Drug intelligence / Profile preview

DHA27

Development stage
Preclinical
Lead developer
College of Pharmacy, Zunyi Medical University
Modality
Small Molecules
Administration
Intravenous
01

Overview

DHA27 is a derivative of artesunate investigated as an antibacterial sensitizer, particularly to restore or enhance the efficacy of aminoglycoside antibiotics such as gentamicin against drug-resistant bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa. DHA27 itself has no direct antibacterial effect at clinically relevant concentrations, but in combination with aminoglycosides, it exerts a synergistic effect by inhibiting the expression of drug resistance mechanisms such as efflux pump genes (notably norA and norC in MRSA) and aminoglycoside-modifying enzyme genes (notably aac(3)-II in P. aeruginosa). This results in increased intracellular accumulation of aminoglycoside antibiotics, restored antibacterial activity, and reduced bacterial load and inflammation in vivo. DHA27 is a synthetic small molecule derived from the antimalarial drug artesunate and has been developed and studied by academic researchers, primarily in China, for its potential to overcome multidrug resistance in serious bacterial infections[1][2][3][5].

Other names
DHA27DHA-27DHA 27
02

Targets

AAC(3)-IIa (Aminoglycoside 3-N-acetyltransferase type IIa)NorC (NorC efflux pump)NorA (NorA efflux pump)

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