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

Stem definition	Drug id	CAS RN
antibacterials, nalidixic acid derivatives	1854	151096-09-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: avelox moxifloxacin moxifloxacin hydrochloride avolex moxeza moxifloxacine moxifloxacin HCl	A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent. Molecular weight: 401.44 Formula: C21H24FN3O4 CLOGP: -0.12 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 82.11 ALOGS: -3.38 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

avelox
moxifloxacin
moxifloxacin hydrochloride
avolex
moxeza
moxifloxacine
moxifloxacin HCl

A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.

Molecular weight: 401.44
Formula: C21H24FN3O4
CLOGP: -0.12
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 82.11
ALOGS: -3.38
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.40	g	O
0.40	g	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	86 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	8.20 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	27.50 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	22 %	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	2.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	14.23 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	1.40 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.60 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 10, 1999	FDA	BAYER HLTHCARE

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
Drug hypersensitivity	433.28	12.67	718	37883	309969	63140452
Iris transillumination defect	310.60	12.67	54	38547	50	63450371
Contrast media allergy	299.08	12.67	94	38507	2307	63448114
Toxic anterior segment syndrome	265.80	12.67	80	38521	1691	63448730
Endophthalmitis	192.48	12.67	75	38526	3517	63446904
Corneal oedema	175.79	12.67	56	38545	1437	63448984
Drug resistance	161.08	12.67	124	38477	22809	63427612
Asthma	158.84	12.67	281	38320	127280	63323141
Asthma-chronic obstructive pulmonary disease overlap syndrome	158.08	12.67	56	38545	2005	63448416
Hypopyon	154.01	12.67	43	38558	689	63449732

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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
Visual acuity reduced	248.00	13.32	143	21475	16006	34919307
Choroiditis	225.76	13.32	65	21553	1150	34934163
Eye pain	206.13	13.32	119	21499	13343	34921970
Toxic anterior segment syndrome	201.52	13.32	59	21559	1110	34934203
Intraocular pressure increased	193.88	13.32	85	21533	5298	34930015
Electrocardiogram QT prolonged	177.58	13.32	169	21449	40783	34894530
Iris transillumination defect	176.06	13.32	28	21590	3	34935310
Corneal oedema	167.85	13.32	53	21565	1298	34934015
Endophthalmitis	165.09	13.32	67	21551	3441	34931872
Delirium	152.88	13.32	161	21457	43830	34891483

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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
Iris transillumination defect	421.66	12.10	76	54654	83	79689575
Toxic anterior segment syndrome	413.15	12.10	128	54602	2636	79687022
Corneal oedema	323.95	12.10	105	54625	2515	79687143
Endophthalmitis	314.38	12.10	130	54600	6298	79683360
Drug hypersensitivity	311.23	12.10	654	54076	298262	79391396
Visual acuity reduced	288.02	12.10	204	54526	29265	79660393
Electrocardiogram QT prolonged	248.14	12.10	308	54422	90078	79599580
Drug resistance	237.23	12.10	211	54519	42002	79647656
Choroiditis	236.45	12.10	71	54659	1310	79688348
Contrast media allergy	228.46	12.10	80	54650	2442	79687216

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J01MA14	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Fluoroquinolones
ATC	S01AE07	SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Fluoroquinolones
CHEBI has role	CHEBI:36047	antibacterial drugs
FDA CS	M0023650	Quinolones
FDA CS	M0372253	Fluoroquinolones
FDA EPC	N0000175937	Quinolone Antimicrobial
FDA EPC	N0000193223	Fluoroquinolone Antibacterial
MeSH PA	D000900	Anti-Bacterial Agents
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000970	Antineoplastic 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
Septicemic plague	indication	9012003	DOID:3481
Infection of skin AND/OR subcutaneous tissue	indication	19824006
Staphylococcal pneumonia	indication	22754005
Pneumonia due to Streptococcus	indication	34020007
Pneumonic plague	indication	38976008	DOID:10398
Pneumonia due to Mycoplasma pneumoniae	indication	46970008
Peritonitis	indication	48661000
Bacterial pneumonia	indication	53084003	DOID:874
Pneumonia due to Klebsiella pneumoniae	indication	64479007
Haemophilus influenzae pneumonia	indication	70036007

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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

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.23	acidic
pKa2	8.54	Basic
pKa3	2.92	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Topoisomerase IV	Enzyme	PARC_ECOLI PARE_ECOLI	INHIBITOR			CHEMBL	CHEMBL
DNA gyrase	Enzyme	GYRA_ECOLI GYRB_ECOLI	INHIBITOR	IC50	6.52	CHEMBL	CHEMBL
DNA topoisomerase 4 subunit A	Enzyme	PARC_STAAU		IC50	6.10	CHEMBL
DNA gyrase subunit A	Enzyme	GYRA_MYCTU		IC50	5.04	CHEMBL

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External reference:

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ID	Source
MFX	PDB_CHEM_ID
007927	NDDF
007928	NDDF
1047505	RXNORM
10915	IUPHAR_LIGAND_ID
116347002	SNOMEDCT_US
152946	PUBCHEM_CID
178916	MMSL
186826-86-8	SECONDARY_CAS_RN
213098	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Avelox ABC Pack	HUMAN PRESCRIPTION DRUG LABEL	1	16590-881	TABLET, FILM COATED	400 mg	ORAL	NDA	17 sections
MOXEZA	HUMAN PRESCRIPTION DRUG LABEL	1	0065-0006	SOLUTION	5 mg	OPHTHALMIC	NDA	23 sections
Moxifloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5430	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	24 sections
Moxifloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5430	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	24 sections
Moxifloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6406	TABLET, FILM COATED	400 mg	ORAL	ANDA	30 sections
Moxifloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6406	TABLET, FILM COATED	400 mg	ORAL	ANDA	30 sections
MOXIFLOXACIN	Human Prescription Drug Label	1	16714-643	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	23 sections
MOXIFLOXACIN	Human Prescription Drug Label	1	16714-643	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	23 sections
Moxifloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	17478-519	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	25 sections
Moxifloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	31722-845	TABLET, FILM COATED	400 mg	ORAL	ANDA	28 sections

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