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

Stem definition	Drug id	CAS RN
antivirals neuraminidase inhibitors	2859	139110-80-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: zanamivir relenza zanamivir hydrate	A guanido-neuraminic acid that is used to inhibit NEURAMINIDASE. Molecular weight: 332.31 Formula: C12H20N4O7 CLOGP: -5.56 LIPINSKI: 2 HAC: 11 HDO: 8 TPSA: 198.22 ALOGS: -2.35 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

zanamivir
relenza
zanamivir hydrate

A guanido-neuraminic acid that is used to inhibit NEURAMINIDASE.

Molecular weight: 332.31
Formula: C12H20N4O7
CLOGP: -5.56
LIPINSKI: 2
HAC: 11
HDO: 8
TPSA: 198.22
ALOGS: -2.35
ROTB: 6

Status: OFP

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

Drug dosage:

Dose	Unit	Route
20	mg	Inhal.powder
1.20	g	P

ADMET properties:

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Property	Value	Reference
S (Water solubility)	36 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	2 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	100 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	1.70 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1.60 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.86 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.86 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.23 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

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Date	Agency	Company	Orphan
April 26, 2019	EMA	GlaxoSmithKline Trading Services Limited
July 26, 1999	FDA	GLAXOSMITHKLINE

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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
Exposure during pregnancy	590.16	42.45	204	1630	155343	63331845
Abnormal behaviour	386.29	42.45	95	1739	21331	63465857
Delivery	181.81	42.45	32	1802	1371	63485817
Hallucination	121.38	42.45	49	1785	54768	63432420
Overdose	120.73	42.45	61	1773	115017	63372171
Loss of consciousness	74.96	42.45	45	1789	118076	63369112
Delirium	68.51	42.45	32	1802	50509	63436679
No adverse event	58.53	42.45	27	1807	41378	63445810
Altered state of consciousness	47.07	42.45	20	1814	25210	63461978

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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
Abnormal behaviour	1108.30	44.67	257	1655	24712	34930307
Hallucination	219.62	44.67	88	1824	51410	34903609
Delirium	139.52	44.67	61	1851	43930	34911089
Overdose	126.49	44.67	72	1840	90987	34864032
Aggression	88.77	44.67	43	1869	38921	34916098
Screaming	84.83	44.67	19	1893	1465	34953554
Restlessness	69.92	44.67	32	1880	25450	34929569
Amnesia	65.56	44.67	31	1881	26532	34928487
Crying	50.90	44.67	17	1895	5845	34949174
Hallucination, auditory	49.23	44.67	20	1892	11897	34943122

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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
Abnormal behaviour	1024.48	39.98	236	2370	36185	79705597
Overdose	310.06	39.98	140	2466	184066	79557716
Hallucination	254.92	39.98	98	2508	85647	79656135
No adverse event	145.03	39.98	52	2554	37140	79704642
Delirium	128.03	39.98	60	2546	84567	79657215
Exposure via breast milk	108.52	39.98	20	2586	976	79740806
Exposure during pregnancy	86.83	39.98	49	2557	101083	79640699
Screaming	71.15	39.98	18	2588	3915	79737867
Pathogen resistance	67.11	39.98	23	2583	14319	79727463
Loss of consciousness	59.76	39.98	47	2559	167896	79573886

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J05AH01	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Neuraminidase inhibitors
CHEBI has role	CHEBI:22587	antiviral agents
CHEBI has role	CHEBI:52425	acetylneuraminidase inhibitors
FDA EPC	N0000175524	Neuraminidase Inhibitor
FDA MoA	N0000175436	Neuraminidase Inhibitors
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000998	Antiviral Agents
MeSH PA	D004791	Enzyme 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
Influenza	indication	6142004	DOID:8469
Delirium	contraindication	2776000
Bronchospasm	contraindication	4386001
Hallucinations	contraindication	7011001
Chronic obstructive lung disease	contraindication	13645005	DOID:3083
Feeling agitated	contraindication	24199005
Seizure disorder	contraindication	128613002
Impaired cognition	contraindication	386806002

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🐶 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	2.46	acidic
pKa2	12.0	acidic
pKa3	13.81	acidic
pKa4	13.85	acidic
pKa5	9.82	Basic

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Orange Book patent data (new drug applications)

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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
Sialidase 3	Enzyme	Q9UQ49	NEUR3_HUMAN		IC50	5.17	CHEMBL
Sialidase 2	Enzyme	Q9Y3R4	NEUR2_HUMAN		Ki	4.77	CHEMBL
Sialidase-4	Enzyme	Q8WWR8	NEUR4_HUMAN		Ki	4.58	CHEMBL
Neuraminidase	Enzyme		NRAM_I34A1	INHIBITOR	IC50	9.30	CHEMBL	CHEMBL
Neuraminidase	Enzyme		NRAM_INBLE	INHIBITOR	Ki	10	CHEMBL	CHEMBL
Neuraminidase	Enzyme		NRAM_I68A0		IC50	8.58	CHEMBL
Neuraminidase	Enzyme		Q6Q793_9INFA		Ki	9.30	CHEMBL
Neuraminidase	Enzyme		A5Z252_9INFA		Ki	9	CHEMBL
Neuraminidase	Enzyme		Q2LFS1_9INFA		Ki	9.40	CHEMBL
Neuraminidase	Enzyme		C4LRQ6_9INFA		Ki	9.30	CHEMBL

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External reference:

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ID	Source
ZMR	PDB_CHEM_ID
007857	NDDF
116100000	SNOMEDCT_US
1217563005	SNOMEDCT_US
12307	IUPHAR_LIGAND_ID
261633	RXNORM
31156	MMSL
387010007	SNOMEDCT_US
4021167	VUID
4021167	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
RELENZA	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0681	POWDER	5 mg	RESPIRATORY (INHALATION)	NDA	26 sections
RELENZA	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0681	POWDER	5 mg	RESPIRATORY (INHALATION)	NDA	26 sections
RELENZA	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0681	POWDER	5 mg	RESPIRATORY (INHALATION)	NDA	26 sections
RELENZA	HUMAN PRESCRIPTION DRUG LABEL	1	54868-4377	POWDER	5 mg	RESPIRATORY (INHALATION)	NDA	25 sections
RELENZA	HUMAN PRESCRIPTION DRUG LABEL	1	68258-3030	POWDER	5 mg	RESPIRATORY (INHALATION)	NDA	25 sections

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