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 179 Target ID: CHEMBL2363135 Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=25136252	Antagonist 2760
Bacterial 70S ribosome 179 Target ID: CHEMBL2363135 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24688035	Inhibitor 8228

Conditions

Condition	Modality	Highest Phase	Product
Skin infections 55 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	Curative	Approved 8360	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 1.40322236E12
Staphylococcal skin infections 4 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	Curative	Approved 8360	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 1.40322236E12
Skin bacterial infections 4 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205435s000lbl.pdf	Curative	Approved 8360	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 1.40322236E12
Unknown 2565

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 1709 inhibitor 1579 inducer 768	substrate 1010 inhibitor 1752 inducer 383	substrate 1193 inhibitor 1837 inducer 97	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1509 CYP2B6 799 CYP2C8 901 CYP2C19 1463 OAT1 595 OAT3 636 OATP1B1 781 OATP1B3 700 OCT1 506 OCT2 638 P-gp 1437 BCRP 691	CYP1A2 1032 CYP2B6 660 CYP2C8 688 CYP2C19 985 OAT1 320 OAT3 333 OATP1B1 403 OATP1B3 347 OCT1 322 OCT2 348 P-gp 1527 SULT1A1 29 SULT2A1 24	CYP1A2 689 CYP2B6 538 CYP2C8 168 CYP2C19 290

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 1673	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2B6 985	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2B6 985	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C19 1537	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C8 955	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C8 955	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C9 1803	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2D6 1875	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP3A4 1909	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP3A4 1909	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT1 599	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT3 638	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B1 796	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B3 709	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT1 523	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT2 639	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
P-gp 1626	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
BCRP 765	inhibitor 3240 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 1032	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2B6 660	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C19 985	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C8 688	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2C9 1010	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP2D6 1193	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
CYP3A4 1709	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT1 320	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OAT3 333	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B1 403	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B3 347	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT1 322	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT2 348	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205436Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
SULT1A1 29	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/205435s013,205436s008lbl.pdf#page=10 Page: 10.0	yes
SULT2A1 24	substrate 3326 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 1632	inhibitor 1613 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
Recent development of potent analogues of oxazolidinone antibacterial agents.	2013 Feb 1	23273607
Absorption, distribution, metabolism, and excretion of the novel antibacterial prodrug tedizolid phosphate.	2014 Aug	24875463
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
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 `Thu Jul 06 22:45:42 UTC 2023` Edited by `admin` on `Thu Jul 06 22:45:42 UTC 2023`
Record UNII	97HLQ82NGL
Record Status	`Validated (UNII)`
Record Version

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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