tedizolid profile

DA 7157: an anti-infective agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

tedizolid : A member of the class of pyridines that is pyridine which is substituted by a 2-methyl-2H-tetrazol-5-yl group at position 2 and by a 2-fluoro-4-[(5R)-5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl group at position 5. It is used as its phosphate pro-drug used for the treatment of acute bacterial skin and skin structure infections caused by certain susceptible bacteria, including Staphylococcus aureus (including methicillin-resistant strains (MRSA) and methicillin-susceptible strains), various Streptococcus species, and Enterococcus faecalis. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	11234049
CHEMBL ID	1257051
CHEBI ID	82717
SCHEMBL ID	440398
MeSH ID	M0542249

Synonym
HY-14855
tr-700
(5r)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)-3-pyridyl]phenyl]-5-(hydroxymethyl)oxazolidin-2-one
da-7157
da 7157
D09685
856866-72-3
tedizolid (usan/inn)
chebi:82717 ,
tedizolid
torezolid
CHEMBL1257051
97hlq82ngl ,
(5r)-3-(3-fluoro-4-(6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one
2-oxazolidinone, 3-(3-fluoro-4-(6-(2-methyl-2h-tetrazol-5-yl)-3-pyridinyl)phenyl)-5-(hydroxymethyl)-, (5r)-
tedizolid [usan:inn]
tr 700
unii-97hlq82ngl
3-(3-fluoro-4-(6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-hydroxymethyloxazolidin-2-one
3-(3-fluoro-4-(6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one
CS-0687
S5278
tedizolid [vandf]
(5r)-3-{3-fluoro-4-[6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl]phenyl}-5-(hydroxymethyl)oxazolidin-2-one
tedizolid [usan]
tedizolid [inn]
tedizolid [who-dd]
tedizolid [mi]
(r)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one
XFALPSLJIHVRKE-GFCCVEGCSA-N
(r)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-on
SCHEMBL440398
(5r)-3-{3-fluoro-4-[6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl]phenyl}-5-(hydroxymethyl)-1,3-oxazolidin-2-one
DTXSID10234975 ,
AC-27738
(r)-3-(3-fluoro-4-(6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one
AKOS025401974
NCGC00379072-02
mfcd19442562
DB14569
bdbm50491954
BCP02830
Q7825683
EX-A5826
CCG-268294
u7v ,
tr700
gtpl10865
previously torezolid
(5r)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
AS-56108
torezolid; sivextro
(5r)-3-{3-fluoro-4-[6-(2-methyl-2h-1,2,3,4-tetrazol-5-yl)pyridin-3-yl]phenyl}-5-(hydroxymethyl)-1,3-oxazolidin-2-one
EN300-18530167
j01xx11
dtxcid40157466
tedizolidum
(5r)-3-(3-fluoro-4-(6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)-1,3-oxazolidin-2-one

Research Excerpts

Overview

Tedizolid is an oxazolidinone antibiotic with high potency against Gram-positive bacteria and currently prescribed in bacterial skin and skin-structure infections. Tedizolid (TZD) is an anti-methicillin-resistant Staphylococcus aureus (MRSA) drug.

Excerpt	Reference	Relevance
"Tedizolid phosphate is an oxazolidinone antibacterial agent approved for the treatment of Gram-positive acute bacterial skin and skin structure infections (ABSSSIs) in patients aged ≥12 years. "	( Population Pharmacokinetics, Exposure-Response, and Probability of Target Attainment Analyses for Tedizolid in Adolescent Patients with Acute Bacterial Skin and Skin Structure Infections. Broyde, N; Chou, MZ; De Anda, CS; Duval, V; Feng, HP; Guiastrennec, B; Hardalo, C; Li, D; Ouerdani, A; Rizk, ML; Sabato, PE; Sears, PS, 2021)	2.28
"Tedizolid is an oxazolidinone antibiotic with high potency against Gram-positive bacteria and currently prescribed in bacterial skin and skin-structure infections. "	( Pharmacokinetics and Pharmacodynamics of Tedizolid. Iqbal, K; Milioudi, A; Wicha, SG, 2022)	2.43
"Tedizolid is a bacteriostatic oxazolidine antibiotic that inhibits bacterial protein synthesis, the same mechanism as its predecessor, linezolid."	( Long-term use of tedizolid for pulmonary nocardiosis. Chomei, Y; Iwata, K; Nishimura, S, 2022)	1.78
"Tedizolid is a novel oxazolidinone antibiotic. "	( A pharmacokinetic-pharmacodynamic (PKPD) model-based analysis of tedizolid against enterococci using the hollow-fibre infection model. Amann, LF; Huang, J; Iqbal, K; Rohde, H; Tikiso, T; Wicha, SG; Zeitlinger, M, 2022)	2.4
"Tedizolid (TZD) is an oxazolidinone anti-methicillin-resistant Staphylococcus aureus (MRSA) drug. "	( The anti-inflammatory effect of tedizolid on carrageenan-induced footpad edema rat model. Chuang, VTG; Enoki, Y; Isobe, N; Liu, X; Matsumoto, K; Taguchi, K, 2023)	2.64
"Tedizolid is a protein synthesis inhibitor in clinical use for the treatment of Gram-positive infections. "	( Tedizolid is a promising antimicrobial option for the treatment of Staphylococcus aureus infections in cystic fibrosis patients. Roch, M; Rosato, AE; Taglialegna, A; Varela, MC, 2020)	3.44
"Tedizolid is a new oxazolidinone antibiotic with little real-life data on use outside of skin and soft tissue infections. "	( Tedizolid: a service evaluation in a large UK teaching hospital. Adams, K; Barlow, G; Cullen, L; Delahay, J; Ivan, M; Lillie, PJ; MacLachlan, L; York, JA, 2021)	3.51
"Tedizolid is an oxazolidinone antimicrobial with activity against Gram-positive bacteria, including MRSA. "	( Identification of a novel tedizolid resistance mutation in rpoB of MRSA after in vitro serial passage. Nath, A; Penewit, K; Salipante, SJ; Shen, T; Waalkes, A; Werth, BJ; Xu, L, 2021)	2.36
"Tedizolid phosphate is an oxazolidinone prodrug approved in 2014 for treatment of adults with acute bacterial skin and skin structure infections (ABSSSIs); however, efficacy has not previously been evaluated in children. "	( Safety and Efficacy of Oral and/or Intravenous Tedizolid Phosphate From a Randomized Phase 3 Trial in Adolescents With Acute Bacterial Skin and Skin Structure Infections. Antadze, T; Bradley, JS; Broyde, N; Butterton, JR; Chou, MZ; De Anda, CS; Kim, JY; Ninov, B; Sears, PS; Tayob, MS, 2021)	2.32
"Tedizolid is a second-generation oxazolidinone with activity against Gram-positive bacteria, including MRSA isolates resistant to linezolid. "	( The role of tedizolid in skin and soft tissue infections. Bouza, E; Burillo, A; Muñoz, P, 2018)	2.3
"Tedizolid is a second-generation oxazolidinone, very convenient for treatment of SSTI, in search for other indications including nosocomial pneumonia and bone and joint infections. "	( The role of tedizolid in skin and soft tissue infections. Bouza, E; Burillo, A; Muñoz, P, 2018)	2.3
"Tedizolid is a new oxazolidinone-class antibacterial indicated for the treatment of adults with SSTI caused by Gram-positive pathogens, including S."	( An in vitro evaluation of the efficacy of tedizolid: implications for the treatment of skin and soft tissue infections. ALeryan, M; Delpech, P; Gemmell, C; Jones, B; Lang, S, 2018)	1.47
"Tedizolid is an oxazolidinone with potent in vitro activity against S."	( Comparative efficacy of human-simulated epithelial lining fluid exposures of tedizolid, linezolid and vancomycin in neutropenic and immunocompetent murine models of staphylococcal pneumonia. Abdelraouf, K; Kidd, JM; Nicolau, DP, 2019)	1.46
"Tedizolid phosphate is a novel oxazolidinone prodrug whose active moiety, tedizolid, has improved potency against Gram-positive pathogens and pharmacokinetics, allowing once-daily administration. "	( In vitro, in vivo, and clinical studies of tedizolid to assess the potential for peripheral or central monoamine oxidase interactions. Bartizal, K; Fang, E; Flanagan, S; Minassian, SL; Prokocimer, P, 2013)	2.1
"Tedizolid is a protein synthesis inhibitor in clinical development for the treatment of gram-positive infections. "	( Tedizolid: a new oxazolidinone antimicrobial. Childs, LM; Kisgen, JJ; Mansour, H; Unger, NR, 2014)	3.29
"Tedizolid is an investigational oxazolidinone antibiotic for the treatment of multidrug-resistant gram-positive pathogens such as MRSA, Streptococcus pneumoniae, and VRE, including some linezolid-resistant strains."	( Tedizolid: a new oxazolidinone antimicrobial. Childs, LM; Kisgen, JJ; Mansour, H; Unger, NR, 2014)	3.29
"Tedizolid phosphate is a novel antibacterial prodrug that is rapidly and extensively converted to its active moiety, tedizolid. "	( Tedizolid population pharmacokinetics, exposure response, and target attainment. Fiedler-Kelly, J; Flanagan, S; Lu, Q; Ludwig, E; Passarell, J; Prokocimer, P, 2014)	3.29
"Tedizolid is a novel oxazolidinone antimicrobial administered in its prodrug form, tedizolid phosphate, as a fixed once-daily dose. "	( Pharmacokinetics of Tedizolid in Morbidly Obese and Covariate-Matched Nonobese Adults. Pai, MP, 2016)	2.2
"Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity. "	( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis. Werth, BJ, 2017)	2.15

Effects

Excerpt	Reference	Relevance
"Tedizolid has a favorable pharmacokinetic profile that allows for once-daily dosing and easy i.v.-to-oral conversion."	( Tedizolid: a new oxazolidinone antimicrobial. Childs, LM; Kisgen, JJ; Mansour, H; Unger, NR, 2014)	2.57

Actions

Tedizolid displays linear pharmacokinetics with good tissue penetration. Tedizolid is thought to cause less frequent myelosuppression than linezolid, at least for short-term use.

