Potential role of tedizolid phosphate in the treatment of acute bacterial skin infections
Olatz Urbina,1 Olivia Ferrández,1 Mercè Espona,1 Esther Salas,1 Irene Ferrández,2 Santiago Grau1 1Services of Hospital Pharmacy, Hospital Universitari del Mar, Universitat Autònoma de Barcelona, 2Ciència i Tecnologia dels Aliments, Pharmacy Depa...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Dove Medical Press
2013-04-01
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| Series: | Drug Design, Development and Therapy |
| Online Access: | http://www.dovepress.com/potential-role-of-tedizolid-phosphate-in-the-treatment-of-acute-bacter-a12641 |
| _version_ | 1818365312956891136 |
|---|---|
| author | Urbina O Ferrández O Espona M Salas E Ferrández I Grau S |
| author_facet | Urbina O Ferrández O Espona M Salas E Ferrández I Grau S |
| author_sort | Urbina O |
| collection | DOAJ |
| description | Olatz Urbina,1 Olivia Ferrández,1 Mercè Espona,1 Esther Salas,1 Irene Ferrández,2 Santiago Grau1 1Services of Hospital Pharmacy, Hospital Universitari del Mar, Universitat Autònoma de Barcelona, 2Ciència i Tecnologia dels Aliments, Pharmacy Department, Universitat de Barcelona, Barcelona, Spain Abstract: Tedizolid phosphate (TR-701), a prodrug of tedizolid (TR-700), is a next-generation oxazolidinone that has shown favorable results in the treatment of acute bacterial skin and skin-structure infections in its first Phase III clinical trial. Tedizolid has high bioavailability, penetration, and tissue distribution when administered orally or intravenously. The activity of tedizolid was greater than linezolid against strains of Staphylococcus spp., Streptococcus spp., and Enterococcus spp. in vitro studies, including strains resistant to linezolid and those not susceptible to vancomycin or daptomycin. Its pharmacokinetic characteristics allow for a once-daily administration that leads to a more predictable efficacy and safety profile than those of linezolid. No hematological adverse effects have been reported associated with tedizolid when used at the therapeutic dose of 200 mg in Phase I, II, or III clinical trials of up to 3 weeks of tedizolid administration. Given that the clinical and microbiological efficacy are similar for the 200, 300, and 400 mg doses, the lowest effective dose of 200 mg once daily for 6 days was selected for Phase III studies in acute bacterial skin and skin-structure infections, providing a safe dosing regimen with low potential for development of myelosuppression. Unlike linezolid, tedizolid does not inhibit monoamine oxidase in vivo, therefore interactions with adrenergic, dopaminergic, and serotonergic drugs are not to be expected. In conclusion, tedizolid is a novel antibiotic with potent activity against Gram-positive microorganisms responsible for skin and soft tissue infections, including strains resistant to vancomycin, linezolid, and daptomycin, thus answers a growing therapeutic need. Keywords: oxazolidinone, TR-700, TR-701 FA, tedizolid, skin and soft tissue infections, linezolid resistance |
| first_indexed | 2024-12-13T22:18:16Z |
| format | Article |
| id | doaj.art-6b35176332074e6e835beb44c8ebe591 |
| institution | Directory Open Access Journal |
| issn | 1177-8881 |
| language | English |
| last_indexed | 2024-12-13T22:18:16Z |
| publishDate | 2013-04-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | Drug Design, Development and Therapy |
| spelling | doaj.art-6b35176332074e6e835beb44c8ebe5912022-12-21T23:29:26ZengDove Medical PressDrug Design, Development and Therapy1177-88812013-04-012013default243265Potential role of tedizolid phosphate in the treatment of acute bacterial skin infectionsUrbina OFerrández OEspona MSalas EFerrández IGrau SOlatz Urbina,1 Olivia Ferrández,1 Mercè Espona,1 Esther Salas,1 Irene Ferrández,2 Santiago Grau1 1Services of Hospital Pharmacy, Hospital Universitari del Mar, Universitat Autònoma de Barcelona, 2Ciència i Tecnologia dels Aliments, Pharmacy Department, Universitat de Barcelona, Barcelona, Spain Abstract: Tedizolid phosphate (TR-701), a prodrug of tedizolid (TR-700), is a next-generation oxazolidinone that has shown favorable results in the treatment of acute bacterial skin and skin-structure infections in its first Phase III clinical trial. Tedizolid has high bioavailability, penetration, and tissue distribution when administered orally or intravenously. The activity of tedizolid was greater than linezolid against strains of Staphylococcus spp., Streptococcus spp., and Enterococcus spp. in vitro studies, including strains resistant to linezolid and those not susceptible to vancomycin or daptomycin. Its pharmacokinetic characteristics allow for a once-daily administration that leads to a more predictable efficacy and safety profile than those of linezolid. No hematological adverse effects have been reported associated with tedizolid when used at the therapeutic dose of 200 mg in Phase I, II, or III clinical trials of up to 3 weeks of tedizolid administration. Given that the clinical and microbiological efficacy are similar for the 200, 300, and 400 mg doses, the lowest effective dose of 200 mg once daily for 6 days was selected for Phase III studies in acute bacterial skin and skin-structure infections, providing a safe dosing regimen with low potential for development of myelosuppression. Unlike linezolid, tedizolid does not inhibit monoamine oxidase in vivo, therefore interactions with adrenergic, dopaminergic, and serotonergic drugs are not to be expected. In conclusion, tedizolid is a novel antibiotic with potent activity against Gram-positive microorganisms responsible for skin and soft tissue infections, including strains resistant to vancomycin, linezolid, and daptomycin, thus answers a growing therapeutic need. Keywords: oxazolidinone, TR-700, TR-701 FA, tedizolid, skin and soft tissue infections, linezolid resistancehttp://www.dovepress.com/potential-role-of-tedizolid-phosphate-in-the-treatment-of-acute-bacter-a12641 |
| spellingShingle | Urbina O Ferrández O Espona M Salas E Ferrández I Grau S Potential role of tedizolid phosphate in the treatment of acute bacterial skin infections Drug Design, Development and Therapy |
| title | Potential role of tedizolid phosphate in the treatment of acute bacterial skin infections |
| title_full | Potential role of tedizolid phosphate in the treatment of acute bacterial skin infections |
| title_fullStr | Potential role of tedizolid phosphate in the treatment of acute bacterial skin infections |
| title_full_unstemmed | Potential role of tedizolid phosphate in the treatment of acute bacterial skin infections |
| title_short | Potential role of tedizolid phosphate in the treatment of acute bacterial skin infections |
| title_sort | potential role of tedizolid phosphate in the treatment of acute bacterial skin infections |
| url | http://www.dovepress.com/potential-role-of-tedizolid-phosphate-in-the-treatment-of-acute-bacter-a12641 |
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