Please use this identifier to cite or link to this item:
|Title:||Semagacestat pharmacokinetics are not significantly affected by formulation, food, or time of dosing in healthy participants|
De La Peña, A.
|Citation:||Willis, B.A., Zhang, W., Ayan-Oshodi, M., Lowe, S.L., Annes, W.F., Sirois, P.J., Friedrich, S., De La Peña, A. (2012-06). Semagacestat pharmacokinetics are not significantly affected by formulation, food, or time of dosing in healthy participants. Journal of Clinical Pharmacology 52 (6) : 904-913. ScholarBank@NUS Repository. https://doi.org/10.1177/0091270011407195|
|Abstract:||Semagacestat, γ-secretase inhibitor, reduces formation of amyloid beta peptide. Two single-dose (140 mg), openlabel, randomized, 3-period, crossover studies evaluated the effect of formulation, food, and time of dosing on the pharmacokinetics and pharmacodynamics of semagacestat in healthy participants. The first study (n = 14) compared tablet to capsules. For all formulations, the median time to maximum plasma concentration (tmax) was generally 1.0 hour. Plasma elimination was rapid, with a half-life of approximately 2.5 hours. Tablet form II bioavailability (F) relative to capsule was approximately 100% (F = 1.03 [90% confidence interval (CI), 0.96-1.10]). In the second study, participants (n = 27) received semagacestat either fed or fasting in the morning or fasting in the evening. No significant change in exposure (AUC0-8 [area under the concentration-time curve from 0 to infinity] ratio = 1.02, [90% CI, 0.990-1.05]) occurred with food, whereas maximum plasma concentration (Cmax) declined approximately 15%, and median tmax was delayed to 1.5 hours. Time of dosing made no significant difference in AUC0-8, Cmax, or tmax (AUC0-8 ratio 1.01, [90% CI, 0.975-1.04]). No clinically significant safety concerns occurred in either study. Accordingly, semagacestat may be dosed without regard to formulation, food, or time of administration. © 2012 The Author(s).|
|Source Title:||Journal of Clinical Pharmacology|
|Appears in Collections:||Staff Publications|
Show full item record
Files in This Item:
There are no files associated with this item.
checked on Mar 26, 2019
WEB OF SCIENCETM
checked on Mar 26, 2019
checked on Mar 22, 2019
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.