Excerpt	Reference	Relevance
"Tedizolid displays linear pharmacokinetics with good tissue penetration."	( Pharmacokinetics and Pharmacodynamics of Tedizolid. Iqbal, K; Milioudi, A; Wicha, SG, 2022)	1.71
"Tedizolid is thought to cause less frequent myelosuppression than linezolid, at least for short-term use."	( Long-term use of tedizolid for pulmonary nocardiosis. Chomei, Y; Iwata, K; Nishimura, S, 2022)	1.78
"Tedizolid could inhibit the intracellular bacterial population of both M."	( Is there a role for tedizolid in the treatment of non-tuberculous mycobacterial disease? Hoefsloot, W; Koeken, VACM; Pennings, LJ; Ruth, MM; Svensson, EM; van Ingen, J; Wertheim, HFL, 2020)	1.6

Toxicity

Treatment-emergent adverse events were balanced between treatment groups (tedizolid, 14.5%)

Excerpt	Reference	Relevance
" Myelosuppression and monoamine oxidase inhibition (MAOI) are key independent causes for limiting adverse effects in therapy with the sole approved drug of this class, linezolid."	( New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile. Gordeev, MF; Yuan, ZY, 2014)	0.4
" Adverse events (AEs) were identified from patients' medical records and laboratory data."	( Safety and Tolerability of More than Six Days of Tedizolid Treatment. Calabuig Muñoz, E; Castells Lao, G; Isernia, V; López Suñé, E; Mensa Pueyo, J; Mensa Vendrell, M; Morata Ruiz, L; Moreno Nuñez, L; Oltra Sempere, MR; Pasquau Liaño, J; Pedro-Botet Montoya, ML; Reynaga Sosa, EA; Salavert Lletí, M; Sequera Arquelladas, S; Soriano Viladomiu, A; Tasias Pitarch, M; Yuste Ara, JR, 2020)	0.81
" Treatment-emergent adverse events were balanced between treatment groups (tedizolid, 14."	( Safety and Efficacy of Oral and/or Intravenous Tedizolid Phosphate From a Randomized Phase 3 Trial in Adolescents With Acute Bacterial Skin and Skin Structure Infections. Antadze, T; Bradley, JS; Broyde, N; Butterton, JR; Chou, MZ; De Anda, CS; Kim, JY; Ninov, B; Sears, PS; Tayob, MS, 2021)	1.11
"BackgroundTo investigate the adverse event (AE) profile of tedizolid and linezolid in post-marketing surveillance."	( Serious adverse events with tedizolid and linezolid: pharmacovigilance insights through the FDA adverse event reporting system. De Ponti, F; Fusaroli, M; Gatti, M; Moretti, U; Poluzzi, E; Raschi, E, 2021)	1.16
" Safety outcomes included assessment of treatment-emergent adverse events."	( Efficacy and safety of tedizolid for the treatment of ventilated gram-positive hospital-acquired or ventilator-associated bacterial pneumonia in Japanese patients: Results from a subgroup analysis of a phase 3, randomized, double-blind study comparing ted De Anda, C; Fujimi, S; Kusachi, S; Mikamo, H; Nagashima, M; Oshima, N; Takase, A, 2022)	1.03

Pharmacokinetics

There are no studies describing the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials. The aim of the review was to summarize and critically review the key pharmacokinetic and pharmacodynamic aspects of tedizolic.

Excerpt	Reference	Relevance
" The pharmacokinetic parameters of DA-7218 and DA-7157 were evaluated after intravenous (5, 10 and 20 mg kg(-1)) and oral (20, 50 and 100 mg kg(-1)) administration of DA-7218 to rats."	( Pharmacokinetics of DA-7218, a new oxazolidinone, and its active metabolite, DA-7157, after intravenous and oral administration of DA-7218 and DA-7157 to rats. Bae, SK; Lee, MG; Rhee, JK; Shin, KN; Yang, SH; Yoo, M, 2007)	0.34
" Torezolid (TR-700) is a novel methyltetrazolyl oxazolidinone with potentially different cellular pharmacokinetic properties."	( Cellular pharmacokinetics and intracellular activity of torezolid (TR-700): studies with human macrophage (THP-1) and endothelial (HUVEC) cell lines. Appelbaum, PC; Lemaire, S; Tulkens, PM; Van Bambeke, F, 2009)	0.35
" Single-dose pharmacokinetic studies were conducted in mice for TR-701/700."	( In vivo pharmacodynamics of torezolid phosphate (TR-701), a new oxazolidinone antibiotic, against methicillin-susceptible and methicillin-resistant Staphylococcus aureus strains in a mouse thigh infection model. Drusano, GL; Kulawy, R; Liu, W; Louie, A, 2011)	0.37
" These data highlight the importance of pharmacokinetic confirmation in each model."	( Pharmacokinetics and pulmonary disposition of tedizolid and linezolid in a murine pneumonia model under variable conditions. Crandon, JL; Keel, RA; Nicolau, DP, 2012)	0.64
" To evaluate the potential of the novel oxazolidinone tedizolid to cause similar side effects, nonclinical and pharmacokinetic assessments were conducted."	( Nonclinical and pharmacokinetic assessments to evaluate the potential of tedizolid and linezolid to affect mitochondrial function. Das, D; Fiedler-Kelly, J; Flanagan, S; Hosako, H; McKee, EE; Passarell, J; Prokocimer, P; Radovsky, A; Tulkens, PM, 2015)	0.9
" There are no studies describing the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials."	( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis. Werth, BJ, 2017)	0.94
" To support the use of tedizolid phosphate in adolescents with ABSSSIs, a population pharmacokinetic (PK) model, developed using adult and pediatric data, was updated to include PK data from a phase 3 clinical trial (PN012) that evaluated the safety and efficacy of once-daily oral or intravenous 200-mg tedizolid phosphate treatment in adolescents (12 to <18 years) with ABSSSIs, along with emerging data from a phase 1 trial (PN013) in children (2 to <12 years)."	( Population Pharmacokinetics, Exposure-Response, and Probability of Target Attainment Analyses for Tedizolid in Adolescent Patients with Acute Bacterial Skin and Skin Structure Infections. Broyde, N; Chou, MZ; De Anda, CS; Duval, V; Feng, HP; Guiastrennec, B; Hardalo, C; Li, D; Ouerdani, A; Rizk, ML; Sabato, PE; Sears, PS, 2021)	1.15
" The aim of the review was to summarize and critically review the key pharmacokinetic and pharmacodynamic aspects of tedizolid."	( Pharmacokinetics and Pharmacodynamics of Tedizolid. Iqbal, K; Milioudi, A; Wicha, SG, 2022)	1.2

Compound-Compound Interactions

Excerpt	Reference	Relevance
"Rifampin (RIF) plus clarithromycin (CLR) for 8 weeks is now the standard of care for Buruli ulcer (BU) treatment, but CLR may not be an ideal companion for rifamycins due to bidirectional drug-drug interactions."	( Oxazolidinones Can Replace Clarithromycin in Combination with Rifampin in a Mouse Model of Buruli Ulcer. Almeida, DV; Converse, PJ; Grosset, JH; Lee, J; Li, SY; Nuermberger, EL; Omansen, TF, 2019)	0.51

Bioavailability

Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity. The addition of other oral anti-staphylococcal agents to tedizolid may be unlikely to improve killing.

Excerpt	Reference	Relevance
"4% coefficient of variation), and absolute bioavailability was high (86%)."	( Tedizolid population pharmacokinetics, exposure response, and target attainment. Fiedler-Kelly, J; Flanagan, S; Lu, Q; Ludwig, E; Passarell, J; Prokocimer, P, 2014)	1.85
"Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity."	( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis. Werth, BJ, 2017)	2.15
" The addition of other orally bioavailable anti-staphylococcal agents to tedizolid may be unlikely to improve killing but further research is warranted to assess the impact of these combinations on resistance prevention, or against biofilm-embedded organisms."	( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis. Werth, BJ, 2017)	0.94
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51
"Many lead compounds fail to reach clinical trials despite being potent because of low bioavailability attributed to their insufficient solubility making solubility a primary and crucial factor in early phase drug discovery."	( Structural modification aimed for improving solubility of lead compounds in early phase drug discovery. Baidya, ATK; Das, B; Kumar, R; Mathew, AT; Yadav, AK, 2022)	0.72

Dosage Studied

Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity. A tedizolid dose of 200 mg/day or 700 mg twice a week is recommended for testing in patients.

Excerpt	Relevance	Reference
" Dose fractionation studies showed that AUC/MIC was the pharmacodynamic index linked with efficacy, indicating that once-daily dosing in humans is feasible."	( In vivo pharmacodynamics of torezolid phosphate (TR-701), a new oxazolidinone antibiotic, against methicillin-susceptible and methicillin-resistant Staphylococcus aureus strains in a mouse thigh infection model. Drusano, GL; Kulawy, R; Liu, W; Louie, A, 2011)	0.37
" Adequate dosing of these agents is emphasized to minimize the potential for paradoxical induction of virulence."	( Antivirulence potential of TR-700 and clindamycin on clinical isolates of Staphylococcus aureus producing phenol-soluble modulins. Synold, T; Wong-Beringer, A; Yamaki, J, 2011)	0.37
" Plasma samples were collected over the dosing interval, and participants were randomized to undergo bronchoalveolar lavage (BAL) at 2, 6, 12, or 24 h after the last dose."	( Pulmonary disposition of tedizolid following administration of once-daily oral 200-milligram tedizolid phosphate in healthy adult volunteers. Housman, ST; Kuti, JL; Nicolau, DP; Pope, JS; Russomanno, J; Salerno, E; Shore, E, 2012)	0.68
" The role of individualized drug dosing regimens for other oxazolidinones remains to be proven."	( Drug monitoring and individual dose optimization of antimicrobial drugs: oxazolidinones. Alffenaar, JW; Cattaneo, D; Neely, M, 2016)	0.43
"Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity."	( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis. Werth, BJ, 2017)	2.15
" A tedizolid dose of 200 mg/day or 700 mg twice a week is recommended for testing in patients; the intermittent tedizolid dosing schedule could be much safer than daily linezolid."	( The Sterilizing Effect of Intermittent Tedizolid for Pulmonary Tuberculosis. Cirrincione, K; Deshpande, D; Dheda, K; Gumbo, T; Lee, PS; Nuermberger, E; Srivastava, S, 2018)	1.37
" Clinical investigations with daily doses of 200 mg for 6 days showed non-inferiority to twice-daily dosing of linezolid 600 mg for 10 days in patients with acute bacterial skin and skin-structure infections."	( Pharmacokinetics and Pharmacodynamics of Tedizolid. Iqbal, K; Milioudi, A; Wicha, SG, 2022)	0.99
" Thus, it is necessary to decide the antibiotic dosage considering the CRRT clearance in addition to residual renal function."	( UHPLC-MS/MS method for simultaneous quantification of doripenem, meropenem, ciprofloxacin, levofloxacin, pazufloxacin, linezolid, and tedizolid in filtrate during continuous renal replacement therapy. Goto, K; Itoh, H; Kai, M; Kitano, T; Ohchi, Y; Suzuki, Y; Tanaka, R; Tatsuta, R; Yasuda, N, 2023)	1.11

