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((S)-TR 700; (S)-DA 7157)
(S)-Tedizolid Chemical Structure
|Product name: (S)-Tedizolid|
|Cat. No.: HY-14855A|
Tedizolid is the active moiety of the prodrug tedizolid phosphate, with high potency against Gram-positive species.
IC50 Value: N/A
The MIC(50) and MIC(90) of tedizolid against both methicillin-susceptible S. aureus (MSSA) and MRSA were 0.25 μg/ml, compared with a MIC(50) of 1 μg/ml and MIC(90) of 2 μg/ml for linezolid. For coagulase-negative staphylococci (n = 7), viridans group streptococci (n = 15), and beta-hemolytic streptococci (n = 3), the MICs ranged from 0.03 to 0.25 μg/ml for tedizolid and from 0.12 to 1 μg/ml for linezolid.
Torezolid (also known as TR-701 and now tedizolid) is an oxazolidinone drug in phase-II clinical trials for complicated skin and skin-structure infections (cSSSI), including those caused by Methicillin-resistant Staphylococcus aureus (MRSA). From Wikipedia
|M.Wt||370.34||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.7002 mL||13.5011 mL||27.0022 mL|
|5 mM||0.5400 mL||2.7002 mL||5.4004 mL|
|10 mM||0.2700 mL||1.3501 mL||2.7002 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|(S)-Tedizolid||Trius Therapeutics Inc||Bacterial skin infection||31-AUG-10||30-SEP-11||Phase 3||19-NOV-13|
|Bayer AG||Bacterial skin infection||30-NOV-13||31-MAR-16||Phase 3||21-NOV-13|
|Trius Therapeutics Inc||Bacterial skin infection||30-SEP-11||31-JAN-13||Phase 3||21-MAY-13|
|Trius Therapeutics Inc||Abscess||29-FEB-12||01-AUG-12||Phase 2||11-SEP-13|
|Trius Therapeutics Inc||Gram positive bacterium infection||30-SEP-08||31-MAY-09||Phase 2||21-FEB-12|
. Choi S, Im W, Bartizal K. Activity of Tedizolid Phosphate (TR-701) in Murine Models of Infection with Penicillin-resistant and Penicillin-sensitive Streptococcus pneumoniae. Antimicrob Agents Chemother. 2012 Jun 19.
The in vitro activity of tedizolid (previously known as torezolid, TR-700) against penicillin-resistant Streptococcus pneumoniae (PRSP) clinical isolates and the in vivo efficacy of tedizolid phosphate (torezolid phosphate, TR-701) in murine models of PRSP systemic infection and penicillin-susceptible S. pneumoniae (PSSP) pneumonia, were examined using linezolid as a comparator. The 90% minimum inhibitory concentration against 28 PRSP isolates was 0.25 μg/ml for tedizolid compared to 1 μg/ml for linezolid. In mice infected systemically with a lethal inoculum of PRSP one hour prior to single administration of either antimicrobial, oral tedizolid phosphate was equipotent (1 isolate) to twofold (3 isolates) more potent than linezolid for survival at day 7, with tedizolid phosphate 50% effective dose (ED(50)) values ranging from 3.19 to 11.53 mg/kg/day. In the PSSP pneumonia model, the ED(50) for survival at day 15 was 2.80 mg/kg/day for oral tedizolid phosphate versus 8.09 mg/kg/day for oral linezolid following 48 h of treatment with either agent. At equivalent doses (10 mg/kg once daily tedizolid phosphate or 5 mg/kg twice daily linezolid), pneumococcal titers in the lungs at 52 h postinfection were approximately 3 orders of magnitude lower with tedizolid phosphate treatment compared with linezolid treatment or no treatment. Lung histopathology showed less inflammatory cell invasion into alveolar spaces in mice treated with tedizolid phosphate than untreated or linezolid-treated mice. These results demonstrate that tedizolid phosphate is effective in murine models of PRSP systemic infection and PSSP pneumonia.
. Prokocimer PP, Bien P, Deanda C, Pillar CM, Bartizal K. In Vitro Activity and Microbiological Efficacy of Tedizolid (TR-700) against Gram-Positive Clinical Isolates from a Phase 2 Study of Oral Tedizolid Phosphate (TR-701) in Patients with Complicated Skin and Skin Structure Infections. Antimicrob Agents Chemother. 2012 Jun 11.
Tedizolid (TR-700, formerly torezolid) is the active moiety of the prodrug tedizolid phosphate (TR-701), a next-generation oxazolidinone, with high potency against gram-positive species, including methicillin-resistant Staphylococcus aureus (MRSA). A recently completed randomized, double-blind phase 2 trial evaluated 200, 300, or 400 mg of oral tedizolid phosphate once daily for 5 to 7 days in patients with complicated skin and skin structure infections. This report examines the in vitro activity of tedizolid and Zyvox? (linezolid) against gram-positive pathogens isolated at baseline and describes the microbiological and clinical efficacy of tedizolid. Of 196 isolates tested, 81.6% were S. aureus, and of these, 76% were MRSA. The MIC(50) and MIC(90) of tedizolid against both methicillin-susceptible S. aureus (MSSA) and MRSA were 0.25 μg/ml, compared with MIC(50) of 1 μg/ml and MIC(90) of 2 μg/ml with linezolid. For coagulase-negative staphylococci (n=7), viridans group streptococci (n=15), and β-hemolytic streptococci (n=3), MICs ranged from 0.03-0.25 μg/ml for tedizolid and 0.12-1 μg/ml for linezolid. Microbiological eradication rates at the test-of-cure visit (7-14 days post-treatment) in the microbiologically evaluable population (n=133) were similar in all treatment groups, with overall eradication rates of 97.7% for all pathogens, 97.9% for MRSA, and 95.7% for MSSA. Clinical cure rates for MRSA and MSSA infections were 96.9% and 95.7%, respectively, across all dose groups. This study confirms the potent in vitro activity of tedizolid against pathogenic gram-positive cocci, including MRSA, and 4-fold greater potency compared with linezolid. All dosages of tedizolid phosphate showed excellent microbiological and clinical efficacy against MRSA and MSSA.
