Effects of High‐ and Low‐Fat Meals on the Pharmacokinetics of Ozanimod, a Novel Sphingosine‐1‐Phosphate Receptor Modulator

Autor: Jeffrey P. Hartung, Jonathan Q. Tran, Cindy-ann Tompkins, Paul A. Frohna
Jazyk: angličtina
Rok vydání: 2017
Předmět:
Ozanimod
Adult
Male
Adolescent
Drug-Related Side Effects and Adverse Reactions
Hydrochloride
Cmax
Pharmaceutical Science
Administration
Oral
Original Manuscript
Pharmacology
ozanimod
Diet
High-Fat
030226 pharmacology & pharmacy
Sphingosine 1-phosphate Receptor Modulator
03 medical and health sciences
chemistry.chemical_compound
Food-Drug Interactions
Young Adult
0302 clinical medicine
Pharmacokinetics
Medicine
Humans
Pharmacology (medical)
Receptor
Diet
Fat-Restricted
Active metabolite
Meal
Oxadiazoles
Cross-Over Studies
Hepatology
business.industry
food effects
Gastroenterology
clinical trial
Articles
Middle Aged
Crossover study
Confidence interval
Healthy Volunteers
Receptors
Lysosphingolipid
chemistry
Indans
Female
business
bioavailability
pharmacokinetics
030217 neurology & neurosurgery
Zdroj: Clinical Pharmacology in Drug Development
ISSN: 2160-7648
2160-763X
Popis: 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.
Databáze: OpenAIRE
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