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Role	Description
antimicrobial agent	A substance that kills or slows the growth of microorganisms, including bacteria, viruses, fungi and protozoans.
drug metabolite	null
protein synthesis inhibitor	A compound, usually an anti-bacterial agent or a toxin, which inhibits the synthesis of a protein.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
pyridines	Any organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives.
tetrazoles	An azole in which the five-membered heterocyclic aromatic skeleton contains four N atoms and one C atom.
organofluorine compound	An organofluorine compound is a compound containing at least one carbon-fluorine bond.
oxazolidinone	An oxazolidine containing one or more oxo groups.
primary alcohol	A primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it.
carbamate ester	Any ester of carbamic acid or its N-substituted derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
G	Vesicular stomatitis virus	Potency	21.3174	0.0123	8.9648	39.8107	AID1645842
Interferon beta	Homo sapiens (human)	Potency	21.3174	0.0033	9.1582	39.8107	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	21.3174	0.0123	8.9648	39.8107	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	21.3174	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	21.3174	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Amine oxidase [flavin-containing] A	Homo sapiens (human)	IC50 (µMol)	8.7000	0.0000	2.3789	9.7700	AID1265126
Amine oxidase [flavin-containing] A	Homo sapiens (human)	Ki	2.0000	0.0019	2.3797	10.0000	AID751392
Amine oxidase [flavin-containing] B	Homo sapiens (human)	IC50 (µMol)	5.7000	0.0000	1.8914	9.5700	AID1265127
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
biogenic amine metabolic process	Amine oxidase [flavin-containing] A	Homo sapiens (human)
positive regulation of signal transduction	Amine oxidase [flavin-containing] A	Homo sapiens (human)
dopamine catabolic process	Amine oxidase [flavin-containing] A	Homo sapiens (human)
response to xenobiotic stimulus	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to toxic substance	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to aluminum ion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to selenium ion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
negative regulation of serotonin secretion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
phenylethylamine catabolic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
substantia nigra development	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to lipopolysaccharide	Amine oxidase [flavin-containing] B	Homo sapiens (human)
dopamine catabolic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to ethanol	Amine oxidase [flavin-containing] B	Homo sapiens (human)
positive regulation of dopamine metabolic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
hydrogen peroxide biosynthetic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to corticosterone	Amine oxidase [flavin-containing] B	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	Amine oxidase [flavin-containing] A	Homo sapiens (human)
primary amine oxidase activity	Amine oxidase [flavin-containing] A	Homo sapiens (human)
aliphatic amine oxidase activity	Amine oxidase [flavin-containing] A	Homo sapiens (human)
monoamine oxidase activity	Amine oxidase [flavin-containing] A	Homo sapiens (human)
flavin adenine dinucleotide binding	Amine oxidase [flavin-containing] A	Homo sapiens (human)
protein binding	Amine oxidase [flavin-containing] B	Homo sapiens (human)
primary amine oxidase activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
electron transfer activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
identical protein binding	Amine oxidase [flavin-containing] B	Homo sapiens (human)
aliphatic amine oxidase activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
monoamine oxidase activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
flavin adenine dinucleotide binding	Amine oxidase [flavin-containing] B	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] A	Homo sapiens (human)
mitochondrial outer membrane	Amine oxidase [flavin-containing] A	Homo sapiens (human)
cytosol	Amine oxidase [flavin-containing] A	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] A	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
mitochondrial envelope	Amine oxidase [flavin-containing] B	Homo sapiens (human)
mitochondrial outer membrane	Amine oxidase [flavin-containing] B	Homo sapiens (human)
dendrite	Amine oxidase [flavin-containing] B	Homo sapiens (human)
neuronal cell body	Amine oxidase [flavin-containing] B	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (153)

