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

Stem definition	Drug id	CAS RN
	5272	4474-91-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: angiotensin II giapreza	Angiotensin II is a naturally occurring peptide hormone of the renin-angiotensin-aldosterone system (RAAS) that causes vasoconstriction and an increase in blood pressure. Angiotensin II raises blood pressure by vasoconstriction and increased aldosterone release. Direct action of angiotensin II on the vessel wall is mediated by binding to the G-protein-coupled angiotensin II receptor type 1 on vascular smooth muscle cells, which stimulates Ca2+/calmodulin-dependent phosphorylation of myosin and causes smooth muscle contraction. Molecular weight: 1046.20 Formula: C50H71N13O12 CLOGP: -3.84 LIPINSKI: None HAC: 25 HDO: 14 TPSA: 406.34 ALOGS: -4.75 ROTB: 29 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

angiotensin II
giapreza

Angiotensin II is a naturally occurring peptide hormone of the renin-angiotensin-aldosterone system (RAAS) that causes vasoconstriction and an increase in blood pressure. Angiotensin II raises blood pressure by vasoconstriction and increased aldosterone release. Direct action of angiotensin II on the vessel wall is mediated by binding to the G-protein-coupled angiotensin II receptor type 1 on vascular smooth muscle cells, which stimulates Ca2+/calmodulin-dependent phosphorylation of myosin and causes smooth muscle contraction.

Molecular weight: 1046.20
Formula: C50H71N13O12
CLOGP: -3.84
LIPINSKI: None
HAC: 25
HDO: 14
TPSA: 406.34
ALOGS: -4.75
ROTB: 29

Status: OFP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

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Date	Agency	Company	Orphan
Aug. 23, 2019	EMA	La Jolla Pharmaceutical II B.V.
Dec. 21, 2017	FDA	LA JOLLA PHARMACEUTICAL CO

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FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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FDA Adverse Event Reporting System (Geriatric)

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C01CX09	CARDIOVASCULAR SYSTEM CARDIAC THERAPY CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES Other cardiac stimulants
CHEBI has role	CHEBI:77746	Homo sapiens metabolite
FDA EPC	N0000192562	Vasoconstrictor
FDA PE	N0000009908	Vasoconstriction
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D014662	Vasoconstrictor Agents

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

Disease	Relation	SNOMED_ID	DOID
Septic shock	symptomatic treatment	76571007

🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	2.68	acidic
pKa2	3.61	acidic
pKa3	9.65	acidic
pKa4	13.04	acidic
pKa5	13.86	acidic
pKa6	10.75	Basic
pKa7	8.45	Basic
pKa8	6.3	Basic

