Bedaquiline: A Mini Review

Abstract

Tuberculosis is a pandemic, chronic infectious disease which affects more than 10 million people in the world. About 3.5% of patients of newly diagnosed have reported having multidrug-resistant tuberculosis (MDR-TB). The standard treatment of MDR-TB has many cons like high cost, less effectiveness, and more drug interactions. Thus, to overcome these disadvantages a new novel compound which belongs to the diarylquinolone group called bedaquiline has been developed as a part of combination therapy in adults with MDR-TB for its bactericidal activity. It mainly acts by inhibiting the adenosine triphosphate synthase enzyme of Mycobacterium tuberculosis. This drug was introduced as a new addition to the standard TB regimen after 50 years.

Shorter All-oral Bedaquiline-containing MDR-TB Regimen : The Backgrounds & Implementations

“…In mice, the combination of bedaquiline-rifapentine-pyrazinamide produces significant bactericidal activity. [24,25] Bedaquiline (molecular weight 555.50 Da) is an antibiotic compound with a quinolinic central heterocyclic nucleus with alcohol and amine side chains that are responsible for the compound's antimycobacterial activity (Figure 3). Bedaquiline was discovered after a high-throughput evaluation of thousands of compounds using Mycobacterium smegmatis in a whole-cell assay.…”

“…There was a synergistic interaction between pyrazinamide and bedaquiline as pyrazinamide being indirect an inhibitor of ATP synthase. [24][25][26] Figure 3. Molecular Structure of Bedaquiline as the Free Base Form [26] CRJIM…”

“…A systematic and critical analysis of the evidence regarding bedaquiline and MDR-TB was performed by Pontali, et al in 2016. [24,29] The resume of several clinical studies on bedaquiline and the highlighted findings are listed in Table 5.…”

Comparison of pharmacokinetics and bioavailability of bedaquiline fumarate, benzoate and maleate in dogs

“…BDQ was introduced in 2012 as the first addition to the standard TB regimen in 50 years. 1 The standard regimen for MDR-TB has many disadvantages such as high cost, drug interactions and less efficacy. However, addition of BDQ provided satisfactory outcome in this form of TB.…”

“…However, addition of BDQ provided satisfactory outcome in this form of TB. 1 Open access to this molecule is critical for keeping the cost of goods competitive, especially for developing countries where MDR-TB is prevalent. Commercially available tablets contain BDQ as fumarate salt.…”