Bedaquiline fumarateProduct ingredient for Bedaquiline

Bedaquiline is a bactericidal antimycobacterial drug belonging to the class of diarylquinoline. The quinolinic central heterocyclic nucleus with alcohol and amine side chains is responsible for bedaquiline-mediated antimycobacterial activity.⁵ Although it is closely related to fluoroquinolones, bedaquiline does not affect DNA gyrase; instead, bedaquiline inhibits the c subunit of ATP synthase responsible for synthesizing ATP.⁵ Consequently, bedaquiline can be used to treat mycobacterial infection, particularly tuberculosis (TB).⁶ Although the current standard of TB treatment of anti-TB drugs for 2 months, including 2 key drugs isoniazid and rifampin, is highly effective, the emergence of multidrug-resistant TB (MDR-TB) to isoniazid and rifampin has substantially worsened patients outcome.⁴

Bedaquiline was approved by the FDA on December 28, 2012, to treat pulmonary MDR-TB, following favorable results in multiple pre-clinical and clinical studies.^3,4 It is the first drug that was approved in the last 40 years by the FDA for TB unresponsive to current treatments on the market.³ Currently, bedaquiline is the last-line anti-TB drug and must only be used in an appropriate combination regimen.^6,5