Assay ID	Title	Year	Journal	Article
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID590059	Antibacterial activity against methicillin-resistant Staphylococcus aureus by agar dilution method	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID590069	Half life in ICR mouse at 10 mg/kg, iv by LC/MS/MS analysis	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID561091	Antibacterial activity against Bacteroides vulgatus by CLSI M11-A7 agar dilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID583875	Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-1 harboring ribosomal protein L3 Gly155Arg mutant by broth microdilution method	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID561092	Antibacterial activity against Bacteroides thetaiotaomicron by CLSI M11-A7 agar dilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID523047	Antimicrobial activity against Haemophilus influenzae by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523784	Antimicrobial activity against linezolid-susceptible coagulase-negative Staphylococcus by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID534162	Antimicrobial activity against linezolid-resistant Staphylococcus sciuri by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID533936	Antimicrobial activity against linezolid-resistant Staphylococcus aureus 131-6952X harboring plasmid borne cfr gene by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID561096	Antibacterial activity against Peptostreptococcus micros by CLSI M11-A7 agar dilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID561077	Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID523793	Antimicrobial activity against oxacillin-susceptible coagulase-negative Staphylococcus aureus by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID561078	Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID590076	Cmax in ICR mouse at 10 mg/kg, po by LC/MS/MS analysis	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID523049	Antimicrobial activity against beta-lactamase positive Haemophilus influenzae by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID561087	Antibacterial activity against Streptococcus agalactiae by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID523030	Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523029	Antimicrobial activity against Staphylococcus sp. by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID590075	Tmax in ICR mouse at 10 mg/kg, po by LC/MS/MS analysis	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID523035	Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID534161	Antimicrobial activity against linezolid-resistant Staphylococcus hominis by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID523040	Antimicrobial activity against penicillin-susceptible Streptococcus pneumoniae by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID561090	Antibacterial activity against Bacteroides fragilis by CLSI M11-A7 agar dilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID523050	Antimicrobial activity against ampicillin-nonsusceptible beta-lactamase negative Haemophilus influenzae by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID561093	Antibacterial activity against Bacteroides ovatus by CLSI M11-A7 agar dilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID562249	Antibacterial activity against Staphylococcus aureus NARSA NRS127 harboring rplC T433 to T435 and L3 Ser145 deletion mutant by CLSI broth microdilution assay	2009	Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12	Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin.
AID523039	Antimicrobial activity against Streptococcus pneumoniae by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523042	Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523027	Antimicrobial activity against methicillin-susceptible Staphylococcus aureus by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523028	Antimicrobial activity against Staphylococcus aureus by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523827	Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 4 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID523025	Antimicrobial activity against linezolid-resistant Staphylococcus aureus by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523043	Antimicrobial activity against Streptococcus viridans by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID561075	Antibacterial activity against methicillin-resistant Staphylococcus aureus by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID751392	Inhibition of MAO-A (unknown origin) by luciferase reporter gene assay	2013	Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3	Recent development of potent analogues of oxazolidinone antibacterial agents.
AID523036	Antimicrobial activity against vancomycin-resistant Enterococcus faecium by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID561076	Antibacterial activity against community-acquired methicillin-resistant Staphylococcus aureus by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID561097	Antibacterial activity against Porphyromonas asaccharolytica by CLSI M11-A7 agar dilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID523778	Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID561080	Antibacterial activity against vancomycin-resistant Enterococcus faecalis by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID523818	Antimicrobial activity against oxacillin-resistant coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID523792	Antimicrobial activity against oxacillin-resistant Staphylococcus aureus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID523026	Antimicrobial activity against methicillin-resistant Staphylococcus aureus by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID534160	Antimicrobial activity against linezolid-resistant Enterococcus faecium by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID533930	Antimicrobial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus NRS119 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID523034	Antimicrobial activity against vancomycin-resistant Enterococcus faecalis by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523037	Antimicrobial activity against vancomycin-susceptible Enterococcus faecium by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523045	Antimicrobial activity against Listeria monocytogenes by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID561074	Antibacterial activity against methicillin-susceptible Staphylococcus aureus by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID533931	Antimicrobial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus NRS120 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID523041	Antimicrobial activity against penicillin-intermediate Streptococcus pneumoniae by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID561095	Antibacterial activity against Peptostreptococcus anaerobius by CLSI M11-A7 agar dilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID583878	Antibacterial activity against laboratory-derived Staphylococcus aureus ATCC 29213 harboring cfr-containing p42262 by broth microdilution method	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID534157	Antimicrobial activity against linezolid-resistant Staphylococcus aureus by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID562246	Antibacterial activity against Staphylococcus epidermidis 1653059 harboring rplC G469A/C470G, L3 Ala157Arg and 23S rRNA G2447T mutant by CLSI broth microdilution assay	2009	Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12	Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin.
AID523805	Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID561085	Antibacterial activity against penicillin-resistant Streptococcus pneumoniae by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID561083	Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID561098	Antibacterial activity against Prevotella sp. by CLSI M11-A7 agar dilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID533943	Antimicrobial activity against linezolid-resistant Enterococcus faecalis 414 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID523823	Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1866020	Thermodynamic aqueous solubility of the compound	2022	Bioorganic & medicinal chemistry, 02-15, Volume: 56	Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
AID523819	Antimicrobial activity against oxacillin-resistant coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID523804	Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID523038	Antimicrobial activity against streptococcal sp. by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523814	Antimicrobial activity against oxacillin-susceptible coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID590073	Half life in ICR mouse at 10 mg/kg, po by LC/MS/MS analysis	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID1265127	Reversible inhibition of human MAO-B	2015	European journal of medicinal chemistry, Dec-01, Volume: 106	Synthesis and biological evaluation of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives.
AID523033	Antimicrobial activity against Enterococcus by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523031	Antimicrobial activity against vancomycin-nonsusceptible Staphylococcus aureus by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523799	Antimicrobial activity against linezolid-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID534159	Antimicrobial activity against linezolid-resistant Enterococcus faecalis by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID533935	Antimicrobial activity against linezolid-resistant Staphylococcus aureus 004-737X harboring plasmid borne cfr gene by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID533940	Antimicrobial activity against linezolid-resistant Enterococcus faecalis 411 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID523048	Antimicrobial activity against beta-lactamase negative Haemophilus influenzae by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID561081	Antibacterial activity against vancomycin-susceptible Enterococcus faecium by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID729219	Antibacterial activity against Staphylococcus aureus ATCC 29213 after 16 hrs by NCCLS agar dilution method	2013	Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6	Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID561082	Antibacterial activity against vancomycin-resistant Enterococcus faecium by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID523032	Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523044	Antimicrobial activity against Corynebacterium jeikeium by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523795	Antimicrobial activity against oxacillin-resistant coagulase-negative Staphylococcus aureus by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID561079	Antibacterial activity against vancomycin-susceptible Enterococcus faecalis by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID523787	Antimicrobial activity against linezolid-resistant Staphylococcus aureus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID561086	Antibacterial activity against Streptococcus pyogenes by CLSI M7-A7 broth microdilution broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID561084	Antibacterial activity against penicillin-intermediate Streptococcus pneumoniae by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID1265126	Reversible inhibition of human MAO-A	2015	European journal of medicinal chemistry, Dec-01, Volume: 106	Synthesis and biological evaluation of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives.
AID590063	Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected po dosed ICR mouse assessed as protection against mouse mortality administered 1 hr after infection measured up to 7 days	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID523837	Antimicrobial activity against methicillin-resistant Staphylococcus aureus by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID729215	Antibacterial activity against linezolid-resistant Enterococcus faecium after 16 hrs by NCCLS agar dilution method	2013	Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6	Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID523810	Antimicrobial activity against linezolid-susceptible coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID729218	Antibacterial activity against linezolid-resistant Staphylococcus aureus after 16 hrs by NCCLS agar dilution method	2013	Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6	Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID523790	Antimicrobial activity against oxacillin-resistant Staphylococcus aureus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1151704	Antibacterial activity against methicillin-resistant Staphylococcus aureus SAU1009	2014	Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11	New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID534158	Antimicrobial activity against linezolid-resistant Staphylococcus epidermidis by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID561089	Antibacterial activity against Moraxella catarrhalis by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID523797	Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID583706	Antibacterial activity against clinical-derived Staphylococcus aureus isolate harboring ribosomal protein L3 deltaSer145/His146Tyr mutant by broth microdilution method	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID590070	AUC in ICR mouse at 10 mg/kg, iv by LC/MS/MS analysis	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID533944	Antimicrobial activity against linezolid-resistant Enterococcus faecalis 1172 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID561088	Antibacterial activity against Haemophilus influenzae by CLSI M7-A7 broth microdilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID561094	Antibacterial activity against Clostridium perfringens by CLSI M11-A7 agar dilution method	2009	Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8	In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID562247	Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 12228 by CLSI broth microdilution assay	2009	Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12	Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin.
AID523780	Antimicrobial activity against oxacillin-resistant Staphylococcus aureus by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID523782	Antimicrobial activity against linezolid-resistant Staphylococcus aureus by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID523046	Antimicrobial activity against Moraxella catarrhalis by broth dilution method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID729216	Antibacterial activity against linezolid-resistant Enterococcus faecalis after 16 hrs by NCCLS agar dilution method	2013	Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6	Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID583705	Antibacterial activity against clinical-derived Staphylococcus aureus isolate 42262 by broth microdilution method	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID590077	Oral bioavailability in ICR mouse at 10 mg/kg by LC/MS/MS analysis	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID583876	Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-2 harboring ribosomal protein L3 Gly155Arg/Met169Leu mutant by broth microdilution method	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID583708	Antibacterial activity against laboratory-derived Staphylococcus aureus ATCC 29213 by broth microdilution method	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID533933	Antimicrobial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus NRS271 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID534154	Antimicrobial activity against linezolid-resistant Enterococcus faecalis 3124 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID533928	Antimicrobial activity against linezolid-resistant Staphylococcus aureus 1652 harboring U2500A mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID533939	Antimicrobial activity against linezolid-resistant Staphylococcus aureus 480 harboring G2447U in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID533932	Antimicrobial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus NRS121 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID583880	Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-2 harboring ribosomal protein L3 Gly155Arg/Met169Leu mutant and cfr-containing p42262 by broth microdilution method	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID523826	Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 2 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID523809	Antimicrobial activity against linezolid-susceptible coagulase-negative Staphylococcus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID583707	Antibacterial activity against clinical-derived Staphylococcus aureus isolate 51312 harboring ribosomal protein L3 deltaMet169-Gly174 mutant by broth microdilution method	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID523957	Antimicrobial activity against teicoplanin and methicillin-resistant coagulase-negative Staphylococcus by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID583879	Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-1 harboring ribosomal protein L3 Gly155Arg mutant and cfr-containing p42262 by broth microdilution method	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID523834	Ratio of Linezolid MIC50 to compound MIC50 for Linezolid-susceptible Staphylococcus aureus	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID523800	Antimicrobial activity against linezolid-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID533929	Antimicrobial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus NRS127 by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID533938	Antimicrobial activity against linezolid-resistant Staphylococcus aureus 425 harboring G2447U in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID523956	Antimicrobial activity against Linezolid and methicillin-resistant coagulase-negative Staphylococcus by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID590061	Antibacterial activity against vancomycin-resistant Enterococcus by agar dilution method	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID523958	Ratio of Linezolid to compound activity for cfr-expressing methicillin-resistant Staphylococcus aureus	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID562248	Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 by CLSI broth microdilution assay	2009	Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12	Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin.
