PBTZ169 (macozinone) – currently in clinical trial phase Ib
PBTZ169 is a highly potent anti-mycobacterial compound that targets the essential enzyme DprE1. Its new, yet well characterized, mode of action makes this molecule a excellent candidate, notably to treat multidrug-resistant tuberculosis.
PBTZ169 has successfully passed preclinical safety and toxicology assessments and two single ascending dose phase I trials, one up to 320 mg performed at the CHUV Service of Clinical Pharmacology centre (NCT03423030) and one up to 640 mg in Russia performed by Nearmedic Plus (NCT03036163).
PBTZ169 successfully passed the first stage of the phase Ia clinical evaluation conducted in Switzerland with a total of 32 healthy volunteers. The objectives of the phase Ia study were to evaluate the safety, tolerability, pharmacokinetics and ex vivo antitubercular activity of PBTZ169 formulations. This study was a mono-centric, prospective, randomized, double-blind, placebo-controlled, single ascending dose study. Volunteers were grouped in 4 panels of 8 subjects, each undergoing 2 investigation periods, during which they received either single doses of PBTZ169 at increasing dose levels or a matching placebo. Safety and pharmacokinetic parameters were evaluated via control of vital signs and serial blood sampling. This study was completed in March 2018 and the promising results and observations encouraged the iM4TB team to prepare a phase Ib, currently being conducted at the CHUV, in Switzerland.
The phase Ib study (NCT03776500) started in March 2019. This trial is a multiple ascending dose study to evaluate the safety, tolerability and pharmacokinetic/pharmacodynamic parameters of PBTZ169 up to a daily dosage of 1200 mg/day in healthy volunteers (32 subjects grouped in 4 consecutive panels) receiving PBTZ169 for 14 consecutive days. Dose escalation will be allowed once the Trial Safety Board has determined that adequate safety and tolerability after each panel completion has been demonstrated to permit proceeding to the next panel. Panels A and B are now completed and the whole study will be finalized by September 2019.
Check more detailed information about our molecule PBTZ169 on https://clinicaltrials.gov/