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The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468.

Author: BossChristoph, GatfieldJohn, JenckFrancois, MuehlanClemens, RochCatherine, SchindelholzBenno, TreiberAlexander, de KanterRuben, van GervenJoop, von RaumerMarkus

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.

Overview

This study describes the discovery of ACT-541468, a dual orexin receptor antagonist, as a potential new sleep drug. The study utilized physiology-based pharmacokinetic and pharmacodynamic (PBPK-PD) modeling to predict the drug's pharmacokinetic profile in humans and identify an effective dose.
Paper Details　
Original Abstract of the Article :
The identification of new sleep drugs poses particular challenges in drug discovery owing to disease-specific requirements such as rapid onset of action, sleep maintenance throughout major parts of the night, and absence of residual next-day effects. Robust tools to estimate drug levels in human bra...See full text at original site
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引用元：
https://doi.org/10.1124/jpet.117.241596

データ提供：米国国立医学図書館（NLM）

A Tale of Two Receptors: Discovering ACT-541468 as a Dual Orexin Receptor Antagonist

Developing new sleep drugs is a complex endeavor, requiring precise control over drug levels in the brain. This study describes the discovery of ACT-541468, a dual orexin receptor antagonist, using physiology-based pharmacokinetic and pharmacodynamic (PBPK-PD) modeling. The researchers leveraged modeling to predict the drug's activity in humans, ensuring effective targeting of the orexin receptors.

Modeling the Way to Effective Sleep Medications

The study highlights the power of PBPK-PD modeling in drug discovery, enabling researchers to predict drug behavior in humans early in the development process. This approach helps to optimize drug design and identify promising candidates for clinical trials.

A Promising New Approach to Sleep Disorders

This research offers a promising new approach to developing effective sleep medications. By applying PBPK-PD modeling, researchers can accelerate the discovery process and identify drugs with optimal pharmacokinetic profiles for treating sleep disorders.

Dr.Camel's Conclusion

You know, finding the right sleep medication can be like searching for an oasis in the desert – a long and arduous journey. This research shows how PBPK-PD modeling can help us find these oases of restful sleep, providing hope for those struggling with sleep disorders.

Date :
  1. Date Completed 2017-08-30
  2. Date Revised 2021-02-12
Further Info :

Pubmed ID

28663311

DOI: Digital Object Identifier

10.1124/jpet.117.241596

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Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

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