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. 2021 Jul 14;26(14):4280. doi: 10.3390/molecules26144280

Table 1.

The main representative oxazolidine antibiotics licensed or under development.

Drug Name Features Ref.
Sutezolid (NU-100480)Pfizer Phase II of clinical trials was completed. The results showed that the drug was well tolerated and safe. [28,29]
Contezolid (MRX-1) Phase III of clinical trials was completed in China. It is awaiting approval for the oral treatment of ABSSSI caused by GPB. [30]
Radezolid (RX-1741) Phase III clinical trials for the treatment of multidrug-resistant infections, including infections caused by LNZ-resistant strains. It is 11-times more active in comparison to LNZ. Currently, its safety profile has not been established and its advantages over LNZ and TDZ are not clear. [14,31]
Delpazolid (LCB01-0371) Phase I/Phase II of clinical trials are ongoing. The safety profile could be suitable for long-term therapies (i.e., TB).
LegoChem Biosciences entered into a license agreement with RMX Biopharma for the development of Delpazolid in China. In addition, Delpazolid received an FDA orphan drug designation.
[32]
Posizolid (AZD2563/AZD5847) Astrazeneca Phase II clinical trials discontinued. The results are not conclusive since the studies for the treatment of TB were discontinued. [29]
TBI-223 It is under phase I clinical trial (NCT03758612) with the aim to evaluate its safety, tolerability and pharmacokinetics. [28,33,34]
Tedizolid (TZD) formerly Torezolid TZD is approved for the treatment of acute bacterial skin and soft tissue infections by the FDA and EMA. Compared to LNZ, TZD is significantly less expensive. Oral and intravenous formulations are available. Tedizolid phosphate is an orally absorbed phosphate prodrug of TZD. Tedizolid phosphate was the second oxazolidinone drug approved by FDA for the treatment of MRSA skin infections in 2014. [35,36]