APX001

Research use only, not for human use.

APX001 (APX 001A;E1210) is a novel broad-spectrum antifungal agent that inhibits the fungal protein Gwt1.

APX001 (APX 001A;E1210) is a novel broad-spectrum antifungal agent that inhibits the fungal protein Gwt1, demonstrates significantly acitive MIC50 and MIC90 values of 0.004 and 0.031 ug/ml (16 strains of C. auris); inhibits the inositol acylation activity of C. albicans Gwt1p and A. fumigatus Gwt1p with IC50 of 0.3 to 0.6 uM but has no inhibitory activity against human Pig-Wp; shows significant efficacy in murine model of disseminated C. auris infection, and log reduction in CFU counts in kidney, lung, and brain tissue.Fungal Infection Phase 1 Clinical.

Manogepix inhibits the inositol acylation activity of C. albicans Gwt1p and A. fumigatus Gwt1p with IC50s of 0.3 to 0.6 μM but has no inhibitory activity against human Pig-Wp even at concentrations as high as 100 μM. To confirm the inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis, expression of ALS1 protein, a GPI-anchored protein, on the surfaces of C. albicans cells treated with Manogepix is studied and shown to be significantly lower than that on untreated cells. Manogepix inhibits germ tube formation, adherence to polystyrene surfaces, and biofilm formation of C. albicans at concentrations above its MIC.

Manogepix (2.5 mg/kg, 5 mg/kg and 10 mg/kg; oral administration; twice daily; for 3 days; specific-pathogen-free female ICR mice) treatment reduces the number of viable C. albicans cells in the oral cavity in a dose-dependent manner. Animal Model:Specific-pathogen-free female ICR mice (5 weeks; ~25 g) with C. albicans Dosage:2.5 mg/kg, 5 mg/kg and 10 mg/kg Administration:Oral administration; twice daily; for 3 days Result:Reduced the number of viable C. albicans cells in the oral cavity in a dose-dependent manner.

APX 001A | E1210

Microbiology/Virology

Fungal

Fungal

Infection

Fungal Infection

936339-60-5

358.401

C21H18N4O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (279.03 mM)

NC1=NC=CC=C1C2=CC(CC3=CC=C(COC4=NC=CC=C4)C=C3)=NO2

3-(3-{4-[(pyridin-2-yloxy)methyl]benzyl}isoxazol-5-yl)pyridin-2-amine

(-20℃)

With Ice Pack

≥ 2 years