INTRODUCTION
infectious disease killer
SECONDARY, TUBERCULOSIS (TB)
According to recent statistics from the World Health Organization, 1.6 million people died in 2021 from tuberculosis (TB), making it the second leading infectious disease killer after COVID-19 (In pursuit of such novel anti-TB drugs, OPC-167832 was identified in a phenotypic screen that selected for and optimized carbostyril derivatives with anti-TB activity (Based on these favorable results, OPC-167832 proceeded to initial human trials. First, a phase I study in healthy adults was conducted to assess the pharmacokinetic, safety, and tolerability profiles of single ascending doses of OPC-167832, as well as the effects of food on its absorption, distribution, and elimination. This phase I study was followed by a phase I/IIa study, in which adult participants with drug-susceptible pulmonary TB were treated for 14 days with ascending doses of OPC-167832 monotherapy. The latter trial was designed to assess not only the pharmacokinetic, safety, and tolerability profiles of OPC-167832, but also to provide preliminary data on early bactericidal activity (EBA) in a clinical setting. The current report describes outcomes from both trials. In addition, as a secondary objective, this report described the use of a biomarker, lipoarabinomannan (LAM) concentration in sputum as measured by a LAM-enzyme-linked immunosorbent assay (LAM-ELISA) as a guide for dose selection in the EBA trial (