Medicinal Chemistry Reviews

Volume 50, Chapter 16
Case History:  Belsomra® (Suvorexant), a First-in-class Dual Orexin Receptor Antagonist for the Treatment of Insomnia
Christopher D. Cox, John J. Renger, Paul J. Coleman, and Christopher J. Winrow

1.    Introduction                                                                                                                419

2.   Genetic and Pharmacological Validation of the Orexin System                            420

3.   Medicinal Chemistry Efforts Leading to Discovery of Belsomra®                         421

      3.1        Identification and Characterization of the Diazepan Series                       422

      3.2       Understanding the Bioactive Conformation                                               424

      3.3       Optimization Efforts Leading to the Discovery of Belsomra®                   426

4.   Pharmacological Characterization of Belsomra®                                                    427

5.   Clinical Data on Belsomra®                                                                                       428

6.         Conclusions               429

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