Bedaquiline is a member of the diarylquinoline class of drugs and has a unique mechanism of action, targeting the adenosine triphosphate (ATP) synthase enzyme of the TB mycobacteria. ATP-synthase is used in the process by which M.tb generates its energy supply. It is active against both M.tb and the drug-resistant TB bacteria that cause MDR-TB. Laboratory tests and clinical trials have shown it to have strong bactericidal and sterilizing properties.
In 2012, bedaquiline received conditional approved by the US FDA for the treatment of MDR-TB, in addition to the current second-line treatment regimen. Interim guidance for its use has also been issued by the WHO. Bedaquiline is a potential cornerstone of novel TB regimens currently in development with a novel mechanism of action. As such, could have an even greater impact on TB disease through inclusion in a first-line regimen and/or as a component of a simpler, more affordable drug-resistant TB regimen.
Peer Reviewed Publications
- A Study to Evaluate the Efficacy and Safety of TMC207 in Patients With Pulmonary Infection With Multi-drug Resistant Mycobacterium Tuberculosis
- Early Access of TMC207 in Patients With Extensively Drug Resistant or Pre-XDR Pulmonary Tuberculosis
- Evaluation of Early Bactericidal Activity in Pulmonary Tuberculosis With (J-M-Pa-Z)
- Evaluation of Early Bactericidal Activity in Pulmonary Tuberculosis With Clofazimine (C)-TMC207 (J)-PA-824 (Pa)-Pyrazinamide (Z) (NC-003)
- TMC207-TiDP13-C208: Anti-bacterial Activity, Safety, and Tolerability of TMC207 in Patients With Multi-drug Resistant Mycobacterium Tuberculosis (MDR-TB).
- To Evaluate the Safety, Tolerability, and Efficacy of TMC207 as Part of an Individualized Multi-drug Resistant Tuberculosis (MDR-TB) Treatment Regimen in Participants With Sputum Smear-positive Pulmonary MDR-TB
- Evaluation of Early Bactericidal Activity in Pulmonary Tuberculosis
- TMC207-C202: Study to Evaluate Bactericidal Activity of Multiple Oral Doses of TMC207 in Subjects With Sputum-Smear Positive Tuberculosis
- TMC207-TiDP13-C110: Interaction Study With Lopinavir/Ritonavir in Healthy Volunteer
- Safety, Tolerability, and Effect of TMC207 and Efavirenz in Healthy Volunteers
- TMC207-TiDP13-C117: Interaction Study in Human Immunodeficiency Virus-type 1 (HIV-1) Infected Patients With Nevirapine (NVP)
- A Study to Assess the Relative Bioavailability of TMC207 Following Single-Dose Administrations of Two Pediatric Formulations in Healthy Adult Participants
- A Study to Determine the Relative Oral Bioavailability of Single Dose Administration of TMC207, Under Fed and Fasted Conditions in Healthy Participants
- TMC207 +/- Rifabutin/Rifampin
- A Study of TMC207 in Patients With Moderately Impaired Hepatic Function
- TMC207TBC1003 - A Study in Healthy Volunteers Investigating the Effect of Single-dose TMC207 on the QT/QTc Interval Under Fed Conditions