Orally Bioavailable Endochin-Like Quinolone Carbonate Ester Prodrug Reduces Toxoplasma gondii Brain Cysts
J. Stone Doggett, Tracey L. Schultz, Alyssa J. Miller, Igor Bruzual, Sovitj Pou, Rolf W. Winter, Rozalia A. Dodean, Lev N. Zakharov, Aaron Nilsen, Michael K. Riscoe, Vern B. Carruthers
Abstract
) and the area under the curve (AUC) of ELQ-316. The increased bioavailability of ELQ-316, when administered as ELQ-334, resulted in efficacy against acute toxoplasmosis greater than that of an equivalent dose of ELQ-316 and had efficacy against latent toxoplasmosis similar to that of ELQ-316 administered intraperitoneally. Treatment with carbonate ester prodrugs is a successful strategy to overcome the limited oral bioavailability of ELQs for the treatment of toxoplasmosis.
Topics & Concepts
Toxoplasma gondiiToxoplasmosisProdrugIn vitroPharmacologyBiologyAdverse effectQuinoloneBioavailabilityPyrimethamineMicrobiologyImmunologyVirologyAntibioticsBiochemistryChloroquineAntibodyMalariaToxoplasma gondii Research StudiesHeme Oxygenase-1 and Carbon MonoxideHerpesvirus Infections and Treatments