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This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ABSOLUTE
Molecular Formula C17H15FN6O3
Molecular Weight 370.3378
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TEDIZOLID

SMILES

CN1N=NC(=N1)C2=NC=C(C=C2)C3=CC=C(C=C3F)N4C[C@H](CO)OC4=O

InChI

InChIKey=XFALPSLJIHVRKE-GFCCVEGCSA-N
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

HIDE SMILES / InChI

Molecular Formula C17H15FN6O3
Molecular Weight 370.3378
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/?term=25136252

Tedizolid phosphate is an oxazolidinone prodrug which in the body is dephosphorylated to the active compound tedizolid. The antibacterial activity of tedizolid is mediated by binding to the 50S subunit of the bacterial ribosome resulting in inhibition of protein synthesis. Tedizolid inhibits bacterial protein synthesis through a mechanism of action different from that of other non-oxazolidinone class antibacterial drugs; therefore, cross-resistance between tedizolid and other classes of antibacterial drugs is unlikely. Tedizolid is bacteriostatic against Gram Positive bacteria such as enterococci, staphylococci, and streptococci. No drug-drug interactions were identified with tedizolid.

Originator

Curator's Comment: It was developed by Cubist Pharmaceuticals, following acquisition of Trius Therapeutics (originator: Dong-A Pharmaceuticals)

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
SIVEXTRO

Approved Use

Indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by designated susceptible bacteria in adults. To reduce the development of drug-resistant bacteria and maintain the effectiveness of SIVEXTRO and other antibacterial drugs, SIVEXTRO should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

Launch Date

2014
Curative
SIVEXTRO

Approved Use

Indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by designated susceptible bacteria in adults. To reduce the development of drug-resistant bacteria and maintain the effectiveness of SIVEXTRO and other antibacterial drugs, SIVEXTRO should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

Launch Date

2014
Curative
SIVEXTRO

Approved Use

Indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by designated susceptible bacteria in adults. To reduce the development of drug-resistant bacteria and maintain the effectiveness of SIVEXTRO and other antibacterial drugs, SIVEXTRO should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

Launch Date

2014
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.2 μg/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3 μg/mL
200 mg 1 times / day steady-state, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2 μg/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2.3 μg/mL
200 mg single, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2 μg/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2.2 μg/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2.3 μg/mL
200 mg single, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3 μg/mL
200 mg 1 times / day steady-state, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.99 μg/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3.77 μg/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5.21 μg/mL
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5.52 μg/mL
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
9.49 μg/mL
1200 mg single, oral
dose: 1200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.8 μg/mL
200 mg 1 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.8 μg/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2.1 μg/mL
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2.7 μg/mL
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
4.2 μg/mL
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
4.7 μg/mL
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.16 μg/mL
100 mg single, intravenous
dose: 100 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2.62 μg/mL
200 mg single, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
4.53 μg/mL
300 mg single, intravenous
dose: 300 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5.13 μg/mL
400 mg single, intravenous
dose: 400 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2.34 μg/mL
200 mg 1 times / day multiple, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3.01 μg/mL
200 mg 1 times / day steady-state, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
25.6 μg × h/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
29.2 μg × h/mL
200 mg 1 times / day steady-state, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
23.8 μg × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
26.6 μg × h/mL
200 mg single, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
23.8 μg × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
25.6 μg × h/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
26.6 μg × h/mL
200 mg single, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
29.2 μg × h/mL
200 mg 1 times / day steady-state, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
25.35 μg × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
56.1 μg × h/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
79.26 μg × h/mL
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
91.8 μg × h/mL
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
123.1 μg × h/mL
1200 mg single, oral
dose: 1200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
16.7 μg × h/mL
200 mg 1 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
22.5 μg × h/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
24.1 μg × h/mL
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
31.2 μg × h/mL
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
46 μg × h/mL
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
52 μg × h/mL
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
17.36 μg × h/mL
100 mg single, intravenous
dose: 100 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
32.58 μg × h/mL
200 mg single, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
51.9 μg × h/mL
300 mg single, intravenous
dose: 300 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
58.7 μg × h/mL
400 mg single, intravenous
dose: 400 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
22.29 μg × h/mL
200 mg 1 times / day multiple, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
29.18 μg × h/mL
200 mg 1 times / day steady-state, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
12 h
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
12 h
200 mg 1 times / day steady-state, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
12 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
12 h
200 mg single, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
11.2 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
10.8 h
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
11.4 h
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
10.6 h
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
10.4 h
1200 mg single, oral
dose: 1200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
11.1 h
200 mg 1 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
10.2 h
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
10.1 h
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
11.9 h
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
8.01 h
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
12.8 h
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
13.4 h
100 mg single, intravenous
dose: 100 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
11 h
200 mg single, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
9.3 h
300 mg single, intravenous
dose: 300 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
11.3 h
400 mg single, intravenous
dose: 400 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
9.33 h
200 mg 1 times / day multiple, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
12.4 h
200 mg 1 times / day steady-state, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
TEDIZOLID plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
20%
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
20%
200 mg 1 times / day steady-state, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
20%
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
20%
200 mg single, intravenous
dose: 200 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
[NO STEREO] TEDIZOLID plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
15.4%
TEDIZOLID plasma
Homo sapiens
Doses

