We are pleased to highlight this important research led by Prof. Laurent Decosterd and his team at the Lausanne University Hospital (CHUV), recently published in EMBO Molecular Medicine.
The study identifies two human enzymes, PTGR1 and PTGR2, involved in the metabolic pathway of macozinone/PBTZ169, an investigational anti-tuberculosis drug currently in clinical development at iM4TB.
Read the publication here.
“Tuberculosis: a new avenue to improve the effectiveness of treatments
A research team from the Clinical Pharmacology Department of the CHUV has identified a previously unknown human metabolic pathway that partially inactivates macozinone, an anti-tuberculosis drug in clinical development.
Published in the scientific journal EMBO Molecular Medicine, this study was led by Prof. Laurent Decosterd, with Dr. Dr. Myriam Briki as first author and the participation of the Dre. PD – MERc, Eva Choong, within the research team of the Clinical Pharmacology Department of the CHUV.
Carried out largely at the CHUV’s Drug Dosing Laboratory, the work showed that two human enzymes, PTGR1 and PTGR2, transform macozinone into a substance that is less active against the bacteria responsible for tuberculosis.
Scientists have also shown that several compounds, including diclofenac and indomethacin, can slow down this transformation and partially restore the drug’s activity in in vitro experiments.
These results open up an avenue for improving the effectiveness of macozinone against tuberculosis by limiting its inactivation by the PTGR1 and PTGR2 enzymes.”
