Atovaquone (4-chlorophenyl-2,3,5,6-d4)

Atovaquone (4-chlorophenyl-2,3,5,6-d4) is the deuterium labeled Atovaquone. Atovaquone is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and  P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia[1][2].

Research Areas >> Infection

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Nilsen A, et al. Quinolone-3-diarylethers: a new class of antimalarial drug.Sci Transl Med. 2013 Mar 20;5(177):177ra37.

[3]. Schöler N, et al. Atovaquone nanosuspensions show excellent therapeutic effect in a new murine model of reactivated toxoplasmosis.Antimicrob Agents Chemother. 2001 Jun;45(6):1771-9.