The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468 - Treiber, Alexander; de Kanter, Ruben; Roch, Catherine; Gatfield, John; Boss, Christoph; von Raumer, Markus; Schindelholz, Benno; Muehlan, Clemens; van Gerven, Joop; Jenck, Francois (The Journal of pharmacology and experimental therapeutics, 2017)
Keywords: Animals; Brain - drug effects; Brain - physiology; CHO Cells; Cricetinae; Cricetulus; Dogs; Dose-Response Relationship, Drug; Double-Blind Method; Drug Discovery - methods; Humans; Imidazoles - pharmacokinetics; Male; Orexin Receptor Antagonists - pharmacokinetics; Pyrrolidines - pharmacokinetics; Rats; Rats, Wistar; σg; DMSO; PBPK-PD; SB-649868; AUC; ADAM; LC-MS/MS; G418; AUC0-last; OxA; DORA; ACT-605143; ACT-658090; EMG; MK-1064; Cmax; ROt1/2; EEG; OX2; CL; OX1; ACT-541468; CLint; logD; PD; CRC; Kb; Tmax; Vss; PK; REM