AID523776	Antimicrobial activity against linezolid-susceptible Staphylococcus aureus by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID533934	Antimicrobial activity against linezolid-resistant Staphylococcus aureus CM/05 3067 harboring chromosomal cfr gene by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID590072	Volume of distribution at steady state in ICR mouse at 10 mg/kg, iv by LC/MS/MS analysis	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID534155	Antimicrobial activity against linezolid-resistant Enterococcus faecalis 3128 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID590074	AUC in ICR mouse at 10 mg/kg, po by LC/MS/MS analysis	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID590060	Antibacterial activity against methicillin-susceptible Staphylococcus aureus by agar dilution method	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID533941	Antimicrobial activity against linezolid-resistant Enterococcus faecalis 412 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID533937	Antimicrobial activity against linezolid-resistant Staphylococcus aureus ATCC 29213 by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID533927	Antimicrobial activity against Staphylococcus aureus 1651 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID523824	Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID729217	Antibacterial activity against linezolid-resistant Staphylococcus epidermidis after 16 hrs by NCCLS agar dilution method	2013	Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6	Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID590062	Antibacterial activity against Haemophilus influenzae by agar dilution method	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID583881	Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-3 harboring ribosomal protein L3 deltaPhe127-His146 mutant and cfr-containing p42262 by broth microdilution method	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID523825	Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 1 ug/ml by CLSI method	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID533942	Antimicrobial activity against linezolid-resistant Enterococcus faecalis 413 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID523833	Ratio of Linezolid MIC90 to compound MIC90 for Linezolid-susceptible Staphylococcus aureus	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID583877	Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-3 harboring ribosomal protein L3 deltaPhe127-His146 mutant by broth microdilution method	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID534156	Antimicrobial activity against linezolid-resistant Enterococcus faecium 854 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID590071	Clearance in ICR mouse at 10 mg/kg, iv by LC/MS/MS analysis	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	10 (7.09)	29.6817
2010's	80 (56.74)	24.3611
2020's	51 (36.17)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	8 (5.67%)	5.53%
Reviews	17 (12.06%)	6.00%
Case Studies	12 (8.51%)	4.05%
Observational	0 (0.00%)	0.25%
Other	104 (73.76%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (25)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Phase III Randomized, Active-comparator-Controlled Clinical Trial to Study the Safety and Efficacy of MK-1986 (Tedizolid Phosphate) and Comparator, in Subjects From Birth to Less Than 12 Years of Age With Acute Bacterial Skin and Skin Structure Infectio [NCT03176134]	Phase 3	100 participants (Actual)	Interventional	2019-01-20	Completed
A Phase 1, Single-Administration Pharmacokinetic and Safety Study of Oral and IV Tedizolid Phosphate in Hospitalized Subjects 2 to <12 Years Old [NCT02750761]	Phase 1	32 participants (Actual)	Interventional	2016-05-02	Completed
Tedizolid Suppressive Antimicrobial Therapy [NCT04662736]		17 participants (Actual)	Observational	2021-02-01	Completed
A Double-Blind, Placebo-Controlled, Single & Multiple Ascending Dose, Safety, Tolerability, & PK Study of an IV Form of TR-701 Free Acid & an Open-Label, Crossover Absolute BA Determination of a TR-701 FA Tablet in Normal Healthy Adults [NCT00983255]	Phase 1	90 participants (Actual)	Interventional	2009-09-30	Completed
A Phase 3 Randomized, Double-Blind, Multicenter Study Comparing the Efficacy and Safety of 6-Day Oral TR-701 Free Acid and 10-Day Oral Linezolid for the Treatment of Acute Bacterial Skin and Skin Structure Infections [NCT01170221]	Phase 3	667 participants (Actual)	Interventional	2010-08-15	Completed
Prospective Cohort Study on Patients With Tedizolid Prolonged Therapy for Orthopedic Device Infections [NCT03378427]		35 participants (Actual)	Interventional	2018-08-28	Completed
Tolerability, Safety, and Efficacy of Tedizolid as Oral Treatment for Bone and Joint Infections [NCT03009045]	Phase 2	44 participants (Actual)	Interventional	2017-02-06	Completed
Evaluation of the Early Bactericidal Activity of Tedizolid and Linezolide Against Mycobacterium Tuberculosis [NCT05534750]	Phase 2	60 participants (Anticipated)	Interventional	2023-04-20	Recruiting
A Phase 1, Single- and Multiple-Dose Safety and Pharmacokinetic Study of Oral and IV Tedizolid Phosphate (MK-1986) in Inpatients Under 2 Years Old [NCT03217565]	Phase 1	47 participants (Actual)	Interventional	2019-02-06	Completed
A Phase 1, Blinded, Placebo-Controlled, Crossover TR-701 FA Study of Blood Pressure Response Post-Tyramine Challenge [NCT01539473]	Phase 1	30 participants (Actual)	Interventional	2012-02-29	Completed
"DART: Sivextro® in Acute Bacterial Skin anD Skin Structure Infection (ABSSSI) in Hospitalized Patients. A Global ObseRvational STudy." [NCT02991131]		108 participants (Actual)	Observational	2016-12-17	Terminated(stopped due to Company decision)
Phase 1, Open-Label, Ophthalmology and Neurology Safety Study of Oral 200 mg TR-701 FA Once Daily for 10 Days in Healthy Adults [NCT01623401]	Phase 1	72 participants (Actual)	Interventional	2012-05-17	Completed
Single Dose Pharmacokinetics of Intravenous Tedizolid Phosphate in Morbidly Obese and Age-, Sex-, and Ideal Body Weight-Matched Non-Obese Adults [NCT02342418]	Phase 4	19 participants (Actual)	Interventional	2015-03-31	Completed
A Phase I Open-Label Study With 200 mg Intravenous TR-701 Free Acid to Assess Safety and Pharmacokinetics in Advanced Renal Impairment Subjects [NCT01452828]	Phase 1	24 participants (Actual)	Interventional	2011-10-31	Completed
Steady-State Pharmacokinetics of Tedizolid in Plasma and Sputum of Patients With Cystic Fibrosis [NCT02444234]	Phase 4	11 participants (Actual)	Interventional	2015-07-31	Completed
A Phase 1 Blinded, Placebo-controlled Crossover Study to Evaluate the Effects of Oral TR 701 Free Acid on the Electrocardiogram [NCT01461460]	Phase 1	48 participants (Actual)	Interventional	2011-11-28	Completed
Phase 2 Open-Label Safety and Exploratory Skin Lesion Measurement Study of 6-Day Oral TR-701 FA in Skin Abscess and Cellulitis Patients [NCT01519778]	Phase 2	200 participants (Actual)	Interventional	2012-02-15	Completed
A Phase 1 Crossover Study of Blood Pressure and Heart Rate Response to Pseudoephedrine Concurrent With Placebo or TR 701 FA [NCT01577459]	Phase 1	18 participants (Actual)	Interventional	2012-04-23	Completed
A Phase 3 Randomized Double-blind Study Comparing TR-701 FA and Linezolid in Ventilated Gram-positive Nosocomial Pneumonia [NCT02019420]	Phase 3	726 participants (Actual)	Interventional	2014-01-06	Completed
Comparative Assessment of Tedizolid Tissue Penetration and Pharmacokinetic Profile Between Diabetic Patients With Wound Infections and Healthy Volunteers Via In Vivo Microdialysis [NCT02620787]	Phase 1	18 participants (Actual)	Interventional	2016-02-23	Completed
A Prospective, Randomized, Open-label, Active-controlled, Multicenter Study to Evaluate the Efficacy and Safety of BAY 1192631 in Japanese Patients With MRSA Infections (Skin and Soft Tissue Infection [SSTI] and SSTI-related Bacteremia) [NCT01967225]	Phase 3	125 participants (Actual)	Interventional	2013-11-23	Completed
A Multiple-Dose Study to Evaluate the Effects of Steady-State Tedizolid Phosphate Administration on the Pharmacokinetics and Safety of a Single Dose of Midazolam and Rosuvastatin [NCT02477514]	Phase 1	18 participants (Actual)	Interventional	2015-06-30	Completed
Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis [NCT05398679]	Phase 4	360 participants (Anticipated)	Interventional	2022-06-01	Not yet recruiting
Phase 3 Study of IV to Oral 6-Day Tedizolid Phosphate Compared With 10-day Comparator in Subjects 12 to < 18 Years With cSSTI. [NCT02276482]	Phase 3	120 participants (Actual)	Interventional	2015-03-25	Completed
A Phase 3 Randomized, Double-Blind, Multicenter Study Comparing the Efficacy and Safety of Intravenous to Oral 6-Day Tedizolid Phosphate and Intravenous to Oral 10-Day Linezolid for the Treatment of Acute Bacterial Skin and Skin Structure Infections [NCT02066402]	Phase 3	598 participants (Actual)	Interventional	2014-03-04	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT01170221 (8) [back to overview]	Clinical Response at 48-72 Hours That is Sustained at the End of Therapy Visit.
NCT01170221 (8) [back to overview]	Clinical Response at 48-72 Hours That is Sustained at the End of Therapy Visit in the Clinically Evaluable-End of Therapy Analysis Sets
NCT01170221 (8) [back to overview]	Early Clinical Response Rate
NCT01170221 (8) [back to overview]	Investigator's Assessment of Clinical Response at the 48-72 Hour Visit
NCT01170221 (8) [back to overview]	Investigator's Assessment of Clinical Response at the Day 7 Visit
NCT01170221 (8) [back to overview]	Investigator's Assessment of Clinical Success at the Post Treatment Evaluation Visit
NCT01170221 (8) [back to overview]	To Compare the Investigator's Assessment of Clinical Success at the Post Treatment Evaluation Visit in the Clinically Evaluable-Post Treatment Evaluation Analysis Set
NCT01170221 (8) [back to overview]	Change From Baseline in Patient-reported Pain, by Study Visit
NCT01519778 (1) [back to overview]	Incidence of Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT01967225 (6) [back to overview]	Reduction Ratio of the Lesion Size From the Screening Visit to Day 3 to Day 4 Visit (Only Skin and Soft Tissue Infection [SSTI])
NCT01967225 (6) [back to overview]	Microbiological Response at Test of Cure (TOC)
NCT01967225 (6) [back to overview]	Microbiological Response at End of Treatment (EOT)
NCT01967225 (6) [back to overview]	Clinical Response at Test of Cure (TOC)
NCT01967225 (6) [back to overview]	Clinical Response at End of Treatment Visit (EOT)
NCT01967225 (6) [back to overview]	Change of the Lesion Size From the Screening Visit by Visit (Only Skin and Soft Tissue Infection [SSTI])
NCT02019420 (12) [back to overview]	Clinical Response at Test of Cure (TOC) Visit in the Clinically-Evaluable (CE) Population
NCT02019420 (12) [back to overview]	Number of Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population
NCT02019420 (12) [back to overview]	Number of Participants With All-Cause Mortality in the Intent-to-Treat (ITT) Population
NCT02019420 (12) [back to overview]	Number of Participants Discontinuing Study Therapy Due to an Adverse Event (AE)
NCT02019420 (12) [back to overview]	Number of Participants With a Favorable Response at Test-of-Cure (TOC) Visit in the Microbiologically-Evaluable 2 (ME-2) Population
NCT02019420 (12) [back to overview]	Number of Participants With a Favorable Response at Test-of-Cure (TOC) Visit in the Microbiological Intent-to-Treat (mITT) Population
NCT02019420 (12) [back to overview]	Number of Participants With a Favorable Response at End-of-Therapy (EOT) Visit in the Microbiologically-Evaluable 1 (ME-1) Population
NCT02019420 (12) [back to overview]	Number of Participants With a Favorable Response at End-of-Therapy (EOT) Visit in the Microbiological Intent-to-Treat (mITT) Population
NCT02019420 (12) [back to overview]	Clinical Response at Test of Cure (TOC) Visit in the Intent-to-Treat (ITT) Population
NCT02019420 (12) [back to overview]	Number of Participants With ≥1 Adverse Events (AEs)
NCT02019420 (12) [back to overview]	Number of Methicillin-Resistant Staphylococcus Aureus (MRSA)-Infected Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population
NCT02019420 (12) [back to overview]	Number of Methicillin-Susceptible Staphylococcus Aureus (MSSA)-Infected Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population
NCT02066402 (11) [back to overview]	Value of the Faces Rating Scale (FRS) Pain Scores at Each Time Point
NCT02066402 (11) [back to overview]	Value of the Visual Analog Scale (VAS) Pain Scores at Each Time Point
NCT02066402 (11) [back to overview]	Change From Baseline in the Faces Rating Scale (FRS) Pain Scores at Each Time Point
NCT02066402 (11) [back to overview]	Percentage of Participants With Early Clinical Response at 48-72 Hours After the First Infusion of Study Drug in the ITT Analysis Set.
NCT02066402 (11) [back to overview]	Change From Baseline in the Visual Analog Scale (VAS) Pain Scores at Each Time Point
NCT02066402 (11) [back to overview]	Investigator's Assessment of Clinical Response at 48-72 Hours
NCT02066402 (11) [back to overview]	Investigator's Assessment of Clinical Response at Day 7 Visit
NCT02066402 (11) [back to overview]	Overall Investigator's Assessment of Clinical Success at Post Therapy Evaluation (PTE) Visit (7-14 Days After EOT Visit) in the Clinically Evaluable at Post Therapy Evaluation (CE-PTE) Analysis Set
NCT02066402 (11) [back to overview]	Overall Investigator's Assessment of Clinical Success at Post Therapy Evaluation (PTE) Visit (7-14 Days After EOT Visit) in the ITT Analysis Set
NCT02066402 (11) [back to overview]	Programmatically Defined Clinical Response at End of Therapy (EOT) Visit in the Clinically Evaluable at EOT (CE-EOT) Analysis Set
NCT02066402 (11) [back to overview]	Programmatically Defined Clinical Response at End of Therapy (EOT) Visit in the ITT Analysis Set
NCT02276482 (9) [back to overview]	Area Under the Plasma Concentration Versus Time Curve Time 0 to 24 Hours (AUC0-24h) of Tedizolid
NCT02276482 (9) [back to overview]	Number of Participants With Investigator's Assessment Indicating Clinical Success at TOC Visit (Clinically Evaluable-Test of Cure [CE-TOC] Analysis Set)
NCT02276482 (9) [back to overview]	Peak Plasma Concentration (Cmax) of Tedizolid
NCT02276482 (9) [back to overview]	Change From Baseline in Lesion Size
NCT02276482 (9) [back to overview]	Number of Participants With Adverse Events on Tedizolid Phosphate and Comparator Drugs
NCT02276482 (9) [back to overview]	Number of Participants With Early Clinical Responses Measured by Lesion Reduction
NCT02276482 (9) [back to overview]	Number of Participants With Investigator's Assessment Indicating Clinical Success at End of Therapy (EOT) Visit (Intent to Treat Analysis Set)
NCT02276482 (9) [back to overview]	Number of Participants With Investigator's Assessment Indicating Clinical Success at EOT Visit (Clinically Evaluable-End of Therapy [CE-EOT] Analysis Set)
NCT02276482 (9) [back to overview]	Number of Participants With Investigator's Assessment Indicating Clinical Success at Test of Cure (TOC) Visit (Intent to Treat Analysis Set)
NCT02342418 (2) [back to overview]	This Outcome Measure is the Tedizolid Area Under the Concentration Time-curve From Time 0 to 72 Hours in Morbidly Obese Subjects and Matched Non-obese Subjects.
NCT02342418 (2) [back to overview]	This Outcome Measure is the Maximum Plasma Concentration of Tedizolid in Morbidly Obese Subjects Compared to Nonobese Subjects
NCT02444234 (6) [back to overview]	Time to Peak Sputum Concentration (Tmax)
NCT02444234 (6) [back to overview]	Time to Peak Plasma Concentration (Tmax)
NCT02444234 (6) [back to overview]	Peak Sputum Concentration
NCT02444234 (6) [back to overview]	Peak Plasma Concentration (Cmax)
NCT02444234 (6) [back to overview]	Area Under the Sputum Concentration Versus Time Curve (AUC)
NCT02444234 (6) [back to overview]	Area Under the Plasma Concentration Versus Time Curve (AUC)
NCT02620787 (3) [back to overview]	Tedizolid AUC in Plasma
NCT02620787 (3) [back to overview]	Tedizolid Tissue Penetration
NCT02620787 (3) [back to overview]	Tedizolid Area Under the Curve (AUC) in Tissue
NCT02750761 (17) [back to overview]	Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid Phosphate (Prodrug) From Time Zero to Infinity
NCT02750761 (17) [back to overview]	Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid Phosphate (Prodrug) From Time Zero to Last Detectable Measurement
NCT02750761 (17) [back to overview]	Clearance (CL) of Tedizolid (Active Metabolite) in Participants Who Received Tedizolid Phosphate Intravenously (IV)
NCT02750761 (17) [back to overview]	Clearance (CL) of Tedizolid Phosphate (Prodrug) in Participants Who Received Tedizolid Phosphate Intravenously (IV)
NCT02750761 (17) [back to overview]	Clearance (CL/F) of Tedizolid (Active Metabolite) in Participants Who Received Oral Tedizolid Phosphate
NCT02750761 (17) [back to overview]	Clearance (CL/F) of Tedizolid Phosphate in Participants Who Received Oral Tedizolid Phosphate (Prodrug)
NCT02750761 (17) [back to overview]	Dose Normalized Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid (Active Metabolite) From Time Zero to Infinity
NCT02750761 (17) [back to overview]	Maximum Observed Drug Concentration in Plasma (Cmax) of Tedizolid Phosphate (Prodrug)
NCT02750761 (17) [back to overview]	Number of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT02750761 (17) [back to overview]	Number of Participants Who Experienced at Least One Adverse Event
NCT02750761 (17) [back to overview]	Terminal Elimination Half-life (T1/2) of Tedizolid (Active Metabolite)
NCT02750761 (17) [back to overview]	Maximum Observed Drug Concentration in Plasma (Cmax) of Tedizolid (the Active Metabolite)
NCT02750761 (17) [back to overview]	Time to Reach Peak Plasma Concentration (Tmax) of Tedizolid Phosphate (Prodrug)
NCT02750761 (17) [back to overview]	Time to Reach Peak Plasma Concentration (Tmax) of Tedizolid (the Active Metabolite)
NCT02750761 (17) [back to overview]	Terminal Elimination Half-life (T1/2) of Tedizolid Phosphate (Prodrug)
NCT02750761 (17) [back to overview]	Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid (Active Metabolite) From Time Zero to Infinity
NCT02750761 (17) [back to overview]	Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid (Active Metabolite) From Time Zero to Last Detectable Measurement
NCT03009045 (3) [back to overview]	Quantify the Safety of Tedizolid for Bone and Joint Infections, Both Hardware and Non-hardware Associated
NCT03009045 (3) [back to overview]	"Number of Participants With an Outcome of Cure as Defined as no Need for Further Antibiotics Beyond the Originally Planned Duration Determined by the Participant's Primary/Treating Physician."
NCT03009045 (3) [back to overview]	Quantify the Tolerability of Tedizolid for Bone and Joint Infections, Both Hardware and Non-hardware Associated

