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

Stem definition	Drug id	CAS RN
blood coagulation factor XA inhibitors, antithrombotics	4298	503612-47-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: apixaban eliquis BMS 562247 BMS-562247 BMS-562247-01	Apixaban is a selective inhibitor of FXa. It does not require antithrombin III for antithrombotic activity. Apixaban inhibits free and clot-bound FXa, and prothrombinase activity. Apixaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, apixaban decreases thrombin generation and thrombus development. Molecular weight: 459.51 Formula: C25H25N5O4 CLOGP: 1.99 LIPINSKI: 0 HAC: 9 HDO: 1 TPSA: 110.76 ALOGS: -3.83 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

apixaban
eliquis
BMS 562247
BMS-562247
BMS-562247-01

Apixaban is a selective inhibitor of FXa. It does not require antithrombin III for antithrombotic activity. Apixaban inhibits free and clot-bound FXa, and prothrombinase activity. Apixaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, apixaban decreases thrombin generation and thrombus development.

Molecular weight: 459.51
Formula: C25H25N5O4
CLOGP: 1.99
LIPINSKI: 0
HAC: 9
HDO: 1
TPSA: 110.76
ALOGS: -3.83
ROTB: 5

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
t_half (Half-life)	12 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
CL (Clearance)	0.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.30 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.13 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.04 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Dec. 28, 2012	FDA	BRISTOL MYERS SQUIBB
May 18, 2011	EMA

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
Death	1495.64	10.82	2828	137064	371553	62977577
Atrial fibrillation	1124.09	10.82	1334	138558	115302	63233828
Gastrointestinal haemorrhage	1054.56	10.82	1086	138806	80090	63269040
Drug ineffective	739.10	10.82	733	139159	1044032	62305098
Haemorrhage	700.94	10.82	765	139127	60257	63288873
Cerebral haemorrhage	698.06	10.82	563	139329	30166	63318964
Cerebrovascular accident	642.63	10.82	977	138915	107047	63242083
Haemorrhage intracranial	620.34	10.82	380	139512	13039	63336091
Fall	557.75	10.82	2013	137879	390321	62958809
Thrombosis	503.75	10.82	666	139226	64089	63285041

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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
Haemorrhage	929.94	11.56	1029	124071	50341	34781490
Gastrointestinal haemorrhage	782.44	11.56	1247	123853	87230	34744601
Atrial fibrillation	739.99	11.56	1460	123640	120933	34710898
Death	686.48	11.56	3023	122077	395026	34436805
Prescribed underdose	643.20	11.56	400	124700	8533	34823298
Cerebral haemorrhage	639.05	11.56	704	124396	34233	34797598
Gastric haemorrhage	563.99	11.56	388	124712	9873	34821958
Haemorrhage intracranial	547.32	11.56	455	124645	15491	34816340
Cerebrovascular accident	487.05	11.56	991	124109	83820	34748011
Fall	350.46	11.56	1545	123555	201340	34630491

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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
Death	1611.40	10.37	4338	220413	562176	78957461
Atrial fibrillation	1566.10	10.37	2330	222421	195556	79324081
Gastrointestinal haemorrhage	1538.76	10.37	1986	222765	145733	79373904
Cerebral haemorrhage	1276.55	10.37	1156	223595	56517	79463120
Haemorrhage	1193.37	10.37	1376	223375	89742	79429895
Haemorrhage intracranial	960.57	10.37	705	224046	25488	79494149
Prescribed underdose	894.32	10.37	709	224042	28805	79490832
Fall	782.24	10.37	3075	221676	484554	79035083
Drug ineffective	746.51	10.37	1189	223562	1079724	78439913
Cerebrovascular accident	692.26	10.37	1421	223330	153871	79365766

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	B01AF02	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
Arterial embolus and thrombosis	indication	266262004
Myocardial Reinfarction Prevention	indication

