Drug intelligence / Profile preview

bedaquiline + pretomanid + linezolid

Development stage
Unknown
Lead developer
TB Alliance
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of **bedaquiline + pretomanid + linezolid** is known as the BPaL regimen, an all-oral, short-course, three-drug combination for the treatment of pulmonary extensively drug-resistant tuberculosis (XDR-TB), pre-XDR-TB, and treatment-intolerant or nonresponsive multidrug-resistant tuberculosis (MDR-TB). The regimen consists of: - **Bedaquiline**: a diarylquinoline that inhibits mycobacterial ATP synthase, disrupting energy metabolism in *Mycobacterium tuberculosis*. - **Pretomanid**: a nitroimidazooxazine antimycobacterial agent that inhibits cell wall mycolic acid biosynthesis and releases reactive nitrogen species under anaerobic conditions. - **Linezolid**: an oxazolidinone antibiotic that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit. This regimen is highly effective, with clinical trials showing cure rates between 84–93% in highly drug-resistant TB populations, but toxicity (notably from linezolid) must be managed. It has been approved by the FDA for use in a limited population of adults with pulmonary XDR-TB or MDR-TB who cannot tolerate or did not respond to previous treatment[1][2][4][5][6][11][13].

Other names
BPaL
02

Targets

InhA60S (Eukaryotic 60S ribosomal subunit)ATP Synthase

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