Clinical Response at 48-72 Hours That is Sustained at the End of Therapy Visit.

Responder: No increase in lesion surface area from baseline and oral temperature ≤37.6°C. (NCT01170221)
Timeframe: Day 11

Intervention	participants (Number)
Tedizolid Phosphate	230
Linezolid	241

Intervention	units on a scale (Mean)
	Day 2	Day 4-6	Day 7-9	Day 10-13
Linezolid	-1.5	-3.1	-4.6	-5.5
Tedizolid Phosphate	-1.3	-3.4	-4.5	-5.3

Intervention	Percentage (Mean)
	Day3/4	Day 5 to 13	End of Treatment	Test of Cure
Linezoid - SSTI	-61.46	-94.61	-90.09	-99.09
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI	-32.32	-53.30	-67.69	-81.82

Intervention	Percentage of participants (Number)
	Eradication	Persistence	Elimination(indeterminate)	Missing
Linezoid - Bacteremia	100.0	0.0	0.0	0.0
Linezoid - SSTI	90.0	0.0	0.0	10.0
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI	93.1	3.4	0.0	3.4

Intervention	Percentage of participants (Number)
	Eradication	Persistence	Elimination (indeterminate)
Linezoid - Bacteremia	100.0	0.0	0.0
Linezoid - SSTI	100.0	0.0	0.0
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI	93.1	6.9	0.0

Intervention	Percentage of participants (Number)
	Clinical cure	Clinical failure	Indeterminate
Linezoid - Bacteremia	0.0	0.0	100.0
Linezoid - SSTI	80.0	10.0	10.0
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI	86.2	6.9	6.9

Intervention	Percentage of participants (Number)
	Effective	Ineffective	Indeterminate
Linezoid - Bacteremia	50.0	0.0	50.0
Linezoid - SSTI	90.0	10.0	0.0
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI	93.1	6.9	0.0

Intervention	cm^2 (Mean)
	Day 3/4	Day 5 to 13	End of treatment	Test of cure (n=28, 9)
Linezoid - SSTI	-173.93	-317.66	-280.69	-314.18
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI	-62.05	-134.31	-174.96	-212.63

Intervention	Participants (Count of Participants)
	Clinical Success	Clinical Failure	Indeterminate
Linezolid	146	97	0
Tedizolid	143	124	0

Intervention	Units on a scale (Mean)
	Day 2	48-72 hours	Day 7	EOT
Linezolid	4.2	3.2	2.0	1.3
Tedizolid Phosphate (Sivextro, BAY119-2631)	4.1	3.2	2.1	1.3

Intervention	Percentage of participants (Number)
Tedizolid Phosphate (Sivextro, BAY119-2631)	75.3
Linezolid	79.9

Intervention	Percentage of participants (Number)
	Improving	Stable	Other	Missing
Linezolid	90.3	3.0	0.0	6.7
Tedizolid Phosphate (Sivextro, BAY119-2631)	86.7	4.7	0.7	8.0

Intervention	Percentage of participants (Number)
	Clinical success	Clinical failure or Indeterminate
Linezolid	93.5	6.5
Tedizolid Phosphate (Sivextro, BAY119-2631)	90.4	9.6

Intervention	cm^2 (Mean)
	Baseline	Change at Day 25
Antibiotic Comparator Drug	83.22	-82.51
Tedizolid Phosphate	135.44	-134.27

Intervention	hr*ng/mL (Median)
Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)	NA
Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)	NA
Group 2 Cohort 1: Tedizolid IV 6 mg/kg (2 to <6 Years)	NA
Group 2 Cohort 2: Tedizolid IV 3 mg/kg (2 to <6 Years)	2000
Group 3: Tedizolid Oral 4 mg/kg (6 to <12 Years)	NA
Group 4: Tedizolid Oral 3 mg/kg (2 to <6 Years)	NA

Intervention	hr*ng/mL (Geometric Least Squares Mean)
Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)	64.8
Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)	63.6
Group 2 Cohort 1: Tedizolid IV 6 mg/kg (2 to <6 Years)	433
Group 2 Cohort 2: Tedizolid IV 3 mg/kg (2 to <6 Years)	182
Group 3: Tedizolid Oral 4 mg/kg (6 to <12 Years)	NA
Group 4: Tedizolid Oral 3 mg/kg (2 to <6 Years)	14.1

Intervention	mL/hr (Geometric Mean)
Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)	4164.60
Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)	4145.73
Group 2 Cohort 1: Tedizolid IV 6 mg/kg (2 to <6 Years)	2582.66
Group 2 Cohort 2: Tedizolid IV 3 mg/kg (2 to <6 Years)	2461.08

Intervention	mL/hr/kg (Geometric Mean)
Group 3: Tedizolid Oral 4 mg/kg (6 to <12 Years)	4073.32
Group 4: Tedizolid Oral 3 mg/kg (2 to <6 Years)	2090.77

Intervention	ng/mL (Geometric Least Squares Mean)
Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)	76.3
Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)	82.4
Group 2 Cohort 1: Tedizolid IV 6 mg/kg (2 to <6 Years)	710
Group 2 Cohort 2: Tedizolid IV 3 mg/kg (2 to <6 Years)	234
Group 3: Tedizolid Oral 4 mg/kg (6 to <12 Years)	NA
Group 4: Tedizolid Oral 3 mg/kg (2 to <6 Years)	9.4

Intervention	Hours (Geometric Mean)
Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)	5.18
Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)	4.93
Group 2 Cohort 1: Tedizolid IV 6 mg/kg (2 to <6 Years)	5.51
Group 2 Cohort 2: Tedizolid IV 3 mg/kg (2 to <6 Years)	5.76
Group 3: Tedizolid Oral 4 mg/kg (6 to <12 Years)	6.15
Group 4: Tedizolid Oral 3 mg/kg (2 to <6 Years)	6.79

Intervention	ng/mL (Geometric Least Squares Mean)
Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)	4960
Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)	4140
Group 2 Cohort 1: Tedizolid IV 6 mg/kg (2 to <6 Years)	7460
Group 2 Cohort 2: Tedizolid IV 3 mg/kg (2 to <6 Years)	4190
Group 3: Tedizolid Oral 4 mg/kg (6 to <12 Years)	2590
Group 4: Tedizolid Oral 3 mg/kg (2 to <6 Years)	1820

tedizolid

Description

Cross-References

Synonyms (58)

Research Excerpts

Overview

Effects

Actions

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (3)

Drug Classes (6)

Protein Targets (7)

Potency Measurements

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Biological Processes (60)

Molecular Functions (24)

Ceullar Components (27)

Bioassays (153)

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Studies (141)

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Research Demand Index: 58.93

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Clinical Trials (25)

Trial Overview

Trial Outcomes

Clinical Response at 48-72 Hours That is Sustained at the End of Therapy Visit.