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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	12.89	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
2.5MG	ELIQUIS	BRISTOL MYERS SQUIBB	N202155	Dec. 28, 2012	RX	TABLET	ORAL	6967208	Nov. 21, 2026	PROPHYLAXIS OF DEEP VEIN THROMBOSIS AND PULMONARY EMBOLISM
2.5MG	ELIQUIS	BRISTOL MYERS SQUIBB	N202155	Dec. 28, 2012	RX	TABLET	ORAL	6967208	Nov. 21, 2026	PROPHYLAXIS OF DEEP VEIN THROMBOSIS (DVT)
2.5MG	ELIQUIS	BRISTOL MYERS SQUIBB	N202155	Dec. 28, 2012	RX	TABLET	ORAL	6967208	Nov. 21, 2026	PROPHYLAXIS OF PULMONARY EMBOLISM
2.5MG	ELIQUIS	BRISTOL MYERS SQUIBB	N202155	Dec. 28, 2012	RX	TABLET	ORAL	6967208	Nov. 21, 2026	REDUCE THE RISK OF RECURRENT DEEP VEIN THROMBOSIS (DVT)
2.5MG	ELIQUIS	BRISTOL MYERS SQUIBB	N202155	Dec. 28, 2012	RX	TABLET	ORAL	6967208	Nov. 21, 2026	REDUCE THE RISK OF RECURRENT PULMONARY EMBOLISM
2.5MG	ELIQUIS	BRISTOL MYERS SQUIBB	N202155	Dec. 28, 2012	RX	TABLET	ORAL	6967208	Nov. 21, 2026	REDUCING THE RISK OF STROKE
2.5MG	ELIQUIS	BRISTOL MYERS SQUIBB	N202155	Dec. 28, 2012	RX	TABLET	ORAL	6967208	Nov. 21, 2026	REDUCING THE RISK OF STROKE AND SYSTEMIC EMBOLISM
2.5MG	ELIQUIS	BRISTOL MYERS SQUIBB	N202155	Dec. 28, 2012	RX	TABLET	ORAL	6967208	Nov. 21, 2026	TREATMENT OF DEEP VEIN THROMBOSIS (DVT)
2.5MG	ELIQUIS	BRISTOL MYERS SQUIBB	N202155	Dec. 28, 2012	RX	TABLET	ORAL	6967208	Nov. 21, 2026	TREATMENT OF PULMONARY EMBOLISM (PE)
5MG	ELIQUIS	BRISTOL MYERS SQUIBB	N202155	Dec. 28, 2012	RX	TABLET	ORAL	6967208	Nov. 21, 2026	REDUCING THE RISK OF STROKE

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Orange Book exclusivity data (new drug applications)

None

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	10.10	CHEMBL	CHEMBL
Prothrombin	Enzyme	P00734	THRB_HUMAN		Ki	5.51	CHEMBL
Coagulation factor X	Enzyme		FA10_RABIT		Ki	9.77	CHEMBL

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External reference:

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ID	Source
013857	NDDF
10182969	PUBCHEM_CID
1364430	RXNORM
185767	MMSL
28142	MMSL
3Z9Y7UWC1J	UNII
4031957	VUID
4031957	VANDF
6390	IUPHAR_LIGAND_ID
698090000	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
apixaban	Human Prescription Drug Label	1	14445-149	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	29 sections
apixaban	Human Prescription Drug Label	1	14445-150	TABLET, FILM COATED	5 mg	ORAL	ANDA	29 sections
ELIQUIS	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0893	TABLET, FILM COATED	2.50 mg	ORAL	NDA	30 sections
ELIQUIS	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0893	TABLET, FILM COATED	2.50 mg	ORAL	NDA	30 sections
ELIQUIS	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0894	TABLET, FILM COATED	5 mg	ORAL	NDA	30 sections
ELIQUIS	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0894	TABLET, FILM COATED	5 mg	ORAL	NDA	30 sections
ELIQUIS	HUMAN PRESCRIPTION DRUG LABEL	1	50090-1436	TABLET, FILM COATED	2.50 mg	ORAL	NDA	29 sections
ELIQUIS	HUMAN PRESCRIPTION DRUG LABEL	1	50090-1437	TABLET, FILM COATED	5 mg	ORAL	NDA	29 sections
ELIQUIS	HUMAN PRESCRIPTION DRUG LABEL	1	50090-6451	TABLET, FILM COATED	2.50 mg	ORAL	NDA	30 sections
ELIQUIS	HUMAN PRESCRIPTION DRUG LABEL	1	50090-6454	TABLET, FILM COATED	5 mg	ORAL	NDA	30 sections

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