(S)-Flurbiprofen-d3 (Esflurbiprofen-d3) is the deuterium labeled (S)-Flurbiprofen. (S)-Flurbiprofen is an active enantiomer of Flurbiprofen, with IC50 values of 0.48 μM and 0.47 μM for COX-1 and COX-2, respectively [1].
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[1].
References:
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. A Carabaza, et al. Stereoselective Inhibition of Inducible Cyclooxygenase by Chiral Nonsteroidal Antiinflammatory Drugs. J Clin Pharmacol. 1996 Jun;36(6):505-12.
[3]. B Averbeck, et al. Inflammatory Mediators Do Not Stimulate CGRP Release if Prostaglandin Synthesis Is Blocked by S(+)-flurbiprofen in Isolated Rat Skin. Inflamm Res. 2003 Dec;52(12):519-23.
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[1].
References:
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. A Carabaza, et al. Stereoselective Inhibition of Inducible Cyclooxygenase by Chiral Nonsteroidal Antiinflammatory Drugs. J Clin Pharmacol. 1996 Jun;36(6):505-12.
[3]. B Averbeck, et al. Inflammatory Mediators Do Not Stimulate CGRP Release if Prostaglandin Synthesis Is Blocked by S(+)-flurbiprofen in Isolated Rat Skin. Inflamm Res. 2003 Dec;52(12):519-23.