Doses

DosePopulationAdverse events​
1200 mg single, oral
Highest studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: unknown
Food Status: UNKNOWN
Sources:
Disc. AE: Vomiting...
Other AEs: Diarrhea, Nausea...
AEs leading to
discontinuation/dose reduction:
Vomiting (2.2%)
Other AEs:
Diarrhea (13%)
Nausea (6.5%)
Headache (10.9%)
Sources:
400 mg 1 times / day multiple, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: unknown
Food Status: UNKNOWN
Sources:
Other AEs: Platelets decreased, Neutrophil Count...
Other AEs:
Platelets decreased (100%)
Neutrophil Count (37.5%)
Sources:
200 mg 1 times / day multiple, oral
Studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Disc. AE: Hypertension...
AEs leading to
discontinuation/dose reduction:
Hypertension
Sources:
200 mg 1 times / day multiple, oral
Studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Disc. AE: Nausea...
Other AEs: Cytopenia...
AEs leading to
discontinuation/dose reduction:
Nausea (7%)
Other AEs:
Cytopenia (14%)
Sources:
1200 mg single, oral
Studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, 18-45 years
Health Status: healthy
Age Group: 18-45 years
Sex: M+F
Sources:
Disc. AE: Vomiting...
Other AEs: Diarrhea, Headache...
AEs leading to
discontinuation/dose reduction:
Vomiting (3 patients)
Other AEs:
Diarrhea (13%)
Headache (10.9%)
Nausea (6.5%)
Abdominal pain (4.3%)
Vomiting (4.3%)
Sources:
400 mg single, intravenous
Highest studied dose
Dose: 400 mg
Route: intravenous
Route: single
Dose: 400 mg
Sources:
healthy, 29 years
Health Status: healthy
Age Group: 29 years
Sex: M+F
Sources:
400 mg 1 times / day steady, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
healthy, 31.0 years (range: 18–41)
Health Status: healthy
Age Group: 31.0 years (range: 18–41)
Sex: M+F
Sources:
Disc. AE: Reticulocyte count, White blood cell decreased...
AEs leading to
discontinuation/dose reduction:
Reticulocyte count (1 patient)
White blood cell decreased (1 patient)
Sources:
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 42 years (range: 17 - 86 years)
Health Status: unhealthy
Age Group: 42 years (range: 17 - 86 years)
Sources:
Disc. AE: Abdominal discomfort, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Abdominal discomfort (0.2%)
Diarrhea (0.2%)
Vomiting (0.2%)
Osteomyelitis (0.2%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Headache 10.9%
1200 mg single, oral
Highest studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: unknown
Food Status: UNKNOWN
Sources:
Diarrhea 13%
1200 mg single, oral
Highest studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: unknown
Food Status: UNKNOWN
Sources:
Vomiting 2.2%
Disc. AE
1200 mg single, oral
Highest studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: unknown
Food Status: UNKNOWN
Sources:
Nausea 6.5%
1200 mg single, oral
Highest studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: unknown
Food Status: UNKNOWN
Sources:
Platelets decreased 100%
400 mg 1 times / day multiple, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: unknown
Food Status: UNKNOWN
Sources:
Neutrophil Count 37.5%
400 mg 1 times / day multiple, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: unknown
Food Status: UNKNOWN
Sources:
Hypertension Disc. AE
200 mg 1 times / day multiple, oral
Studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Cytopenia 14%
200 mg 1 times / day multiple, oral
Studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Nausea 7%
Disc. AE
200 mg 1 times / day multiple, oral
Studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Headache 10.9%
1200 mg single, oral
Studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, 18-45 years
Health Status: healthy
Age Group: 18-45 years
Sex: M+F
Sources:
Diarrhea 13%
1200 mg single, oral
Studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, 18-45 years
Health Status: healthy
Age Group: 18-45 years
Sex: M+F
Sources:
Vomiting 3 patients
Disc. AE
1200 mg single, oral
Studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, 18-45 years
Health Status: healthy
Age Group: 18-45 years
Sex: M+F
Sources:
Abdominal pain 4.3%
1200 mg single, oral
Studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, 18-45 years
Health Status: healthy
Age Group: 18-45 years
Sex: M+F
Sources:
Vomiting 4.3%
1200 mg single, oral
Studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, 18-45 years
Health Status: healthy
Age Group: 18-45 years
Sex: M+F
Sources:
Nausea 6.5%
1200 mg single, oral
Studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, 18-45 years
Health Status: healthy
Age Group: 18-45 years
Sex: M+F
Sources:
Reticulocyte count 1 patient
Disc. AE
400 mg 1 times / day steady, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
healthy, 31.0 years (range: 18–41)
Health Status: healthy
Age Group: 31.0 years (range: 18–41)
Sex: M+F
Sources:
White blood cell decreased 1 patient
Disc. AE
400 mg 1 times / day steady, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
healthy, 31.0 years (range: 18–41)
Health Status: healthy
Age Group: 31.0 years (range: 18–41)
Sex: M+F
Sources:
Abdominal discomfort 0.2%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 42 years (range: 17 - 86 years)
Health Status: unhealthy
Age Group: 42 years (range: 17 - 86 years)
Sources:
Diarrhea 0.2%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 42 years (range: 17 - 86 years)
Health Status: unhealthy
Age Group: 42 years (range: 17 - 86 years)
Sources:
Osteomyelitis 0.2%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 42 years (range: 17 - 86 years)
Health Status: unhealthy
Age Group: 42 years (range: 17 - 86 years)
Sources:
Vomiting 0.2%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 42 years (range: 17 - 86 years)
Health Status: unhealthy
Age Group: 42 years (range: 17 - 86 years)
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes [IC50 51.1 uM]
yes (co-administration study)
Comment: Coadministration of multiple oral doses of SIVEXTRO (200 mg once daily) increased the Cmax and AUC of rosuvastatin (10 mg single oral dose), a known BCRP substrate, by approximately 55% and 70%, respectively, in healthy adult subjects
Page: 10.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes
yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Critical role of tedizolid in the treatment of acute bacterial skin and skin structure infections.
2017
Prolonged use of tedizolid in a pulmonary non-tuberculous mycobacterial infection after linezolid-induced toxicity.
2017 Feb
Systematic review and network meta-analysis of tedizolid for the treatment of acute bacterial skin and skin structure infections caused by MRSA.
2017 Jan 7
Patents

