Drug intelligence / Profile preview

afabicin

Development stage
Phase 2
Lead developer
Debiopharm
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

Afabicin is a first-in-class, narrow-spectrum antibiotic specifically targeting staphylococcal infections. It is a prodrug that is rapidly converted in vivo to its active form, afabicin desphosphono (formerly known as Debio 1452 or AFN-1252), which acts by inhibiting the enoyl-acyl carrier protein reductase FabI enzyme. This enzyme plays an essential role in the bacterial fatty acid synthesis pathway (FAS-II), which is critical for cell membrane production in staphylococci but distinct from eukaryotic fatty acid synthesis. Afabicin’s selective mechanism results in potent activity against all staphylococcal species, including methicillin-resistant Staphylococcus aureus (MRSA), while sparing most other bacteria and preserving gut microbiota. The drug has both intravenous and oral formulations and has demonstrated efficacy and safety comparable to vancomycin/linezolid for acute bacterial skin and skin structure infections (ABSSSI) due to staphylococci. It is also being developed for bone and joint infections (BJI) caused by staphylococcus[1][3][6][7][8].

Other names
afabicin desphosphono
02

Targets

FabI (Enoyl-acyl carrier protein reductase FabI)InhA

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