249	anticoagulants
CHEBI has role	CHEBI:68581	factor Xa inhibitors
FDA EPC	N0000175637	Factor Xa Inhibitor
FDA MoA	N0000175635	Factor Xa Inhibitors
MeSH PA	D000925	Anticoagulants
MeSH PA	D000991	Antithrombins
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D065427	Factor Xa Inhibitors
MeSH PA	D006401	Hematologic Agents

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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
Nonvalvular atrial fibrillation	indication	49436004	DOID:0060224
Pulmonary embolism	indication	59282003	DOID:9477
Prevention of pulmonary embolism	indication	59282003	DOID:9477
Deep venous thrombosis	indication	128053003
Stroke prevention	indication	135875009
Prevention of stroke caused by a clot in a blood vessel in the brain	indication	135875009
Prevention of atherothrombotic events after an acute coronary syndrome	indication	394659003
Prevention of systemic embolism caused by a clot in a blood vessel	indication	414086009
Venous thromboembolic disease	indication	429098002
Prevention of venous thromboembolism from re-occuring	indication	429098002

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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	10.89	acidic

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
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	7157456	Aug. 28, 2024	TREATMENT OF DEEP VEIN THROMBOSIS (DVT)
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	7157456	Aug. 28, 2024	TREATMENT OF PULMONARY EMBOLISM (PE)
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	9415053	Nov. 13, 2024	PROPHYLAXIS OF DEEP VEIN THROMBOSIS (DVT)
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	9415053	Nov. 13, 2024	PROPHYLAXIS OF THROMBOEMBOLIC DISEASES IN PEDIATRIC PATIENTS AGED 2 YEARS AND OLDER WITH CONGENITAL HEART DISEASE WHO HAVE UNDERGONE THE FONTAN PROCEDURE AND A BODY WEIGHT OF >=50 KG
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	9415053	Nov. 13, 2024	PROPHYLAXIS OF VENOUS THROMBOEMBOLISM IN ACUTELY ILL MEDICAL PATIENTS AT RISK FOR THROMBOEMBOLIC COMPLICATIONS NOT AT HIGH RISK OF BLEEDING
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	9415053	Nov. 13, 2024	REDUCTION IN THE RISK OF RECURRENCE OF DEEP VEIN THROMBOSIS (DVT) AND/OR PULMONARY EMBOLISM (PE) IN PATIENTS AT CONTINUED RISK FOR RECURRENT DVT AND/OR AFTER COMPLETION OF INITIAL TREATMENT LASTING AT LEAST 6 MONTHS
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	9539218	Feb. 17, 2034	AFTER COMPLETION OF INITIAL TREATMENT LASTING AT LEAST 6 MONTHS, TO REDUCE THE RISK OF RECURRENCE OF DEEP VEIN THROMBOSIS AND/OR PULMONARY EMBOLISM IN CERTAIN PATIENTS WITH ONCE DAILY, RAPID-RELEASE TABLET ADMINISTERED FOR AT LEAST 5 CONSECUTIVE DAYS
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	9539218	Feb. 17, 2034	PROPHYLAXIS OF DEEP VEIN THROMBOSIS, WHICH MAY LEAD TO PULMONARY EMBOLISM IN PATIENTS UNDERGOING KNEE OR HIP REPLACEMENT SURGERY, WITH ONCE DAILY, RAPID-RELEASE TABLET ADMINISTERED FOR AT LEAST FIVE CONSECUTIVE DAYS
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	9539218	Feb. 17, 2034	PROPHYLAXIS OF PE, DVT AND/OR STROKE IN PEDIATRIC PATIENTS (>=50 KG) AGED 2 YEARS AND OLDER WITH CONGENITAL HEART DISEASE AFTER FONTAN PROCEDURE WITH ONCE DAILY, RAPID-RELEASE TABLET ADMINISTERED FOR AT LEAST 5 CONSECUTIVE DAYS
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	9539218	Feb. 17, 2034	PROPHYLAXIS OF VENOUS THROMBOEMBOLISM IN ACUTELY ILL MEDICAL PATIENTS AT RISK FOR THROMBOEMBOLIC COMPLICATIONS NOT AT HIGH RISK OF BLEEDING WITH ONCE DAILY, RAPID-RELEASE TABLET ADMINISTERED FOR AT LEAST 5 CONSECUTIVE DAYS