. Keel RA, Tessier PR, Crandon JL, Nicolau DP. Comparative Efficacies of Human Simulated Exposures of Tedizolid and Linezolid against Staphylococcus aureus in the Murine Thigh Infection Model. Antimicrob Agents Chemother. 2012 Aug;56(8):4403-7.
Tedizolid (formally torezolid) is an expanded-spectrum oxazolidinone with enhanced in vitro potency against Gram-positive pathogens, including methicillin-susceptible Staphylococcus aureus (MSSA) and methicillin-resistant S. aureus (MRSA). The efficacies of human simulated exposures of tedizolid and linezolid against S. aureus in an immunocompetent mouse thigh model over 3 days were compared. Four strains of MRSA and one of MSSA with tedizolid and linezolid MICs ranging from 0.25 to 0.5 and from 2 to 4 μg/ml, respectively, were utilized. Tedizolid or linezolid was administered in a regimen simulating a human steady-state 24-h area under the free concentration-time curve of 200 mg every 24 h (Q24) or 600 mg Q12, respectively. Thighs were harvested after 4, 8, 12, 24, 36, 48, and 72 h, and efficacy was determined by the change in bacterial density. The mean bacterial density in control mice increased over the 3-day period. After 24 h of treatment, a reduction in bacterial density of ≥1 log CFU was observed for both the tedizolid and linezolid treatments. Antibacterial activity was enhanced for both agents with a reduction of ≥2.6 log CFU after 72 h of treatment. Any statistically significant differences (P ≤ 0.05) in efficacy between the agents were transient and did not persist throughout the 72-h treatment period. The tedizolid and linezolid regimens demonstrated similar in vivo efficacies against the S. aureus isolates tested. Both agents were bacteriostatic at 24 h and bactericidal on the third day of treatment. These data support the clinical utility of tedizolid for skin and skin structure infections caused by S. aureus, as well as the bactericidal activity of the oxazolidinones after 3 days of treatment.
. Sahre M, Sabarinath S, Grant M, Seubert C, Deanda C, Prokocimer P, Derendorf H. Skin and soft tissue concentrations of tedizolid (formerly torezolid), a novel oxazolidinone, following a single oral dose in healthy volunteers. Int J Antimicrob Agents. 2012 Jul;40(1):51-4.
Plasma concentrations of antimicrobial drugs have long been used to correlate exposure with effect, yet one cannot always assume that unbound plasma and tissue concentrations are similar. Knowledge about unbound tissue concentrations is important in the development of antimicrobial drugs, since most infections are localised in tissues. Therefore, a clinical microdialysis study was conducted to evaluate the distribution of tedizolid (TR-700), the active moiety of the antimicrobial prodrug tedizolid phosphate (TR-701), into interstitial fluid (ISF) of subcutaneous adipose and skeletal muscle tissues following a single oral 600 mg dose of tedizolid phosphate in fasting conditions. Twelve healthy adult subjects were enrolled. Two microdialysis probes were implanted into the thigh of each subject, one into the vastus medialis muscle and one into subcutaneous adipose tissue. Probes were calibrated using retrodialysis. Dialysate samples were collected every 20 min for 12h following a single oral dose of 600 mg tedizolid phosphate, and blood samples were drawn over 24h. Unbound tedizolid levels in plasma were similar to those in muscle and adipose tissue. The ratios of unbound (free) AUC in tissues over unbound AUC in plasma (fAUC(tissue)/fAUC(plasma)) were 1.1 ± 0.2 and 1.2 ± 0.2 for adipose and muscle tissue, respectively. The median half-life was 8.1, 9.2 and 9.6h for plasma, adipose tissue and muscle tissue, respectively. Mean protein binding was 87.2 ± 1.8%. The study drug was very well tolerated. The results of this study show that tedizolid distributes well into ISF of adipose and muscle tissues. Unbound levels of tedizolid in plasma, adipose tissue and muscle tissue were well correlated. Free plasma levels are indicative of unbound levels in the ISF of muscle and adipose tissues.
. Kanafani ZA, Corey GR. Tedizolid (TR-701): a new oxazolidinone with enhanced potency. Expert Opin Investig Drugs. 2012 Apr;21(4):515-22.
INTRODUCTION: Tedizolid phosphate (TR-701) is a new oxazolidinone prodrug that is transformed in the serum into the active drug tedizolid (TR-700). Tedizolid acts by inhibiting protein synthesis and has broad activity against Gram-positive pathogens, including strains that are resistant to linezolid. AREAS COVERED: This review summarizes the currently available data on this new antimicrobial agent. In vitro activity, pharmacokinetics/pharmacodynamics, clinical efficacy and safety are all addressed. EXPERT OPINION: Tedizolid will provide a useful addition to the antimicrobial armamentarium, particularly in complicated skin and skin structure infections, due to its high oral bioavailability and once-daily dosing. The results of future studies will serve to better position tedizolid among the newly approved agents for infections caused by Gram-positive organisms.
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