Moxidectin-d 3 (CL-301423-d 3 ) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk [1] [2] [3] [4].
In Vitro, 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.
References:
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
[2]. Moxidectin, From Wikipedia
[3]. Kiki-Mvouaka S, et al. Role of P-glycoprotein in the disposition of macrocyclic lactones: A comparison between ivermectin, eprinomectin, and moxidectin in mice. Drug Metab Dispos. 2010 Apr;38(4):573-80.
[4]. Perez M, et al. In vitro and in vivo interaction of moxidectin with BCRP/ABCG2. Chem Biol Interact. 2009 Jun 15;180(1):106-12.
In Vitro, 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.
References:
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
[2]. Moxidectin, From Wikipedia
[3]. Kiki-Mvouaka S, et al. Role of P-glycoprotein in the disposition of macrocyclic lactones: A comparison between ivermectin, eprinomectin, and moxidectin in mice. Drug Metab Dispos. 2010 Apr;38(4):573-80.
[4]. Perez M, et al. In vitro and in vivo interaction of moxidectin with BCRP/ABCG2. Chem Biol Interact. 2009 Jun 15;180(1):106-12.