MMV390048 is an antimalarial compound belonging to the aminopyridine class for treating malaria. It is efficacious against all Plasmodium life cycle stages, apart from late hypnozoites in the liver.
MMV390048 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Plasmodium falciparum gametocytes (stages I-III and IV-V, luciferase-expressing)
214 nM (I-III), 140 nM (IV-V)
Assess the activity of MMV390048 against different stages of gametocytes, showing faster killing of late-stage gametocytes
Sci Transl Med. 2017 Apr 26;9(387):eaad9735
Babesia gibsoni (Oita strain)
100, 50, 25, 10, 5, 1 μM
96 hours
To evaluate the in vitro anti-Babesia activity of MMV390048, with an IC50 value of 6.9 ± 0.9 μM.
Plasmodium falciparum gametocytes (stages IV and V)
285 nM
Evaluate the effect of MMV390048 on gametocyte viability, showing inhibition of late-stage gametocytes
Sci Transl Med. 2017 Apr 26;9(387):eaad9735
Plasmodium falciparum NF54 strain
28 nM (IC50), 40 nM (IC90)
48 hours
Evaluate the inhibitory activity of MMV390048 against the intraerythrocytic life cycle stages of P. falciparum, showing high efficacy against the NF54 strain
Sci Transl Med. 2017 Apr 26;9(387):eaad9735
MMV390048 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Plasmodium berghei infection model
Oral
1.1 mg/kg (ED90), 0.57 mg/kg (ED50)
Four doses (4, 24, 48, and 72 hours post-infection)
Evaluate the efficacy of MMV390048 in a mouse malaria model, showing high efficacy and complete cure
Sci Transl Med. 2017 Apr 26;9(387):eaad9735
Rat
Embryofetal developmental studies
Oral
2, 6, 20, 40, 60 mg/kg/day
Once daily from GD6 to GD17
Evaluate the embryofetal toxicity of MMV390048 in rats, observed diaphragmatic hernias and cardiovascular malformations
Birth Defects Res. 2022 Jun;114(10):487-498
SCID mice
Babesia microti infection model
Oral
20 mg/kg
64 consecutive days
To evaluate the radical cure effect of MMV390048 on Babesia microti infection, results showed that parasites were cleared after 64 days of continuous treatment.
Front Cell Infect Microbiol. 2022 Nov 14;12:1048962
BALB/c mice and SCID mice
B. microti (Peabody mjr strain) and B. rodhaini (Australia strain) infection models
Oral
20 mg/kg
7 consecutive days, starting at 4 DPI
To evaluate the in vivo anti-Babesia activity of MMV390048 against B. microti and B. rodhaini. Results showed that MMV390048 significantly inhibited parasite growth and prevented anemia development.
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