| Identification | Back Directory | [Name]
Fanotaprim | [CAS]
2120282-75-7 | [Synonyms]
Fanotaprim
CD-1,Inhibitor,Fanotaprim,mice,VYR 006,DHFR,VYR-006,inhibit,Antifolate,dhydrofolate,reductase,survival,toxoplasmosis,VYR006 | [Molecular Formula]
C19H22N8O | [MDL Number]
MFCD32206950 | [MOL File]
2120282-75-7.mol | [Molecular Weight]
378.44 |
| Hazard Information | Back Directory | [Uses]
Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis[1]. | [in vivo]
Fanotaprim (1-10 mg/kg; p.o.; daily; beginning on day 1 through day 7) shows highly effective in control of acute infection by highly virulent strains of T. gondii in the murine model[1].
Fanotaprim (1mg/kg; i.v; mouse) shows CL, Vd, and t1/2 values of 10.6 mL/min/kg, 1.14 L/kg, and 3.9 hours, respectively[1].
Fanotaprim (0.83 mg/kg; p.o; mouse) shows F, Cmax, Tmax, and AUC0-last of 47.3%, 178 ng/mL, 0.05 hours and 750 ng h/mL, respectively[1]. | Animal Model: | CD-1female mice (murine model of acute toxoplasmosis)[1] | | Dosage: | 1-10 mg/kg | | Administration: | p.o.; daily; beginning on day 1 through day 7 | | Result: | Mice were monitored for survival for 30 days within termittent IVIS monitoring. At doses of 10 mg/kg Fanotaprim, q.d. or b.i.d. for 7 days, yielded 100% survival for 30 days.
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| [References]
[1] Hopper AT, et al. Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis. J Med Chem. 2019;62(3):1562-1576. DOI:10.1021/acs.jmedchem.8b01754 |
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