TEDIZOLID

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 Search

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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24688035http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf
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

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Bacterial 70S ribosome 180 Target ID: CHEMBL2363135 Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=25136252	Antagonist 2849
Bacterial 70S ribosome 180 Target ID: CHEMBL2363135 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24688035	Inhibitor 8504

Conditions

Condition	Modality	Highest Phase	Product
Skin infections 59 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	Curative	Approved 8583	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
Staphylococcal skin infections 4 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	Curative	Approved 8583	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
Skin bacterial infections 4 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	Curative	Approved 8583	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
Unknown 2596

C_max

Value	Dose	Analyte	Population
2.2 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=9	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=9	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=9	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=9	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=29	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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

Value	Dose	Analyte	Population
25.6 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=9	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=9	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=9	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=9	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=29	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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

T_1/2

Value	Dose	Analyte	Population
12 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=27	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=29	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=28	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

F_unbound

Value	Dose	Analyte	Population
20% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	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% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000ClinPharmR.pdf#page=58		TEDIZOLID plasma	Homo sapiens

Doses

Dose	Population	Adverse events
1200 mg single, oral Highest studied dose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf	Other AEs: Platelets decreased, Neutrophil Count... Other AEs: Platelets decreased (100%) Neutrophil Count (37.5%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf
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: https://pubmed.ncbi.nlm.nih.gov/32064090/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/32064090/	Disc. AE: Hypertension... AEs leading to discontinuation/dose reduction: Hypertension Sources: https://pubmed.ncbi.nlm.nih.gov/32064090/
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: https://pubmed.ncbi.nlm.nih.gov/33884276/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/33884276/	Disc. AE: Nausea... Other AEs: Cytopenia... AEs leading to discontinuation/dose reduction: Nausea (7%) Other AEs: Cytopenia (14%) Sources: https://pubmed.ncbi.nlm.nih.gov/33884276/
1200 mg single, oral Studied dose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: https://pubmed.ncbi.nlm.nih.gov/27342387	healthy, 18-45 years Health Status: healthy Age Group: 18-45 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/27342387	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: https://pubmed.ncbi.nlm.nih.gov/27342387
400 mg single, intravenous Highest studied dose Dose: 400 mg Route: intravenous Route: single Dose: 400 mg Sources: https://pubmed.ncbi.nlm.nih.gov/24989138	healthy, 29 years Health Status: healthy Age Group: 29 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/24989138	Sources: https://pubmed.ncbi.nlm.nih.gov/24989138
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: https://pubmed.ncbi.nlm.nih.gov/27317442	healthy, 31.0 years (range: 18–41) Health Status: healthy Age Group: 31.0 years (range: 18–41) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/27317442	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: https://pubmed.ncbi.nlm.nih.gov/27317442
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf	unhealthy, 42 years (range: 17 - 86 years) Health Status: unhealthy Age Group: 42 years (range: 17 - 86 years) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252 inducer 1087	substrate 1193 inhibitor 2438 inducer 440	substrate 1388 inhibitor 2507 inducer 109	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2B6 926 CYP2C8 1057 CYP2C19 2057 OAT1 725 OAT3 747 OATP1B1 1079 OATP1B3 961 OCT1 620 OCT2 779 P-gp 1741 BCRP 910	CYP1A2 1197 CYP2B6 776 CYP2C8 810 CYP2C19 1119 OAT1 395 OAT3 391 OATP1B1 503 OATP1B3 435 OCT1 393 OCT2 434 P-gp 2052 SULT1A1 37 SULT2A1 28	CYP1A2 832 CYP2B6 669 CYP2C8 198 CYP2C19 329

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C8 1117	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2D6 2546	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0

Drug as victim

Target	Modality	Activity
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2B6 776	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
SULT1A1 37	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/205435s013,205436s008lbl.pdf#page=10 Page: 10.0	yes
SULT2A1 28	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/205435s013,205436s008lbl.pdf#page=10 Page: 10.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000PharmR.pdf#page=31 Page: 31.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:82717	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:82717
ChemicalBook	CB02484972	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB02484972
MolPort	MolPort-042-624-220	https://www.molport.com/shop/molecule-link/MolPort-042-624-220
ZINC	ZINC000043100956	http://zinc15.docking.org/substances/ZINC000043100956

PubMed

Title	Date	PubMed
Critical role of tedizolid in the treatment of acute bacterial skin and skin structure infections.	2017	28053508
Prolonged use of tedizolid in a pulmonary non-tuberculous mycobacterial infection after linezolid-induced toxicity.	2017 Feb	27999019
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	28061827

Patents

Sample Use Guides

In Vivo Use Guide

Unknown

Route of Administration: Unknown

In Vitro Use Guide

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

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