Sample Use Guides

In Vivo Use Guide
Curator's Comment: SIVEXTRO (tedizolid phosphate) tablet, for oral use or SIVEXTRO (tedizolid phosphate) for injection, for intravenous use.
Unknown
Route of Administration: Unknown
In vitro activities of DA-7157 against clinical isolates of Nocardia brasiliensis and Mycobacterium tuberculosis were determined. Equal MIC50s and MIC90s (0.25 and 0.5 μg/ml, respectively) were found for susceptible and multidrug-resistant isolates of M. tuberculosis. The N. brasiliensis isolates showed an MIC90 of 1 μg/ml and an MIC50 of 1 μg/ml.
Substance Class Chemical
Created
by admin
on Wed Apr 02 09:02:20 GMT 2025
Edited
by admin
on Wed Apr 02 09:02:20 GMT 2025
Record UNII
97HLQ82NGL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TEDIZOLID
INN   MI   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
tedizolid [INN]
Preferred Name English
Tedizolid [WHO-DD]
Common Name English
(5R)-3-{3-Fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl]phenyl}-5-(hydroxymethyl)oxazolidin-2-one
Systematic Name English
TOREZOLID
Common Name English
TEDIZOLID [USAN]
Common Name English
TEDIZOLID [MI]
Common Name English
TR-700
Code English
2-OXAZOLIDINONE, 3-(3-FLUORO-4-(6-(2-METHYL-2H-TETRAZOL-5-YL)-3-PYRIDINYL)PHENYL)-5-(HYDROXYMETHYL)-, (5R)-
Systematic Name English
TEDIZOLID [VANDF]
Common Name English
Classification Tree Code System Code
NDF-RT N0000175495
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
WHO-ATC J01XX11
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
NCI_THESAURUS C258
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
Code System Code Type Description
RXCUI
1540825
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY RxNorm
USAN
UU-155
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
NDF-RT
N0000190113
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY Breast Cancer Resistance Protein Inhibitors [MoA]
PUBCHEM
11234049
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
CHEBI
82717
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
LACTMED
Tedizolid
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
MERCK INDEX
m10517
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY Merck Index
FDA UNII
97HLQ82NGL
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
WIKIPEDIA
Tedizolid
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
DAILYMED
97HLQ82NGL
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
SMS_ID
100000168846
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
ChEMBL
CHEMBL1257051
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
DRUG BANK
DB14569
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
CAS
856866-72-3
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
INN
9136
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
NCI_THESAURUS
C84222
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
EVMPD
SUB182420
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
EPA CompTox
DTXSID10234975
Created by admin on Wed Apr 02 09:02:20 GMT 2025 , Edited by admin on Wed Apr 02 09:02:20 GMT 2025
PRIMARY
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INTRAVENOUS ADMINISTRATION