Pharmacokinetics and pharmacodynamics of the novel Nrf2 activator omaveloxolone in primates

Reisman SA, Gahir SS, Lee CY, Proksch JW, Sakamoto M, Ward KW (Reata Pharmaceuticals, Inc., Irving, TX 75063, USA); Drug Des Devel Ther. 2019; 13: 1259–1270.Published online 2019 Apr 17. doi: 10.2147/DDDT.S193889

Overall, the monkey data demonstrate a well-characterized and dose-proportional PK and tissue distribution profile after oral administration of omaveloxolone, which was associated with Nrf2 activation. Further, systemic exposures to omaveloxolone that produce Nrf2 activation in monkeys were readily achievable in Friedreich's ataxia patients after oral administration.

Pharmacokinetics and pharmacodynamics of the novel Nrf2 activator omaveloxolone in primates