Drug intelligence / Profile preview

delamanid + linezolid + levofloxacin + pyrazinamide

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

Overview

A combination regimen of **delamanid**, **linezolid**, **levofloxacin**, and **pyrazinamide** is an investigational all-oral regimen designed for the treatment of **fluoroquinolone-sensitive multidrug-resistant tuberculosis (MDR-TB)**. This fixed set of four small-molecule antibiotics targets Mycobacterium tuberculosis through synergistic inhibition of cell wall synthesis, DNA replication, protein synthesis, and energy metabolism. - **Delamanid** is a nitro-dihydro-imidazooxazole derivative that inhibits mycolic acid synthesis, disrupting cell wall formation in M. tuberculosis. - **Linezolid** is an oxazolidinone antibiotic that inhibits bacterial protein synthesis by binding to the 23S rRNA of the 50S ribosomal subunit. - **Levofloxacin** is a fluoroquinolone that inhibits DNA gyrase and topoisomerase IV, enzymes vital for bacterial DNA replication and repair. - **Pyrazinamide** is a prodrug that disrupts membrane transport and energy production after conversion to pyrazinoic acid in mycobacteria. The regimen offers an injectable-sparing, shorter-duration alternative to traditional MDR-TB therapy and is under clinical investigation for its efficacy and tolerability.

Other names
delamanid + linezolid + levofloxacin + pyrazinamideMDR-END Registry
02

Targets

NeuraminidaseMycobacterial energy metabolism componentsDendrin23S rRNA (23S ribosomal RNA)

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