Details of the Drug

General Information of Drug (ID: DMG2SKR)

Drug Name
Tedizolid
Synonyms
Tedizolid; Torezolid; 856866-72-3; TR-700; Da 7157; UNII-97HLQ82NGL; DA-7157; TR 700; 97HLQ82NGL; CHEBI:82717; (5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)-3-pyridyl]phenyl]-5-(hydroxymethyl)oxazolidin-2-one; Tedizolid [USAN:INN]; Tedizolid (USAN/INN); SCHEMBL440398; CHEMBL1257051; DTXSID10234975; XFALPSLJIHVRKE-GFCCVEGCSA-N; MolPort-042-624-220; AI025; BCP02830; ZINC43100956; AKOS025401974; CS-0687; NCGC00379072-02; AN-27109; AK322133; AC-27738; BC600578; HY-14855
Indication
Disease Entry ICD 11 Status REF
Skin infection 1F28-1G0Z Approved [1]
Affected Organisms
EnterococcusStreptococcusStaphylococcus
ATC Code
J01XX11: Tedizolid
J01XX: Other antibacterials
J01X: OTHER ANTIBACTERIALS
J01: ANTIBACTERIALS FOR SYSTEMIC USE
J: ANTIINFECTIVES FOR SYSTEMIC USE
J01XX11: Tedizolid
J01XX: Other antibacterials
J01X: OTHER ANTIBACTERIALS
J01: ANTIBACTERIALS FOR SYSTEMIC USE
J: ANTIINFECTIVES FOR SYSTEMIC USE
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 370.3
Logarithm of the Partition Coefficient (xlogp) 1.4
Rotatable Bond Count (rotbonds) 4
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 8
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 23.8-25.6 mgh/L [2]
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 2.0-2.2 mg/L [2]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 2.5-3.5 h [2]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
Bioavailability
The bioavailability of drug is 91% [2]
Clearance
The apparent oral clearance of drug is 6.9 +/- 1.7 L/h [2]
Elimination
When given as a single oral dose, approximately 82% of tedizolid is excreted via the feces and 18% in urine [2]
Half-life
The concentration or amount of drug in body reduced by one-half in 12 hours [2]
Metabolism
The drug is metabolized via the liver [2]
Vd
The volume of distribution (Vd) of drug is 67-80 L [2]
Chemical Identifiers
Formula
C17H15FN6O3
IUPAC Name
(5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
Canonical SMILES
CN1N=C(N=N1)C2=NC=C(C=C2)C3=C(C=C(C=C3)N4C[C@@H](OC4=O)CO)F
InChI
InChI=1S/C17H15FN6O3/c1-23-21-16(20-22-23)15-5-2-10(7-19-15)13-4-3-11(6-14(13)18)24-8-12(9-25)27-17(24)26/h2-7,12,25H,8-9H2,1H3/t12-/m1/s1
InChIKey
XFALPSLJIHVRKE-GFCCVEGCSA-N
Cross-matching ID
PubChem CID
11234049
ChEBI ID
CHEMBL82717
CAS Number
856866-72-3
UNII
97HLQ82NGL
DrugBank ID
DB14569
TTD ID
D08KBK
Drug-Molecule Activity Atlas (DMA)NEW Click to Jump to the Detailed DMA Information of This Drug
Drug Pharmacogenomic Perturbation (DPP)NEW Click to Jump to the Detailed DPP Information of This Drug
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Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Bacterial 50S ribosomal RNA (Bact 50S rRNA) TTUWYEA NOUNIPROTAC Modulator [4]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Tedizolid (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Berotralstat DMWA2DZ Major Decreased clearance of Tedizolid due to the transporter inhibition by Berotralstat. Innate/adaptive immunodeficiency [4A00] [5]
Ubrogepant DM749I3 Moderate Decreased clearance of Tedizolid due to the transporter inhibition by Ubrogepant. Migraine [8A80] [6]

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 FDA Approved Products: Sivextro (tedizolid phosphate) tablet and injection
3 BDDCS predictions, self-correcting aspects of BDDCS assignments, BDDCS assignment corrections, and classification for more than 175 additional drugs
4 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
5 Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
6 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.