Literature DB >> 32096020

Lemborexant: First Approval.

Lesley J Scott1.   

Abstract

Lemborexant (DAYVIGO™) is an orally administered, dual orexin receptor (OXR) antagonist that exhibits reversible competitive antagonism at OXR1 and OXR2 (> affinity at OXR2) that was discovered and developed by Eisai Inc. for the treatment of adult patients with insomnia. In December 2019, lemborexant received its first approval (with final interim scheduling) in the USA for the treatment of adult patients with insomnia, characterized by difficulties with sleep onset and/or sleep maintenance. In January 2020, lemborexant also received approval in Japan for the treatment of insomnia. It is also being investigated for the treatment of irregular sleep-wake rhythm disorder (ISWRD) associated with mild to moderate Alzheimer's disease. This article summarizes the milestones in the development of lemborexant leading to its first global approval.

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Year:  2020        PMID： 32096020     DOI： 10.1007/s40265-020-01276-1

Source DB:  PubMed          Journal:  Drugs        ISSN： 0012-6667            Impact factor:   9.546


  10 in total

1.  Structure-based development of a subtype-selective orexin 1 receptor antagonist.

Authors:  Jan Hellmann; Matthäus Drabek; Jie Yin; Jakub Gunera; Theresa Pröll; Frank Kraus; Christopher J Langmead; Harald Hübner; Dorothee Weikert; Peter Kolb; Daniel M Rosenbaum; Peter Gmeiner
Journal:  Proc Natl Acad Sci U S A       Date:  2020-07-15       Impact factor: 11.205

2.  Physiologically-based pharmacokinetic modeling to predict drug interactions of lemborexant with CYP3A inhibitors.

Authors:  Takashi Ueno; Yukiko Miyajima; Ishani Landry; Bojan Lalovic; Edgar Schuck
Journal:  CPT Pharmacometrics Syst Pharmacol       Date:  2021-05-01

3.  Population Pharmacokinetics and Exposure-Response Analyses for the Most Frequent Adverse Events Following Treatment With Lemborexant, an Orexin Receptor Antagonist, in Subjects With Insomnia Disorder.

Authors:  Bojan Lalovic; Oneeb Majid; Jagadeesh Aluri; Ishani Landry; Margaret Moline; Ziad Hussein
Journal:  J Clin Pharmacol       Date:  2020-07-14       Impact factor: 3.126

Review 4.  New approaches to symptomatic treatments for Alzheimer's disease.

Authors:  Jeffrey Cummings
Journal:  Mol Neurodegener       Date:  2021-01-13       Impact factor: 14.195

5.  Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation.

Authors:  Chuan Hong; Noel J Byrne; Beata Zamlynny; Srivanya Tummala; Li Xiao; Jennifer M Shipman; Andrea T Partridge; Christina Minnick; Michael J Breslin; Michael T Rudd; Shawn J Stachel; Vanessa L Rada; Jeffrey C Kern; Kira A Armacost; Scott A Hollingsworth; Julie A O'Brien; Dawn L Hall; Terrence P McDonald; Corey Strickland; Alexei Brooun; Stephen M Soisson; Kaspar Hollenstein
Journal:  Nat Commun       Date:  2021-02-05       Impact factor: 14.919

Review 6.  G protein-coupled receptors: structure- and function-based drug discovery.

Authors:  Dehua Yang; Qingtong Zhou; Viktorija Labroska; Shanshan Qin; Sanaz Darbalaei; Yiran Wu; Elita Yuliantie; Linshan Xie; Houchao Tao; Jianjun Cheng; Qing Liu; Suwen Zhao; Wenqing Shui; Yi Jiang; Ming-Wei Wang
Journal:  Signal Transduct Target Ther       Date:  2021-01-08

7.  FLUID study: study protocol for an open-label, single-centre pilot study to investigate the efFect of Lemborexant on sleep management in Japanese sUbjects aged 50 years and older with Insomnia Disorder.

Authors:  Ippei Okada; Kunihiro Iwamoto; Seiko Miyata; Akihiro Fujimoto; Masaki Tanaka; Manabu Amano; Nao Matsuyama; Toshiaki Taoka; Shinji Naganawa; Norio Ozaki
Journal:  BMJ Open       Date:  2021-11-26       Impact factor: 2.692

Review 8.  Orexins: A promising target to digestive cancers, inflammation, obesity and metabolism dysfunctions.

Authors:  Alain Couvineau; Thierry Voisin; Pascal Nicole; Valerie Gratio; Anne Blais
Journal:  World J Gastroenterol       Date:  2021-11-28       Impact factor: 5.742

Review 9.  The Orexin receptors: Structural and anti-tumoral properties.

Authors:  Alain Couvineau; Pascal Nicole; Valérie Gratio; Thierry Voisin
Journal:  Front Endocrinol (Lausanne)       Date:  2022-07-28       Impact factor: 6.055

Review 10.  Selecting a pharmacotherapy regimen for patients with chronic insomnia.

Authors:  Amanda B Hassinger; Nikolas Bletnisky; Rizwan Dudekula; Ali A El-Solh
Journal:  Expert Opin Pharmacother       Date:  2020-03-23       Impact factor: 3.889
  10 in total

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