Our colleagues from the Laboratory & Service of Clinical Pharmacology at the CHUV validated an innovative methodology using multiplex UHPLC-MS/MS for the analysis and quantification of PBTZ169, as well as five of its metabolites, in the plasma of the healthy volunteers who participated in the phase Ia clinical study.
This highly precise technique notably enabled the detection of a reduced, dihydrogenated metabolite measured in large quantities in human plasma. It will enable the detailed pharmacokinetic profile of PBTZ169 to be fully understood, and generate new evidence to promote the clinical development of our drug. The description of the method has been published in PLoS ONE, and the full text is available here:
Spaggiari D, Desfontaine V, Cruchon S, et al. Development and validation of a multiplex UHPLC-MS/MS method for the determination of the investigational antibiotic against multi-resistant tuberculosis macozinone (PBTZ169) and five active metabolites in human plasma. PLoS One. 2019;14(5):e0217139. Published 2019 May 31. doi:10.1371/journal.pone.0217139