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

Stem definition	Drug id	CAS RN
oxazolidinone antibacterials	1584	165800-03-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: linezolid linospan linox zyvox zyvoxid linezolid sodium chloride linezolide U-100766 U 100766	An oxazolidinone and acetamide derived ANTI-BACTERIAL AGENT and PROTEIN SYNTHESIS INHIBITOR that is used in the treatment of GRAM-POSITIVE BACTERIAL INFECTIONS of the skin and respiratory tract. Molecular weight: 337.35 Formula: C16H20FN3O4 CLOGP: 0.42 LIPINSKI: 0 HAC: 7 HDO: 1 TPSA: 71.11 ALOGS: -2.37 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

linezolid
linospan
linox
zyvox
zyvoxid
linezolid sodium chloride
linezolide
U-100766
U 100766

An oxazolidinone and acetamide derived ANTI-BACTERIAL AGENT and PROTEIN SYNTHESIS INHIBITOR that is used in the treatment of GRAM-POSITIVE BACTERIAL INFECTIONS of the skin and respiratory tract.

Molecular weight: 337.35
Formula: C16H20FN3O4
CLOGP: 0.42
LIPINSKI: 0
HAC: 7
HDO: 1
TPSA: 71.11
ALOGS: -2.37
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
1.20	g	O
1.20	g	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	8 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	50.82 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	4.50 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	30 %	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	1.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.69 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.58 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
April 18, 2000	FDA	PHARMACIA AND UPJOHN

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
Lactic acidosis	767.65	17.20	351	24911	37936	63425824
Thrombocytopenia	709.94	17.20	540	24722	150617	63313143
Serotonin syndrome	609.67	17.20	274	24988	28408	63435352
Anaemia	354.33	17.20	505	24757	292925	63170835
Drug resistance	345.67	17.20	173	25089	22760	63441000
Pathogen resistance	299.52	17.20	108	25154	6290	63457470
Multiple organ dysfunction syndrome	270.45	17.20	205	25057	56547	63407213
Pancytopenia	239.98	17.20	241	25021	96692	63367068
Electrocardiogram QT prolonged	225.67	17.20	188	25074	59342	63404418
Drug interaction	222.89	17.20	357	24905	228774	63234986

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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
Thrombocytopenia	928.14	15.62	905	30632	155342	34770052
Serotonin syndrome	583.40	15.62	307	31230	19626	34905768
Lactic acidosis	389.64	15.62	291	31246	34481	34890913
Electrocardiogram QT prolonged	345.49	15.62	290	31247	40662	34884732
Optic neuropathy	321.41	15.62	104	31433	1861	34923533
Drug resistance	281.47	15.62	213	31324	25714	34899680
Anaemia	276.16	15.62	632	30905	232703	34692691
Pancytopenia	266.55	15.62	376	31161	94781	34830613
Off label use	208.36	15.62	836	30701	418688	34506706
Choroiditis	193.39	15.62	63	31474	1152	34924242

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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
Thrombocytopenia	1579.73	14.96	1345	51548	263914	79427581
Serotonin syndrome	1020.84	14.96	528	52365	44499	79646996
Lactic acidosis	976.77	14.96	598	52295	69761	79621734
Anaemia	608.92	14.96	1070	51823	443945	79247550
Electrocardiogram QT prolonged	536.76	14.96	459	52434	89927	79601568
Drug resistance	520.38	14.96	333	52560	41880	79649615
Optic neuropathy	495.23	14.96	154	52739	3330	79688165
Pancytopenia	488.31	14.96	575	52318	165170	79526325
Pathogen resistance	397.77	14.96	193	52700	14149	79677346
Neuropathy peripheral	374.81	14.96	465	52428	140840	79550655

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J01XX08	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER ANTIBACTERIALS Other antibacterials
CHEBI has role	CHEBI:36047	antibacterial drugs
CHEBI has role	CHEBI:48001	protein synthesis inhibitors
FDA CS	M0361132	Oxazolidinones
FDA EPC	N0000175495	Oxazolidinone Antibacterial
MeSH PA	D000900	Anti-Bacterial Agents
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D011500	Protein Synthesis 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
Staphylococcal pneumonia	indication	22754005
Pneumonia due to Streptococcus	indication	34020007
Vancomycin resistant enterococcus	indication	113727004
Streptococcus pyogenes infection	indication	302809008
Infection due to Staphylococcus aureus	indication	406602003
Complicated Skin and Skin Structure Staphylococcus Aureus Infection	indication
Diabetic Foot Infection Due to Gram-Positive Bacteria	indication
Complicated Skin and Skin Structure Streptococcus Agalactiae Infection	indication
Complicated Skin and Skin Structure Streptococcus Pyogenes Infection	indication
Vancomycin-Resistant Enterococcus Faecium Infection	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	11.4	acidic
pKa2	1.59	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	Pharos	UniProt	Type	Activity value (-log[M])	Bioact source
Amine oxidase [flavin-containing] B	Enzyme	P27338	AOFB_HUMAN	Ki	4.50	WOMBAT-PK
Amine oxidase [flavin-containing] A	Enzyme	P21397	AOFA_HUMAN	Ki	5.10	CHEMBL
Succinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrial	Enzyme	P31040	SDHA_HUMAN	IC50	5.09	CHEMBL
Amine oxidase [flavin-containing] B	Enzyme		AOFB_RAT	IC50	4.77	CHEMBL

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External reference:

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ID	Source
ZLD	PDB_CHEM_ID
008223	NDDF
10827	IUPHAR_LIGAND_ID
125695009	SNOMEDCT_US
190376	RXNORM
229070	MMSL
31932	MMSL
387056004	SNOMEDCT_US
4021218	VUID
4021218	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Linezolid	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0319	POWDER, FOR SUSPENSION	100 mg	ORAL	ANDA	27 sections
Linezolid	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0319	POWDER, FOR SUSPENSION	100 mg	ORAL	ANDA	27 sections
Linezolid	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9534	INJECTION, SOLUTION	600 mg	INTRAVENOUS	ANDA	29 sections
Linezolid	HUMAN PRESCRIPTION DRUG LABEL	1	0409-4883	INJECTION, SOLUTION	2 mg	INTRAVENOUS	NDA	30 sections
Linezolid	HUMAN PRESCRIPTION DRUG LABEL	1	0409-4883	INJECTION, SOLUTION	2 mg	INTRAVENOUS	NDA	30 sections
Linezolid	HUMAN PRESCRIPTION DRUG LABEL	1	0409-4883	INJECTION, SOLUTION	2 mg	INTRAVENOUS	NDA	30 sections
Linezolid	HUMAN PRESCRIPTION DRUG LABEL	1	0781-3431	INJECTION, SOLUTION	200 mg	INTRAVENOUS	ANDA	29 sections
Linezolid	HUMAN PRESCRIPTION DRUG LABEL	1	0781-3433	INJECTION, SOLUTION	600 mg	INTRAVENOUS	ANDA	29 sections
Linezolid	Human Prescription Drug Label	1	0904-6553	TABLET, FILM COATED	600 mg	ORAL	ANDA	28 sections
linezolid	HUMAN PRESCRIPTION DRUG LABEL	1	25021-169	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	29 sections

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