Initially known as R207910 and TMC207, bedaquiline (BDQ) is a first-in-class diarylquinoline, and an important oral medication used to treat adults with pulmonary MDR-TB. BDQ was developed by Janssen in 2005 and is now part of the WHO's List of Essential Medicines. It was approved as an orphan drug by the US Food and Drug Administration (FDA) in December 2012 under the accelerated approval program. Sold under the brand name Sirturo ® , BDQ fumarate salt is usually administered as a combination therapy and is mandated to be used only in patients who do not have other treatment options. In August 2019, the FDA approved the BPaL regimen developed by the Global Alliance for TB Drug Development (TB Alliance), which is a 6-month oral treatment regimen composed of bedaquiline (BDQ), pretomanid (Pa), and linezolid (L) for treating extensively drug-resistant tuberculosis (XDR-TB). Alternative XDR-TB treatments require a 20-month treatment course and a combination of at least seven different drugs, which consequently results in an increase in the overall treatment cost, making BPaL a promising option for patients with this need. BDQ possesses a novel mechanism of action via the inhibition of a critical enzyme responsible for adenosine triphosphate (ATP) synthesis. The lack of efficient energy production by the bacteria cells leads to the inhibition of mycobacterial growth and ultimately results in its death. The bulk of the previously available anti-TB drugs acts by inhibiting the synthesis of the cell wall or affecting the bacteria's genetic material replication and transcription process. In this sense, when compared to the alternatives in the market, the discovery of BDQ is considered a breakthrough for TB treatment, breaking the hiatus of 40 years without the development of a new TB drug targeting a different point of the M. tuberculosis lifecycle.