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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
EQ 0.5MG BASE/ML (EQ 0.5MG BASE/ML)	GIAPREZA	LA JOLLA PHARMA	N209360	Dec. 23, 2021	RX	SOLUTION	INTRAVENOUS	10335451	Dec. 16, 2029	TREATING HYPOTENSION WITH ABOUT 20 NG/KG/MIN TO ABOUT 40 NG/KG/MIN ANGIOTENSIN II IN A HUMAN SUBJECT HAVING SEPTIC SHOCK
EQ 0.5MG BASE/ML (EQ 0.5MG BASE/ML)	GIAPREZA	LA JOLLA PHARMA	N209360	Dec. 23, 2021	RX	SOLUTION	INTRAVENOUS	10500247	Dec. 16, 2029	TREATING LOW BLOOD PRESSURE WITH ANGIOTENSIN II WITH AN INITIAL RATE OF ABOUT 5 NG/KG/MIN TO ABOUT 20 NG/KG/MIN IN A SUBJECT HAVING REFRACTORY HYPOTENSION OR SEVERE HYPOTENSION
EQ 0.5MG BASE/ML (EQ 0.5MG BASE/ML)	GIAPREZA	LA JOLLA PHARMA	N209360	Dec. 23, 2021	RX	SOLUTION	INTRAVENOUS	10500247	Dec. 16, 2029	TREATING LOW BLOOD PRESSURE WITH ANGIOTENSIN II WITH AN INITIAL RATE OF ABOUT 5 NG/KG/MIN TO ABOUT 20 NG/KG/MIN IN A SUBJECT HAVING REFRACTORY HYPOTENSION OR SEVERE HYPOTENSION, AND TITRATING THE RATE UP
EQ 0.5MG BASE/ML (EQ 0.5MG BASE/ML)	GIAPREZA	LA JOLLA PHARMA	N209360	Dec. 23, 2021	RX	SOLUTION	INTRAVENOUS	10548943	Dec. 16, 2029	INCREASING BLOOD PRESSURE WITH AN INITIAL RATE OF ABOUT 20 NG/KG/MIN ANGIOTENSIN II IN A HUMAN SUBJECT HAVING SEPTIC SHOCK, AND TITRATING THE RATE UP.
EQ 0.5MG BASE/ML (EQ 0.5MG BASE/ML)	GIAPREZA	LA JOLLA PHARMA	N209360	Dec. 23, 2021	RX	SOLUTION	INTRAVENOUS	10548943	Dec. 16, 2029	INCREASING BLOOD PRESSURE WITH A RATE OF ABOUT 20 NG/KG/MIN TO ABOUT 40 NG/KG/MIN ANGIOTENSIN II IN A HUMAN SUBJECT HAVING SEPTIC SHOCK
EQ 0.5MG BASE/ML (EQ 0.5MG BASE/ML)	GIAPREZA	LA JOLLA PHARMA	N209360	Dec. 23, 2021	RX	SOLUTION	INTRAVENOUS	9867863	Dec. 16, 2029	TREATING REFRACTORY HYPOTENSION WITH ABOUT 5 NG/KG/MIN TO ABOUT 20 NG/KG/MIN ANGIOTENSIN II IN A PATIENT RECEIVING VASOPRESSOR
EQ 0.5MG BASE/ML (EQ 0.5MG BASE/ML)	GIAPREZA	LA JOLLA PHARMA	N209360	Dec. 23, 2021	RX	SOLUTION	INTRAVENOUS	9572856	July 18, 2031	TREATING REFRACTORY HYPOTENSION WITH ABOUT 20 NG/KG/MIN ANGIOTENSIN II IN A PATIENT RECEIVING VASOPRESSOR
EQ 0.5MG BASE/ML (EQ 0.5MG BASE/ML)	GIAPREZA	LA JOLLA PHARMA	N209360	Dec. 23, 2021	RX	SOLUTION	INTRAVENOUS	10028995	Dec. 18, 2034	MAINTAINING MEAN ARTERIAL PRESSURE OF ABOUT 65 MMHG OR ABOVE WITH ABOUT 1 NG/KG/MIN TO ABOUT 40 NG/KG/MIN ANGIOTENSIN II IN HYPOTENSIVE PATIENTS TREATED WITH VASOPRESSIN OR A VASOPRESSIN ANALOGUE AND REDUCING VASOPRESSIN OR VASOPRESSIN ANALOGUE USE
EQ 0.5MG BASE/ML (EQ 0.5MG BASE/ML)	GIAPREZA	LA JOLLA PHARMA	N209360	Dec. 23, 2021	RX	SOLUTION	INTRAVENOUS	10493124	Dec. 18, 2034	TREATING LOW BLOOD PRESSURE WITH ANGIOTENSIN II AT AN INITIAL RATE OF ABOUT 20 NG/KG/MIN AND TITRATING DOWN TO ACHIEVE AND/OR MAINTAIN A MAP OF ABOUT 65 MM HG OR ABOVE
EQ 0.5MG BASE/ML (EQ 0.5MG BASE/ML)	GIAPREZA	LA JOLLA PHARMA	N209360	Dec. 23, 2021	RX	SOLUTION	INTRAVENOUS	11096983	Dec. 18, 2034	TREATING DISTRIBUTIVE SHOCK WITH ANGIOTENSIN II

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Type-1 angiotensin II receptor	GPCR	P30556	AGTR1_HUMAN	AGONIST	IC50	9.30	IUPHAR	DRUG LABEL
Type-2 angiotensin II receptor	GPCR	P50052	AGTR2_HUMAN	AGONIST	Kd	10.20	IUPHAR
Type-1B angiotensin II receptor	GPCR		AGTRB_RAT		Ki	9.51	CHEMBL
Type-1 angiotensin II receptor	GPCR		AGTR1_BOVIN		Kd	8.24	CHEMBL
Type-1A angiotensin II receptor	GPCR		AGTRA_RAT		IC50	9.40	CHEMBL

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External reference:

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ID	Source
172198	PUBCHEM_CID
1999003	RXNORM
2504	IUPHAR_LIGAND_ID
267286	MMSL
4037288	VANDF
6707	INN_ID
764385008	SNOMEDCT_US
85267009	SNOMEDCT_US
C0003009	UMLSCUI
C000627694	MESH_SUPPLEMENTAL_RECORD_UI

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Giapreza	HUMAN PRESCRIPTION DRUG LABEL	1	68547-005	INJECTION	0.50 mg	INTRAVENOUS	NDA	27 sections
Giapreza	HUMAN PRESCRIPTION DRUG LABEL	1	68547-005	INJECTION	0.50 mg	INTRAVENOUS	NDA	27 sections
Giapreza	HUMAN PRESCRIPTION DRUG LABEL	1	68547-501	INJECTION	2.50 mg	INTRAVENOUS	NDA	27 sections
Giapreza	HUMAN PRESCRIPTION DRUG LABEL	1	68547-501	INJECTION	2.50 mg	INTRAVENOUS	NDA	27 sections
Giapreza	HUMAN PRESCRIPTION DRUG LABEL	1	68547-501	INJECTION	2.50 mg	INTRAVENOUS	NDA	27 sections

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