Tedizolid Phosphate: A Comprehensive Review

Authors

  • E. Hepsi Beula
  • S.Gayatri

Keywords:

Acute bacterial skin & skin structure infections, Analytical method development, Clinical trials, Methicillin-resistant Staphylococcus aureus, Oxazolidinone

Abstract

Tedizolid phosphate is a highly effective antimicrobial therapy that is mainly used in the treatment of Acute Bacterial Skin and Skin Structure Infections (ABSSSI), particularly those involving Methicillin-Resistant Staphylococcus Sureus (MRSA) infections. The review systematically reviews its pharmacokinetics, pharmacodynamics, clinical efficacy, safety profile, and analytical techniques. Compared to its ancestor, linezolid, tedizolid has lower toxicity, a longer half-life, and enhanced in vitro activity. Tedizolid is a notable improvement in the therapy for ABSSSIs, thanks to its high oral bioavailability of 91%, once-daily dosing, and efficiency against drug-resistant gram-positive pathogens. Pharmacokinetic trials show that drug exposure is stable among different groups of patients with hepatic or renal impairment. Tedizolid was shown to be noninferior to linezolid by clinical studies like ESTABLISH-1 and ESTABLISH-2, which showed equivalent or superior clinical response rates with lower side effects, especially with respect to hematologic parameters. To determine stability and drug quantification, several analytical techniques like HPLC, UPLC-MS/MS, and TLC were used; out of these, the highest sensitivity and accuracy was seen for UPLC-MS/MS. Tedizolid phosphate was stable against thermal and photolytic stress but was shown to degrade in the presence of oxidative and hydrolytic stress. In summary, tedizolid phosphate is a worthwhile addition to the antimicrobial armamentarium, providing increased safety, efficacy, and dosing convenience. More research would be beneficial to investigate its use in various infectious disease scenarios and in immunocompromised patients.

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Published

2025-06-17

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