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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
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	March 10, 2023	REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM GALILEO TRIAL
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	April 11, 2023	PEDIATRIC EXCLUSIVITY
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	Sept. 10, 2023	PEDIATRIC EXCLUSIVITY
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	Aug. 23, 2024	INDICATED TO REDUCE THE RISK OF MAJOR THROMBOTIC VASCULAR EVENTS (MYOCARDIAL INFARCTION, ISCHEMIC STROKE, ACUTE LIMB ISCHEMIA, AND MAJOR AMPUTATION OF VASCULAR ETIOLOGY) IN PATIENTS WITH PAD, INCLUDING PATIENTS WHO HAVE RECENTLY UNDERGONE A LOWER EXTREMITY REVASCULARIZATION PROCEDURE DUE TO SYMPTOMATIC PAD
10MG	XARELTO	JANSSEN PHARMS	N022406	July 1, 2011	RX	TABLET	ORAL	Feb. 23, 2025	PEDIATRIC EXCLUSIVITY
15MG	XARELTO	JANSSEN PHARMS	N022406	Nov. 4, 2011	RX	TABLET	ORAL	March 10, 2023	REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM GALILEO TRIAL
15MG	XARELTO	JANSSEN PHARMS	N022406	Nov. 4, 2011	RX	TABLET	ORAL	April 11, 2023	PEDIATRIC EXCLUSIVITY
15MG	XARELTO	JANSSEN PHARMS	N022406	Nov. 4, 2011	RX	TABLET	ORAL	Sept. 10, 2023	PEDIATRIC EXCLUSIVITY
15MG	XARELTO	JANSSEN PHARMS	N022406	Nov. 4, 2011	RX	TABLET	ORAL	Aug. 23, 2024	INDICATED TO REDUCE THE RISK OF MAJOR THROMBOTIC VASCULAR EVENTS (MYOCARDIAL INFARCTION, ISCHEMIC STROKE, ACUTE LIMB ISCHEMIA, AND MAJOR AMPUTATION OF VASCULAR ETIOLOGY) IN PATIENTS WITH PAD, INCLUDING PATIENTS WHO HAVE RECENTLY UNDERGONE A LOWER EXTREMITY REVASCULARIZATION PROCEDURE DUE TO SYMPTOMATIC PAD
15MG	XARELTO	JANSSEN PHARMS	N022406	Nov. 4, 2011	RX	TABLET	ORAL	Feb. 23, 2025	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
Coagulation factor X	Enzyme	P00742	FA10_HUMAN	INHIBITOR	Ki	9.40	CHEMBL	CHEMBL
Suppressor of tumorigenicity 14 protein	Enzyme	Q9Y5Y6	ST14_HUMAN		Ki	5.47	CHEMBL
Coagulation factor X	Enzyme		FA10_RABIT		IC50	6.29	CHEMBL

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External reference:

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ID	Source
RIV	PDB_CHEM_ID
012873	NDDF
1114195	RXNORM
159029	MMSL
26019	MMSL
4030906	VANDF
442031002	SNOMEDCT_US
442539005	SNOMEDCT_US
6388	IUPHAR_LIGAND_ID
8428	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Xarelto	HUMAN PRESCRIPTION DRUG LABEL	1	50090-3625	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Xarelto	HUMAN PRESCRIPTION DRUG LABEL	1	50090-3639	TABLET, FILM COATED	20 mg	ORAL	NDA	31 sections
Xarelto	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4468	TABLET, FILM COATED	20 mg	ORAL	NDA	32 sections
Xarelto	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4469	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Xarelto	HUMAN PRESCRIPTION DRUG LABEL	1	50458-575	GRANULE, FOR SUSPENSION	155 mg	ORAL	NDA	35 sections
Xarelto	HUMAN PRESCRIPTION DRUG LABEL	1	50458-575	GRANULE, FOR SUSPENSION	155 mg	ORAL	NDA	35 sections
Xarelto	HUMAN PRESCRIPTION DRUG LABEL	1	50458-575	GRANULE, FOR SUSPENSION	155 mg	ORAL	NDA	35 sections
Xarelto	HUMAN PRESCRIPTION DRUG LABEL	1	50458-575	GRANULE, FOR SUSPENSION	155 mg	ORAL	NDA	35 sections
XARELTO	HUMAN PRESCRIPTION DRUG LABEL	1	50458-577	TABLET, FILM COATED	2.50 mg	ORAL	NDA	35 sections
XARELTO	HUMAN PRESCRIPTION DRUG LABEL	1	50458-577	TABLET, FILM COATED	2.50 mg	ORAL	NDA	35 sections

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