Clinical Response at 48-72 Hours That is Sustained at the End of Therapy Visit in the Clinically Evaluable-End of Therapy Analysis Sets

Early Clinical Response Rate

Investigator's Assessment of Clinical Response at the 48-72 Hour Visit

Investigator's Assessment of Clinical Response at the Day 7 Visit

Investigator's Assessment of Clinical Success at the Post Treatment Evaluation Visit

To Compare the Investigator's Assessment of Clinical Success at the Post Treatment Evaluation Visit in the Clinically Evaluable-Post Treatment Evaluation Analysis Set

Change From Baseline in Patient-reported Pain, by Study Visit

Incidence of Adverse Events (AEs) and Serious Adverse Events (SAEs)

Reduction Ratio of the Lesion Size From the Screening Visit to Day 3 to Day 4 Visit (Only Skin and Soft Tissue Infection [SSTI])

Microbiological Response at Test of Cure (TOC)

Microbiological Response at End of Treatment (EOT)

Clinical Response at Test of Cure (TOC)

Clinical Response at End of Treatment Visit (EOT)

Change of the Lesion Size From the Screening Visit by Visit (Only Skin and Soft Tissue Infection [SSTI])

Clinical Response at Test of Cure (TOC) Visit in the Clinically-Evaluable (CE) Population

Number of Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population

Number of Participants With All-Cause Mortality in the Intent-to-Treat (ITT) Population

Number of Participants Discontinuing Study Therapy Due to an Adverse Event (AE)

Number of Participants With a Favorable Response at Test-of-Cure (TOC) Visit in the Microbiologically-Evaluable 2 (ME-2) Population

Number of Participants With a Favorable Response at Test-of-Cure (TOC) Visit in the Microbiological Intent-to-Treat (mITT) Population

Number of Participants With a Favorable Response at End-of-Therapy (EOT) Visit in the Microbiologically-Evaluable 1 (ME-1) Population

Number of Participants With a Favorable Response at End-of-Therapy (EOT) Visit in the Microbiological Intent-to-Treat (mITT) Population

Clinical Response at Test of Cure (TOC) Visit in the Intent-to-Treat (ITT) Population

Number of Participants With ≥1 Adverse Events (AEs)

Number of Methicillin-Resistant Staphylococcus Aureus (MRSA)-Infected Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population

Number of Methicillin-Susceptible Staphylococcus Aureus (MSSA)-Infected Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population

Value of the Faces Rating Scale (FRS) Pain Scores at Each Time Point

Value of the Visual Analog Scale (VAS) Pain Scores at Each Time Point

Change From Baseline in the Faces Rating Scale (FRS) Pain Scores at Each Time Point

Percentage of Participants With Early Clinical Response at 48-72 Hours After the First Infusion of Study Drug in the ITT Analysis Set.

Change From Baseline in the Visual Analog Scale (VAS) Pain Scores at Each Time Point

Investigator's Assessment of Clinical Response at 48-72 Hours

Investigator's Assessment of Clinical Response at Day 7 Visit

Overall Investigator's Assessment of Clinical Success at Post Therapy Evaluation (PTE) Visit (7-14 Days After EOT Visit) in the Clinically Evaluable at Post Therapy Evaluation (CE-PTE) Analysis Set

Overall Investigator's Assessment of Clinical Success at Post Therapy Evaluation (PTE) Visit (7-14 Days After EOT Visit) in the ITT Analysis Set

Programmatically Defined Clinical Response at End of Therapy (EOT) Visit in the Clinically Evaluable at EOT (CE-EOT) Analysis Set

Programmatically Defined Clinical Response at End of Therapy (EOT) Visit in the ITT Analysis Set

Area Under the Plasma Concentration Versus Time Curve Time 0 to 24 Hours (AUC0-24h) of Tedizolid

Number of Participants With Investigator's Assessment Indicating Clinical Success at TOC Visit (Clinically Evaluable-Test of Cure [CE-TOC] Analysis Set)

Peak Plasma Concentration (Cmax) of Tedizolid

Change From Baseline in Lesion Size

Number of Participants With Adverse Events on Tedizolid Phosphate and Comparator Drugs

Number of Participants With Early Clinical Responses Measured by Lesion Reduction

Number of Participants With Investigator's Assessment Indicating Clinical Success at End of Therapy (EOT) Visit (Intent to Treat Analysis Set)

Number of Participants With Investigator's Assessment Indicating Clinical Success at EOT Visit (Clinically Evaluable-End of Therapy [CE-EOT] Analysis Set)

Number of Participants With Investigator's Assessment Indicating Clinical Success at Test of Cure (TOC) Visit (Intent to Treat Analysis Set)

This Outcome Measure is the Tedizolid Area Under the Concentration Time-curve From Time 0 to 72 Hours in Morbidly Obese Subjects and Matched Non-obese Subjects.

This Outcome Measure is the Maximum Plasma Concentration of Tedizolid in Morbidly Obese Subjects Compared to Nonobese Subjects

Time to Peak Sputum Concentration (Tmax)

Intervention	Hours (Median)
Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)	1.18
Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)	1.10
Group 2 Cohort 1: Tedizolid IV 6 mg/kg (2 to <6 Years)	1.12
Group 2 Cohort 2: Tedizolid IV 3 mg/kg (2 to <6 Years)	1.02
Group 3: Tedizolid Oral 4 mg/kg (6 to <12 Years)	NA
Group 4: Tedizolid Oral 3 mg/kg (2 to <6 Years)	6.0

Intervention	hr*ng/mL (Geometric Least Squares Mean)
Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)	29600
Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)	21000
Group 2 Cohort 1: Tedizolid IV 6 mg/kg (2 to <6 Years)	27300
Group 2 Cohort 2: Tedizolid IV 3 mg/kg (2 to <6 Years)	17300
Group 3: Tedizolid Oral 4 mg/kg (6 to <12 Years)	24900
Group 4: Tedizolid Oral 3 mg/kg (2 to <6 Years)	17200

Intervention	hr*ng/mL (Geometric Least Squares Mean)
Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)	28200
Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)	19700
Group 2 Cohort 1: Tedizolid IV 6 mg/kg (2 to <6 Years)	26800
Group 2 Cohort 2: Tedizolid IV 3 mg/kg (2 to <6 Years)	17100
Group 3: Tedizolid Oral 4 mg/kg (6 to <12 Years)	22700
Group 4: Tedizolid Oral 3 mg/kg (2 to <6 Years)	14600

Intervention	participants (Number)
	High leukocytes	Low leukocytes	Low hemoglobin	Low plateltes	High AST	High ALT	High ALP
Drug: 200mg Oral Tedizolid	0	0	0	0	0	0	0

Intervention	participants (Number)
	Reported peripheral neuropathy	Reported optic neuropathy
Drug: 200mg Oral Tedizolid	0	0

