Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Marjoleen J.M.A. Nijsen"'
Autor:
Erica L. Bradshaw, Mary E. Spilker, Richard Zang, Loveleena Bansal, Handan He, Rhys D.O. Jones, Kha Le, Mark Penney, Edgar Schuck, Brian Topp, Alice Tsai, Christine Xu, Marjoleen J.M.A. Nijsen, Jason R. Chan
Publikováno v:
CPT: Pharmacometrics & Systems Pharmacology, Vol 8, Iss 11, Pp 777-791 (2019)
Abstract Quantitative systems pharmacology (QSP) approaches have been increasingly applied in the pharmaceutical since the landmark white paper published in 2011 by a National Institutes of Health working group brought attention to the discipline. In
Externí odkaz:
https://doaj.org/article/cfab4d71279e43a58805b6626dcdac0c
Autor:
Volker Fischer, Xiaomei Zhang, Colin Phipps, Marjoleen J.M.A Nijsen, Lance Heinle, Gary J. Jenkins, J. Cory Kalvass, Patricia Stuart
Publikováno v:
Drug Metabolism and Disposition. 46:458-469
A flux dialysis method to measure unbound fraction (fu) of compounds with high protein binding and other challenging properties was tested and validated. This method is based on the principle that the initial flux rate of a compound through a size-ex
Autor:
Majid Vakilynejad, Arijit Chakravarty, Tonika Bohnert, Anu Shilpa Krishnatry, Jerome T. Mettetal, Tristan S. Maurer, Christopher R. Gibson, Daniel R. Mudra, Edgar Schuck, Yaming Su, Marjoleen J.M.A Nijsen, Tycho Heimbach, Shining Wang, Virna J A Schuck, Cheng-Pang Hsu, Harvey Wong, Patrick Trapa, Joseph Raybon, Patricia Schroeder, Satyendra Suryawanshi, Jing Lin, Bianca M. Liederer, Valeriu Damian-Iordache, Alice Tsai
Publikováno v:
The AAPS Journal. 17:462-473
The application of modeling and simulation techniques is increasingly common in preclinical stages of the drug discovery and development process. A survey focusing on preclinical pharmacokinetic/pharmacodynamics (PK/PD) analysis was conducted across
Autor:
Bianca M. Liederer, Edgar Schuck, Daniel R. Mudra, Jing Lin, Patricia Schroeder, Fan Wu, Harvey Wong, Cheng-Pang Hsu, Anu Shilpa Krishnatry, Haiqing Wang, Jerome T. Mettetal, Tonika Bohnert, Christopher R. Gibson, Alice Tsai, Marjoleen J.M.A Nijsen, Qiang Lu, Valeriu Damian-Iordache, Satyendra Suryawanshi, Patrick Trapa
Publikováno v:
Drug discovery today. 22(10)
With inadequate efficacy being the primary cause for the attrition of drug candidates in clinical development, the need to better predict clinical efficacy earlier in the drug development process has increased in importance in the pharmaceutical indu
Autor:
Marjoleen J.M.A Nijsen, Theo Meert, Michel Surkyn, Harrie J.M. Gijsen, Bie Verbist, Guy Rosalia Eugeen Van Lommen, Jeroen Aerssens, Jean Pierre Frans Van Wauwe, Michel Anna Jozef De Cleyn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:547-552
In a previous communication, the SAR of a series of potent and selective 5-sulfonyl-benzimidazole CB2-receptor agonists was described. The lack of in vivo activity of compounds from this series was attributed to their poor solubility and metabolic st
Autor:
Luca A. Fenu, Eva Hoeben, Achiel Van Peer, Ron Gilissen, Karin Vaarties, Stefan De Buck, Wendy Sanderson, Marjoleen J.M.A Nijsen, Johan W. Smit, Kelly Van Uytsel, Vikash K. Sinha, Claire Mackie
Publikováno v:
Clinical Pharmacokinetics. 50:307-318
Background: It is imperative that new drugs demonstrate adequate pharmacokinetic properties, allowing an optimal safety margin and convenient dosing regimens in clinical practice, which then lead to better patient compliance. Such pharmacokinetic pro
Autor:
Michel A.J. De Cleyn, Harrie J.M. Gijsen, Marjoleen J.M.A Nijsen, Erwin Fraiponts, Michel Surkyn, Bie M.P. Verbist, Jeroen Aerssens
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2574-2579
A novel series of benzimidazole CB2-receptor agonists was synthesized and the structure-activity relationship explored. The results showed agonistic activities with an EC(50) up to 0.5 nM and excellent selectivity (>4000-fold) over the CB1 receptor.
Autor:
Vikash K. Sinha, Ron Gilissen, Stefan S De Buck, Luca A. Fenu, Claire Mackie, Marjoleen J.M.A Nijsen
Publikováno v:
Drug Metabolism and Disposition. 35:649-659
The aim of this study was to assess a physiologically based modeling approach for predicting drug metabolism, tissue distribution, and bioavailability in rat for a structurally diverse set of neutral and moderate-to-strong basic compounds (n = 50). H
Autor:
Marjoleen J.M.A Nijsen, Petra Gysemberg, Philip Timmerman, Marc Haseldonckx, Koen Wuyts, Claire Mackie, Iris Verhoeven, Saskia Blokland
Publikováno v:
Journal of Pharmacological and Toxicological Methods. 52:293-301
Introduction: There is a continuing need for increased throughput in the examination of new chemical entities (NCEs) in terms of the pharmacokinetic (PK) parameters. The aim was to validate a new study method designed to improve throughput and reduce
Publikováno v:
Neurogastroenterology and Motility. 17:423-432
Both anti- and pro-nociceptive effects of corticotropin-releasing factor (CRF) treatment on visceral pain have been reported. Here, this dual action of CRF was differentiated by selective (in)activation of the CRF1 and CRF2 receptor prior to a viscer