Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections

The clinical management
of prosthetic joint infections and other
persistent bacterial infections represents a major unmet medical need.
The rifamycins are one of the most potent antibiotic classes against
persistent bacterial infections, but bacteria can develop resistance
to rifamycins rapidly and the clinical utility of the rifamycin class
is typically limited to antibiotic combinations to minimize the development
of resistance. To develop a better therapy against persistent bacterial
infections, a series of rifamycin based bifunctional molecules were
designed, synthesized, and evaluated with the goal to identify a dual-acting
drug that maintains the potent activity of rifamycins against persistent
pathogens and at the same time minimize the development of rifamycin
resistance. TNP-2092 was identified as a drug candidate and is currently
in an early stage of clinical development for the treatment of prosthetic
joint infections.