Condition	Indicated	Relationship Strength	Studies	Trials
Infections, Staphylococcal [description not available]	0	8.13	20	0
Staphylococcal Infections Infections with bacteria of the genus STAPHYLOCOCCUS.	0	8.13	20	0
Blood Poisoning [description not available]	0	4.31	2	0
Sepsis Systemic inflammatory response syndrome with a proven or suspected infectious etiology. When sepsis is associated with organ dysfunction distant from the site of infection, it is called severe sepsis. When sepsis is accompanied by HYPOTENSION despite adequate fluid infusion, it is called SEPTIC SHOCK.	0	4.31	2	0
Bacterial Infections, Gram-Positive [description not available]	0	6.46	16	0
Gram-Positive Bacterial Infections Infections caused by bacteria that retain the crystal violet stain (positive) when treated by the gram-staining method.	0	6.46	16	0
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	4.44	7	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
Actinomycetoma [description not available]	0	2.44	2	0
Mycetoma A chronic progressive subcutaneous infection caused by species of fungi (eumycetoma), or actinomycetes (actinomycetoma). It is characterized by tumefaction, abscesses, and tumor-like granules representing microcolonies of pathogens, such as MADURELLA fungi and bacteria ACTINOMYCETES, with different grain colors.	0	2.44	2	0
Actinomyces Infections [description not available]	0	2.04	1	0
Cerebral Nocardiosis [description not available]	0	3.29	5	0
Bacterial Skin Diseases [description not available]	0	11.5	16	6
Skin Diseases, Bacterial Skin diseases caused by bacteria.	0	11.5	16	6
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	0	2.41	1	0
Endotoxemia A condition characterized by the presence of ENDOTOXINS in the blood. On lysis, the outer cell wall of gram-negative bacteria enters the systemic circulation and initiates a pathophysiologic cascade of pro-inflammatory mediators.	0	2.41	1	0
Tuberculosis, Drug-Resistant [description not available]	0	2.41	1	0
Tuberculosis, Multidrug-Resistant Tuberculosis resistant to chemotherapy with two or more ANTITUBERCULAR AGENTS, including at least ISONIAZID and RIFAMPICIN. The problem of resistance is particularly troublesome in tuberculous OPPORTUNISTIC INFECTIONS associated with HIV INFECTIONS. It requires the use of second line drugs which are more toxic than the first line regimens. TB with isolates that have developed further resistance to at least three of the six classes of second line drugs is defined as EXTENSIVELY DRUG-RESISTANT TUBERCULOSIS.	0	2.41	1	0
Bacterial Pneumonia [description not available]	0	10.02	2	1
Ventilator-Associated Pneumonia [description not available]	0	4.72	1	1
Pneumonia, Bacterial Inflammation of the lung parenchyma that is caused by bacterial infections.	0	5.02	2	1
Pneumonia, Ventilator-Associated Serious INFLAMMATION of the LUNG in patients who required the use of PULMONARY VENTILATOR. It is usually caused by bacterial CROSS INFECTION in hospitals.	0	4.72	1	1
Cutaneous Fistula An abnormal passage or communication leading from an internal organ to the surface of the body.	0	2.41	1	0
Koch's Disease [description not available]	0	2.66	2	0
Tuberculosis Any of the infectious diseases of man and other animals caused by species of MYCOBACTERIUM TUBERCULOSIS.	0	2.66	2	0
Anasarca [description not available]	0	2.6	1	0
Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.	0	7.6	1	0
Co-infection [description not available]	0	2.25	1	0
Cystic Fibrosis of Pancreas [description not available]	0	2.25	1	0
Cystic Fibrosis An autosomal recessive genetic disease of the EXOCRINE GLANDS. It is caused by mutations in the gene encoding the CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR expressed in several organs including the LUNG, the PANCREAS, the BILIARY SYSTEM, and the SWEAT GLANDS. Cystic fibrosis is characterized by epithelial secretory dysfunction associated with ductal obstruction resulting in AIRWAY OBSTRUCTION; chronic RESPIRATORY INFECTIONS; PANCREATIC INSUFFICIENCY; maldigestion; salt depletion; and HEAT PROSTRATION.	0	7.25	1	0
Acute Myelogenous Leukemia [description not available]	0	3.12	1	0
Leukemia, Myeloid, Acute Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.	0	3.12	1	0
Airflow Obstruction, Chronic [description not available]	0	2.21	1	0
Pulmonary Disease, Chronic Obstructive A disease of chronic diffuse irreversible airflow obstruction. Subcategories of COPD include CHRONIC BRONCHITIS and PULMONARY EMPHYSEMA.	0	2.21	1	0
Atypical Mycobacterial Infection, Disseminated [description not available]	0	3.3	5	0
Serotonin Syndrome An adverse drug interaction characterized by altered mental status, autonomic dysfunction, and neuromuscular abnormalities. It is most frequently caused by use of both serotonin reuptake inhibitors and monoamine oxidase inhibitors, leading to excess serotonin availability in the CNS at the serotonin 1A receptor.	0	7.25	1	0
Blood Pressure, High [description not available]	0	2.25	1	0
Infections, Prosthesis-Related [description not available]	0	2.25	1	0
Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.	0	2.25	1	0
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	2.25	1	0
Bacterial Endocarditides [description not available]	0	2.61	2	0
Endocarditis, Bacterial Inflammation of the ENDOCARDIUM caused by BACTERIA that entered the bloodstream. The strains of bacteria vary with predisposing factors, such as CONGENITAL HEART DEFECTS; HEART VALVE DISEASES; HEART VALVE PROSTHESIS IMPLANTATION; or intravenous drug use.	0	2.61	2	0
Chronic Illness [description not available]	0	2.25	1	0
Bright Disease A historical classification which is no longer used. It described acute glomerulonephritis, acute nephritic syndrome, or acute nephritis. Named for Richard Bright.	0	2.25	1	0
Primary Peritonitis [description not available]	0	2.63	2	0
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	0	2.25	1	0
Glomerulonephritis Inflammation of the renal glomeruli (KIDNEY GLOMERULUS) that can be classified by the type of glomerular injuries including antibody deposition, complement activation, cellular proliferation, and glomerulosclerosis. These structural and functional abnormalities usually lead to HEMATURIA; PROTEINURIA; HYPERTENSION; and RENAL INSUFFICIENCY.	0	2.25	1	0
Peritonitis INFLAMMATION of the PERITONEUM lining the ABDOMINAL CAVITY as the result of infectious, autoimmune, or chemical processes. Primary peritonitis is due to infection of the PERITONEAL CAVITY via hematogenous or lymphatic spread and without intra-abdominal source. Secondary peritonitis arises from the ABDOMINAL CAVITY itself through RUPTURE or ABSCESS of intra-abdominal organs.	0	7.63	2	0
Diabetic Feet [description not available]	0	2.25	1	0
Diabetes Mellitus, Adult-Onset [description not available]	0	2.25	1	0
Burns Injuries to tissues caused by contact with heat, steam, chemicals (BURNS, CHEMICAL), electricity (BURNS, ELECTRIC), or the like.	0	2.25	1	0
Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.	0	2.25	1	0
Osteomyelitis INFLAMMATION of the bone as a result of infection. It may be caused by a variety of infectious agents, especially pyogenic (PUS - producing) BACTERIA.	0	2.63	2	0
Diabetic Foot Common foot problems in persons with DIABETES MELLITUS, caused by any combination of factors such as DIABETIC NEUROPATHIES; PERIPHERAL VASCULAR DISEASES; and INFECTION. With the loss of sensation and poor circulation, injuries and infections often lead to severe foot ulceration, GANGRENE and AMPUTATION.	0	2.25	1	0
Bone Diseases, Infectious Bone diseases caused by pathogenic microorganisms.	0	2.31	1	0
Buruli Ulcer Disease [description not available]	0	2.63	2	0
Buruli Ulcer A lesion in the skin and subcutaneous tissues due to infections by MYCOBACTERIUM ULCERANS. It was first reported in Uganda, Africa.	0	2.63	2	0
Infections, Soft Tissue [description not available]	0	7.7	8	1
Infection, Wound [description not available]	0	4.62	1	1
Abscess Accumulation of purulent material in tissues, organs, or circumscribed spaces, usually associated with signs of infection.	0	4.62	1	1
Soft Tissue Infections Infections of non-skeletal tissue, i.e., exclusive of bone, ligaments, cartilage, and fibrous tissue. The concept is usually referred to as skin and soft tissue infections and usually subcutaneous and muscle tissue are involved. The predisposing factors in anaerobic infections are trauma, ischemia, and surgery. The organisms often derive from the fecal or oral flora, particularly in wounds associated with intestinal surgery, decubitus ulcer, and human bites. (From Cecil Textbook of Medicine, 19th ed, p1688)	0	7.7	8	1
Experimental Lung Inflammation Inflammation of any part, segment or lobe, of the lung parenchyma.	0	2.54	2	0
Pneumonia Infection of the lung often accompanied by inflammation.	0	2.54	2	0
Bacteremia The presence of viable bacteria circulating in the blood. Fever, chills, tachycardia, and tachypnea are common acute manifestations of bacteremia. The majority of cases are seen in already hospitalized patients, most of whom have underlying diseases or procedures which render their bloodstreams susceptible to invasion.	0	3.55	2	0
Neutropenia A decrease in the number of NEUTROPHILS found in the blood.	0	7.66	2	0
Acute Liver Injury, Drug-Induced [description not available]	0	2.31	1	0
Chemical and Drug Induced Liver Injury A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment.	0	2.31	1	0
2019 Novel Coronavirus Disease [description not available]	0	2.31	1	0
Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).	0	3.53	1	1
Thrombopenia [description not available]	0	2.59	2	0
Thrombocytopenia A subnormal level of BLOOD PLATELETS.	0	7.59	2	0
Adverse Drug Event [description not available]	0	3.09	1	0
Infectious Skin Diseases [description not available]	0	8.65	5	4
Skin Diseases, Infectious Skin diseases caused by bacteria, fungi, parasites, or viruses.	0	8.65	5	4
Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.	0	3.09	1	0
Recrudescence [description not available]	0	3.09	1	0
Health Care Associated Infection [description not available]	0	3.51	2	0
MODS [description not available]	0	2.17	1	0
Cross Infection Any infection which a patient contracts in a health-care institution.	0	3.51	2	0
Multiple Organ Failure A progressive condition usually characterized by combined failure of several organs such as the lungs, liver, kidney, along with some clotting mechanisms, usually postinjury or postoperative.	0	2.17	1	0
Infections, Staphylococcal Skin [description not available]	0	10.98	13	9
Staphylococcal Skin Infections Infections to the skin caused by bacteria of the genus STAPHYLOCOCCUS.	0	10.98	13	9
Pulmonary Consumption [description not available]	0	2.59	2	0
Tuberculosis, Pulmonary MYCOBACTERIUM infections of the lung.	0	2.59	2	0
Arthritis, Degenerative [description not available]	0	2.21	1	0
Osteoarthritis A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.	0	2.21	1	0
Staphylococcal Pneumonia [description not available]	0	8.44	2	0
Pneumonia, Staphylococcal Pneumonia caused by infections with bacteria of the genus STAPHYLOCOCCUS, usually with STAPHYLOCOCCUS AUREUS.	0	3.44	2	0
Community Acquired Infection [description not available]	0	3.12	1	0
Arthritides, Bacterial [description not available]	0	2.21	1	0
Bacterial Disease [description not available]	0	9.38	7	4
Chronic Kidney Failure [description not available]	0	7.71	5	4
Liver Dysfunction [description not available]	0	7.52	4	4
Bacterial Infections Infections by bacteria, general or unspecified.	1	11.38	7	4
Kidney Failure, Chronic The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.	0	7.71	5	4
Liver Diseases Pathological processes of the LIVER.	0	7.52	4	4
Encephalopathy, Toxic [description not available]	0	3.03	1	0
Morbid Obesity [description not available]	0	3.04	1	0
Obesity, Morbid The condition of weighing two, three, or more times the ideal weight, so called because it is associated with many serious and life-threatening disorders. In the BODY MASS INDEX, morbid obesity is defined as having a BMI greater than 40.0 kg/m2.	0	3.04	1	0
Infection, Mycobacterium avium-intracellulare [description not available]	0	2.15	1	0
Mycobacterium avium-intracellulare Infection A nontuberculous infection when occurring in humans. It is characterized by pulmonary disease, lymphadenitis in children, and systemic disease in AIDS patients. Mycobacterium avium-intracellulare infection of birds and swine results in tuberculosis.	0	2.15	1	0