Ozanimod (RPC1063) is an oral selective modulator of the sphingosine-1-phosphate 
1 and 5 receptors under development for the treatment of relapsing multiple 
sclerosis and inflammatory bowel disease. The effects of high-fat and low-fat 
meals on the pharmacokinetics (PK) of a single oral dose of ozanimod were 
evaluated in 24 healthy volunteers in a randomized, open-label crossover trial. 
Each subject received a 1-mg dose of ozanimod hydrochloride under 3 meal 
conditions (fasted, high-fat, and low-fat), each separated by 7 days. Mean 
plasma concentration-time profiles for ozanimod and its active metabolites 
(RP101988 [major], RP101075 [minor]) were similar under all 3 conditions. 
Moreover, all PK parameters for ozanimod, RP101988, and RP101075 were similar 
under the 3 meal conditions. The 90% confidence intervals (CIs) for the ratios 
of geometric least-squares mean (fed/fasted) were within the equivalence limits 
of 0.80 to 1.25 for area under the concentration-time curve from time 0 to 
infinity (AUC0-∞ ) and maximum plasma concentration (Cmax ) for ozanimod, 
RP101988, and RP101075, except for the high-fat effect on RP101075 Cmax (90%CI, 
0.76-0.88). Given this lack of a food effect on the exposure of ozanimod and its 
active metabolites, ozanimod can be taken without regard to meals.