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

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdfhttps://www.ncbi.nlm.nih.gov/pubmed/24688035
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/?term=25136252

Tedizolid (also known as TR-700, DA-7157) as is an active compound, which is produced by plasma or intestinal phosphatases, after administration of the drug, tedizolid phosphate either orally or intravenously. The mechanism of action of tedizolid occurs through inhibition of bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S subunit, thereby preventing the formation of the 70S initiation complex and inhibiting protein synthesis.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Bacterial 70S ribosome 179 Target ID: CHEMBL2363135 Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=25136252	Antagonist 2778
Bacterial 70S ribosome 179 Target ID: CHEMBL2363135 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24688035	Inhibitor 8297

Conditions

Condition	Modality	Highest Phase	Product
Skin infections 59 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	Curative	Approved 8429	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 8429	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 8429	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 2578

C_max

Value	Dose	Analyte	Population
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
2.2 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
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
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

AUC

Value	Dose	Analyte	Population
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
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
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
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

T_1/2

Value	Dose	Analyte	Population
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 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 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
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

F_unbound

Value	Dose	Analyte	Population
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 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 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
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

Doses

Dose	Population	Adverse events
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 n = 6 Health Status: healthy Age Group: 18-45 years Sex: M+F Population Size: 6 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 n = 9 Health Status: healthy Age Group: 29 years Sex: M+F Population Size: 9 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) n = 8 Health Status: healthy Age Group: 31.0 years (range: 18–41) Sex: M+F Population Size: 8 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 Page: p. 117	unhealthy, 42 years (range: 17 - 86 years) n = 662 Health Status: unhealthy Age Group: 42 years (range: 17 - 86 years) Population Size: 662 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf Page: p. 117	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 Page: p. 117

AEs

AE	Significance	Dose	Population
Headache	10.9%	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 n = 6 Health Status: healthy Age Group: 18-45 years Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27342387
Diarrhea	13%	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 n = 6 Health Status: healthy Age Group: 18-45 years Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27342387
Vomiting	3 patients Disc. AE	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 n = 6 Health Status: healthy Age Group: 18-45 years Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27342387
Abdominal pain	4.3%	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 n = 6 Health Status: healthy Age Group: 18-45 years Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27342387
Vomiting	4.3%	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 n = 6 Health Status: healthy Age Group: 18-45 years Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27342387
Nausea	6.5%	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 n = 6 Health Status: healthy Age Group: 18-45 years Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27342387
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: https://pubmed.ncbi.nlm.nih.gov/27317442	healthy, 31.0 years (range: 18–41) n = 8 Health Status: healthy Age Group: 31.0 years (range: 18–41) Sex: M+F Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/27317442
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: https://pubmed.ncbi.nlm.nih.gov/27317442	healthy, 31.0 years (range: 18–41) n = 8 Health Status: healthy Age Group: 31.0 years (range: 18–41) Sex: M+F Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/27317442
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf Page: p. 117	unhealthy, 42 years (range: 17 - 86 years) n = 662 Health Status: unhealthy Age Group: 42 years (range: 17 - 86 years) Population Size: 662 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf Page: p. 117
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf Page: p. 117	unhealthy, 42 years (range: 17 - 86 years) n = 662 Health Status: unhealthy Age Group: 42 years (range: 17 - 86 years) Population Size: 662 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf Page: p. 117
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf Page: p. 117	unhealthy, 42 years (range: 17 - 86 years) n = 662 Health Status: unhealthy Age Group: 42 years (range: 17 - 86 years) Population Size: 662 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf Page: p. 117
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf Page: p. 117	unhealthy, 42 years (range: 17 - 86 years) n = 662 Health Status: unhealthy Age Group: 42 years (range: 17 - 86 years) Population Size: 662 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205435Orig1s000MedR.pdf Page: p. 117

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587 inducer 781	substrate 1037 inhibitor 1767 inducer 389	substrate 1217 inhibitor 1852 inducer 97	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2B6 810 CYP2C8 911 CYP2C19 1478 OAT1 599 OAT3 642 OATP1B1 788 OATP1B3 706 OCT1 512 OCT2 647 P-gp 1461 BCRP 699	CYP1A2 1054 CYP2B6 664 CYP2C8 693 CYP2C19 991 OAT1 326 OAT3 339 OATP1B1 406 OATP1B3 350 OCT1 327 OCT2 355 P-gp 1537 SULT1A1 29 SULT2A1 24	CYP1A2 701 CYP2B6 547 CYP2C8 168 CYP2C19 293

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C19 1553	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C8 965	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2D6 1891	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT1 543	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
BCRP 773	inhibitor 3277 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 1054	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2B6 664	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C9 1037	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT1 326	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT3 339	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT1 327	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT2 355	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
SULT1A1 29	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/205435s013,205436s008lbl.pdf#page=10 Page: 10.0	yes
SULT2A1 24	substrate 3367 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 1647	inhibitor 1626 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
Tedizolid phosphate for the treatment of acute bacterial skin and skin structure infections.	2014 Nov	25525633
Single- and multiple-dose pharmacokinetics and absolute bioavailability of tedizolid.	2014 Sep	24989138
Tedizolid Phosphate: a Next-Generation Oxazolidinone.	2015 Feb 24	25708156
Critical role of tedizolid in the treatment of acute bacterial skin and skin structure infections.	2017	28053508

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dosage of SIVEXTRO is 200 mg administered once daily for six (6) days either orally (with or without food) or as an intravenous (IV) infusion in patients 18 years of age or older.

Route of Administration: Oral

In Vitro Use Guide

At least 90% of the microorganisms (Staphylococcus aureus (including methicillin-resistant [MRSA] and methicillinsusceptible [MSSA] isolates); Streptococcus pyogenes; Streptococcus agalactiae; Streptococcus anginosus Group (including S. anginosus, S. intermedius, and S. constellatus); Enterococcus faecalis; Staphylococcus epidermidis (including methicillin-susceptible and methicillin-resistant isolates); Staphylococcus haemolyticus; Staphylococcus lugdunensis; Enterococcus faecium) exhibit an in vitro minimum inhibitory concentration (MIC) less than or equal to 0.5 mcg/mL for tedizolid.

Name

Type

Language

TEDIZOLID

Official 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 [INN]

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