Synergistic Effect of Q203 Combined with PBTZ169 against Mycobacterium tuberculosis

Abstract

Q203 is a first-in-class drug candidate against Mycobacterium tuberculosis . In its recently completed phase 2 clinical trial, Q203 reduced the number of live M. tuberculosis cells in a dose-dependent manner.

Propionylpromazine: Unveiling a Novel Inhibitory Agent AgainstMycobacterium tuberculosis

“…Despite this, the need for new, more effective, and simpler treatments is critical. Promising research into new chemical entities and antimicrobial compounds, such as ganfeborole, DprE1 inhibitors, Q203, MmpL3 inhibitors, gwanakosides A, and retinestatin, offers hope for improved management of drug-resistant TB strains (Piton et al, n.d.;Li et al, 2016;Huynh et al, 2022Huynh et al, , 2023Nguyen et al, 2022).…”

“…This underscores the urgent need for the development of new drugs and treatment regimens that are shorter and simpler, to improve TB management. Recently, several new chemical entities and antimicrobial compounds have shown promise against the highly drug-resistant M. tuberculosis, including ganfeborole, DprE1 inhibitors, Q203, MmpL3 inhibitors, gwanakosides A, retinestatin, etc (Piton et al, n.d.;Li et al, 2016;Huynh et al, 2022Huynh et al, , 2023Nguyen et al, 2022).…”

Targeted protein degradation of the CPSF complex by benzoxaboroles through sumoylation

“…Two new compounds recently entered the pipeline for the treatment of African trypanosomiasis; fexinidazole and acoziborole (Solana et al, 2023). Acoziborole is a benzoxaborole (BoB), a class that recently emerged as potent microbicides against a wide spectrum of infections, spanning viral, bacterial, protozoan and fungal agents (Nguyen et al, 2023, Tarleton 2023, Huang et al, 2023. Significantly, BoBs demonstrate activity towards both kinetoplastida and apicomplexan parasites, despite their wide evolutionary divergence.…”

Ceclazepide as novelMycobacterium abscessusinhibitor

“…In recent times, a number of newly developed chemical entities and antimicrobial compounds have emerged, displaying promising activity against the highly drug-resistant pathogen M. abscessus. Some notable examples include ohmyungsamycin, omadacycline, epetraborole, DS86760016, delpazolid, etc (Cho et al, n.d.;Kim et al, n.d.;Aziz et al, 2017;Bich Hanh et al, 2021;Egorova et al, 2021;Ganapathy et al, 2021;Jeon et al, 2022;Fujiwara et al, 2023;Nguyen et al, 2023bNguyen et al, , 2023a). These compounds offer potential avenues for combating the challenges posed by M. abscessus infections.…”

“…Rifabutin has demonstrated remarkable activity against M. abscessus both in vivo and in vitro (Aziz et al, 2017;Nguyen et al, 2023a). This can be attributed to its favorable oral bioavailability, excellent pharmacokinetic properties (including a long half-life and high cellular penetration), and its ability to achieve appropriate concentrations in human lung tissue.…”