ELQ-598, as a prodrug, is converted into the active drug ELQ-596 upon oral administration. ELQ-598 demonstrates potent parasitic growth inhibition capabilities (IC50= 37 nM). ELQ-598 also shows low toxicity towards human cells (IC50= 19 μM). ELQ-598 can be used for research into babesiosis[1].
in vivo
ELQ-598 (10 mg/kg; p.o.; daily DPI 3-7) achieves complete elimination of B. duncaniinfection in C3H mice[1].
ELQ-598 (10 mg/kg; p.o.; daily DPI 3-7) is effective at eliminating B. microtiinfection in mice[1].
ELQ-598 (10 mg/kg; p.o.; daily DPI 3-7) combined with atovaquone (HY-13832) can eliminative of the infection in the C3H/HeJ mice infected with B. duncani and SCID mice model infected with B. microti[1].
Animal Model:
C3H mice genetically prone to B. duncani infection[1]
Dosage:
10mg/kg
Administration:
p.o.; daily DPI 3-7
Result:
Resulted in a complete elimination of the parasites. Mice survived for the duration of the study with no recurrence of parasitemia observed.
Animal Model:
C3H/HeJ mice for B. duncani infection, and SCID mice for B. microti infection[1]
Dosage:
10mg/kg with 10mg/kg atovaquone,
Administration:
p.o.; daily DPI 3-7
Result:
All mice survived without any recurrence of parasitemia.
A potent synergistic or additive effect of the drug combination in eradicating the lethal infection.This combination strategy offers enhanced efficacy compared to the use of either compound alone.
References
[1] Vydyam P, et al. Effectiveness of Two New Endochin-like Quinolones, ELQ-596 and ELQ-650, in Experimental Mouse Models of Human Babesiosis. ACS Infect Dis. 2024 Apr 12;10(4):1405-1413. DOI:10.1021/acsinfecdis.4c00143
