Scroll

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

Stem definition	Drug id	CAS RN
thromboxane A2-receptor antagonists; antithrombotic agents	239	74863-84-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: argatroban argatroban sodium argatroban hydrate novastan argatroban monohydrate	Molecular weight: 508.64 Formula: C23H36N6O5S CLOGP: 0.23 LIPINSKI: 3 HAC: 11 HDO: 6 TPSA: 177.71 ALOGS: -3.48 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

argatroban
argatroban sodium
argatroban hydrate
novastan
argatroban monohydrate

Molecular weight: 508.64
Formula: C23H36N6O5S
CLOGP: 0.23
LIPINSKI: 3
HAC: 11
HDO: 6
TPSA: 177.71
ALOGS: -3.48
ROTB: 8

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.20	g	P

ADMET properties:

Show entries

Search:

Property	Value	Reference
CL (Clearance)	5 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	16 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.46 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	0.40 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.17 L/kg	Lombardo F, Berellini G, Obach RS

Showing 1 to 6 of 6 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
June 30, 2000	FDA	PFIZER

FDA Adverse Event Reporting System (Female)

Show entries

Search:

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
Heparin-induced thrombocytopenia	239.36	49.81	44	953	4538	63483487
Coagulation time prolonged	193.26	49.81	31	966	1417	63486608
Activated partial thromboplastin time prolonged	133.66	49.81	29	968	6864	63481161
International normalised ratio increased	121.71	49.81	40	957	46385	63441640
Oesophageal intramural haematoma	52.06	49.81	7	990	90	63487935

Showing 1 to 5 of 5 entries

Previous1Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

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
Heparin-induced thrombocytopenia	302.07	37.04	65	1405	5530	34949931
Activated partial thromboplastin time prolonged	111.81	37.04	32	1438	8663	34946798
Coagulation time prolonged	110.13	37.04	22	1448	1280	34954181
International normalised ratio increased	85.55	37.04	41	1429	47286	34908175
Coagulopathy	54.34	37.04	23	1447	19766	34935695
Haemorrhage	54.02	37.04	31	1439	51339	34904122
Disseminated intravascular coagulation	52.18	37.04	23	1447	21793	34933668
Thrombosis	44.01	37.04	27	1443	50431	34905030
Subarachnoid haemorrhage	39.09	37.04	16	1454	12619	34942842

Showing 1 to 9 of 9 entries

Previous1Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

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
Heparin-induced thrombocytopenia	526.74	35.66	108	2446	9574	79732260
Activated partial thromboplastin time prolonged	176.44	35.66	48	2506	14180	79727654
Coagulation time prolonged	154.06	35.66	31	2523	2464	79739370
International normalised ratio increased	110.74	35.66	54	2500	84667	79657167
Coagulopathy	65.82	35.66	29	2525	35977	79705857
Thrombosis	65.52	35.66	38	2516	84062	79657772
Haemorrhage	62.69	35.66	38	2516	91080	79650754
Disseminated intravascular coagulation	59.54	35.66	27	2527	35815	79706019
Subarachnoid haemorrhage	59.02	35.66	24	2530	24441	79717393
Cerebral haemorrhage	52.85	35.66	29	2525	57644	79684190

Showing 1 to 10 of 18 entries

Previous1 2Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	B01AE03	BLOOD AND BLOOD FORMING ORGANS ANTITHROMBOTIC AGENTS ANTITHROMBOTIC AGENTS Direct thrombin inhibitors
FDA EPC	N0000175518	Direct Thrombin Inhibitor
FDA EPC	N0000175980	Anti-coagulant
FDA MoA	N0000009963	Thrombin Inhibitors
MeSH PA	D000925	Anticoagulants
MeSH PA	D000991	Antithrombins
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D006401	Hematologic Agents
MeSH PA	D010975	Platelet Aggregation Inhibitors
MeSH PA	D011480	Protease Inhibitors

Showing 1 to 10 of 11 entries

Previous1 2Next

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

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Percutaneous coronary intervention	indication	415070008
Thrombosis Prevention in Heparin-Induced Thrombocytopenia	indication
Thrombosis in Heparin Induced Thrombocytopenia	indication
Peptic ulcer	contraindication	13200003	DOID:750
Duodenal ulcer disease	contraindication	51868009	DOID:1724
Blood coagulation disorder	contraindication	64779008	DOID:1247
Procedure on central nervous system	contraindication	118679007
Bleeding	contraindication	131148009
Disease of liver	contraindication	235856003	DOID:409
Lumbar puncture	contraindication	277762005

Showing 1 to 10 of 14 entries

Previous1 2Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Show entries

Search:

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.3	acidic
pKa2	9.73	acidic
pKa3	9.18	Basic
pKa4	3.93	Basic

Showing 1 to 4 of 4 entries

Previous1Next

Orange Book patent data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
50MG/50ML (1MG/ML) Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	ARGATROBAN IN SODIUM CHLORIDE	CIPLA	N022434	June 29, 2011	DISCN	INJECTABLE	INTRAVENOUS	7589106	Sept. 26, 2027	METHOD OF TREATING THROMBOSIS
50MG/50ML (1MG/ML) Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	ARGATROBAN IN SODIUM CHLORIDE	CIPLA	N022434	June 29, 2011	DISCN	INJECTABLE	INTRAVENOUS	7687516	Sept. 26, 2027	METHOD OF TREATING AN ARGATROBAN TREATABLE CONDITION

Showing 1 to 2 of 2 entries

Previous1Next

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Prothrombin	Enzyme	P00734	THRB_HUMAN	INHIBITOR	Ki	7.40	WOMBAT-PK	CHEMBL
Coagulation factor X	Enzyme	P00742	FA10_HUMAN		Ki	4.28	CHEMBL
Tissue-type plasminogen activator	Enzyme	P00750	TPA_HUMAN		Ki	4.06	CHEMBL
Cationic trypsin	Enzyme		TRY1_BOVIN		Ki	5.54	CHEMBL
Prothrombin	Enzyme		THRB_BOVIN		Ki	8.02	CHEMBL

Showing 1 to 5 of 5 entries

Previous1Next

External reference:

Show entries

Search:

ID	Source
008966	NDDF
116508003	SNOMEDCT_US
141396-28-3	SECONDARY_CAS_RN
15202	RXNORM
15642	MMSL
398738008	SNOMEDCT_US
4021239	VUID
4021239	VANDF
6385	IUPHAR_LIGAND_ID
63931	MMSL

Showing 1 to 10 of 21 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ARGATROBAN	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0930	INJECTION, SOLUTION	100 mg	INTRAVENOUS	NDA	27 sections
Argatroban	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9288	INJECTION	250 mg	INTRAVENOUS	NDA	25 sections
Argatroban	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9288	INJECTION	250 mg	INTRAVENOUS	NDA	25 sections
Argatroban	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9377	INJECTION	50 mg	INTRAVENOUS	NDA	25 sections
Argatroban	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9377	INJECTION	50 mg	INTRAVENOUS	NDA	25 sections
Argatroban	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9559	INJECTION	50 mg	INTRAVENOUS	NDA	25 sections
Argatroban	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9559	INJECTION	50 mg	INTRAVENOUS	NDA	25 sections
Argatroban	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9674	INJECTION	250 mg	INTRAVENOUS	NDA	25 sections
Argatroban	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9674	INJECTION	250 mg	INTRAVENOUS	NDA	25 sections
Argatroban	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1140	INJECTION, SOLUTION	100 mg	INTRAVENOUS	ANDA	26 sections

Showing 1 to 10 of 29 entries

Previous1 2 3Next