Drug intelligence / Profile preview

TBAJ-876

Development stage
Phase 1
Lead developer
TB Alliance
Modality
Small Molecules
Administration
Oral
01

Overview

TBAJ-876 is a second-generation diarylquinoline small molecule developed as an antimycobacterial agent for the treatment of tuberculosis (TB), including both drug-sensitive and drug-resistant forms. It is structurally related to bedaquiline but features modifications designed to improve potency against Mycobacterium tuberculosis and reduce cardiac safety risks such as QT interval prolongation. Preclinical and early clinical data indicate that TBAJ-876 has greater antimycobacterial activity than bedaquiline and a potentially better safety profile with reduced risk of hERG channel blockade. The drug acts by inhibiting mycobacterial adenosine triphosphatase (ATP synthase), disrupting energy production in the bacteria. It is being evaluated in combination regimens with pretomanid and linezolid for its potential to shorten TB treatment duration and improve outcomes[1][3][4][8][9].

Brand names
Sorfequiline
Other names
3,5-dialkoxypyridine analogue of bedaquiline3-QUINOLINEETHANOL, 6-BROMO-.ALPHA.-(2,6-DIMETHOXY-4-PYRIDINYL)-.ALPHA.-(2-(DIMETHYLAMINO)ETHYL)-2-METHOXY-.BETA.-(2,3,6-TRIMETHOXY-4-PYRIDINYL)-, (.ALPHA.S,.BETA.R)
02

Targets

AtpE (ATP synthase subunit c of Mycobacterium tuberculosis)AtpC (ATP synthase epsilon subunit)

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