AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1) with an IC50 value of 10 nM.1 It also inhibits PDE6 with an IC50 value of 4 µM.1 AZ 7371 has been shown to be active against M. tuberculosis with an MIC range of 0.78-3.12 µM and demonstrates efficacy in a rodent model of tuberculosis.
August 2021. Publication. Robertson et al. Comparative Analysis of Pharmacodynamics in the C3HeB/FeJ Mouse Tuberculosis Model for DprE1 inhibitors TBA-7371, PBTZ169 and OPC-167832. Antimicrob Agents Chemother August 9; AAC0058321. Advance online publication. https://doi.org/10.1128/AAC.00583-21.
January 16, 2020. Bill & Melinda Gates Medical Research Institute began a Phase 2a, Dose Escalation, Controlled, Randomized Study to Evaluate Safety, Early Bactericidal Activity (EBA) and Pharmacokinetics of TBA-7371 in Adult Patients With Rifampicin-sensitive Pulmonary Tuberculosis NCT04176250
August 2017. The TB Alliance began a Phase 1, Partially-Blind, Placebo Controlled, Randomized, Combined Single Ascending Dose With a Food Effect Cohort and Multiple Ascending Dose and a Drug-Drug Interaction Study to Evaluate the Safety, Tolerability, Pharmacokinetics and the Pharmacokinetic Interaction Between TBA-7371 With Midazolam and Bupropion in Healthy Adult Subjects