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New Developments in Drug Treatment
Published in Lloyd N. Friedman, Martin Dedicoat, Peter D. O. Davies, Clinical Tuberculosis, 2020
Alexander S. Pym, Camus Nimmo, James Millard
Delpazolid (LCB01-0371) appears more potent than linezolid for a range of Gram-positive infections72 and thus is an attractive candidate for assessment of its potential to treat TB. It has demonstrated activity against clinical drug-resistant Mycobacterium tuberculosis isolates in vitro, albeit with a 2-fold higher MIC90 than linezolid.73 The drug has now gone forward for testing in an EBA study, interim results of which suggest that the drug is well tolerated, with modest EBA.74–76 Posizolid (AZD5847) appears to have a similar or higher range of Mycobacterium tuberculosis MICs to delpazolid, but improved extra-, and particularly, intra-cellular killing of Mycobacterium tuberculosis compared to linezolid.77,78 In a murine chronic infection model, posizolid activity was intermediate between linezolid and sutezolid.79 However, in a murine model of non-replicating TB, posizolid activity was minimal compared to linezolid and sutezolid,80 This observation, combined with the relatively high MIC and less favorable pharmacokinetics of posizolid compared to sutezolid and linezolid,81 may explain the modest activity, which was inferior to that previously described for linezolid, in a recent EBA study.82 It is unlikely that posizolid will advance further.
News on therapeutic management of MDR-tuberculosis: a literature review
Published in Journal of Chemotherapy, 2018
Lucie Barthod, Jean-Guillaume Lopez, Christophe Curti, Charléric Bornet, Manon Roche, Marc Montana, Patrice Vanelle
The oxazolidinone derivatives are protein synthesis inhibitors that stop the growth and reproduction of bacteria by disrupting the processes resulting in the generation of new proteins. Linezolid is the most established agent in this class but newer oxazolidinones, including sutezolid (PNU-100480) and posizolid (AZD-5847) have also been studied.54