Drug intelligence / Profile preview

clarithromycin + ethambutol + clofazimine

Development stage
Unknown
Lead developer
Taisho Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

This is an **oral fixed-dose combination regimen** consisting of three small molecule antibiotics: **clarithromycin** (a macrolide that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit), **ethambutol** (an antimycobacterial agent inhibiting arabinosyl transferases involved in the synthesis of the mycobacterial cell wall), and **clofazimine** (a riminophenazine dye that disrupts mycobacterial respiratory chains and ion transporters). The combination has been primarily studied and used to treat **Mycobacterium avium complex (MAC) pulmonary disease** and disseminated MAC infection, particularly in immunocompromised patients or those intolerant of rifamycins. Clinical and preclinical studies demonstrate that while clarithromycin offers strong bactericidal activity, clofazimine and ethambutol add synergistic or additive antimycobacterial efficacy, and the triple-drug regimen may serve as an alternative when standard rifamycin-containing regimens are unsuitable[2][3][4][5].

02

Targets

bc1 complex (Cytochrome bc1 complex (plasmodium))AftA (Arabinosyltransferase AftA)Bacterial 50S ribosomal subunit

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