File:Peak-normalized concentrations of orexin receptor antagonists with administration in humans.png

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Summary

Description
English: Peak-normalized concentrations (% of Cmax) of the orexin receptor antagonists suvorexant, lemborexant, daridorexant, and seltorexant with administration in humans. The terminal elimination half-lives were 12 hours, 55 hours, 6 hours, and 2.5 hours, respectively.

Source of the data:

  • (November 2020). "Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders". Expert Opin Drug Metab Toxicol 16 (11): 1063–1078. DOI:10.1080/17425255.2020.1817380. PMID 32901578.

Original sources of the data:

  • Suvorexant: Center for Drug Evaluation and Research, Application Number: 204569Orig1s000, Medical Review(s)[1] (PDF), Food and Drug Administration, 2014
  • Lemborexant: Dayal, S., Aluri, J., Hall, N., Lalovic, B., Filipov, G., Chang, M. K., Murphy, P., Moline, M., & Landry, I. (13 February 2019). "PII-043 Effect of Hepatic Impairment on Pharmacokinetics, Safety, and Tolerability of Lemborexant, an Investigational Dual Orexin Receptor Antagonist Agent". Clinical Pharmacology & Therapeutics 105 (S1): S54–S54. DOI:10.1002/cpt.1344. ISSN 0009-9236.
  • Daridorexant: (November 2018). "Accelerated Development of the Dual Orexin Receptor Antagonist ACT-541468: Integration of a Microtracer in a First-in-Human Study". Clin Pharmacol Ther 104 (5): 1022–1029. DOI:10.1002/cpt.1046. PMID 29446069.
  • Seltorexant: (September 2015). "Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia". J Pharmacol Exp Ther 354 (3): 471–82. DOI:10.1124/jpet.115.225466. PMID 26177655.
Date
Source (November 2020). "Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders". Expert Opin Drug Metab Toxicol 16 (11): 1063–1078. DOI:10.1080/17425255.2020.1817380. PMID 32901578.
Author Muehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J

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Public domain This chart is ineligible for copyright and therefore in the public domain, because it consists entirely of information that is common property and contains no original authorship. For more information, see Commons:Threshold of originality § Charts

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current02:10, 7 April 2022Thumbnail for version as of 02:10, 7 April 20222,077 × 1,213 (284 KB)Vanished user 0x8cSXE0x6Uploaded a work by Muehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J from {{cite journal | vauthors = Muehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J | title = Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders | journal = Expert Opin Drug Metab Toxicol | volume = 16 | issue = 11 | pages = 1063–1078 | date = November 2020 | pmid = 32901578 | doi = 10.1080/17425255.2020.1817380 | url = }} with Uploa...
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