Current Phase II investigational therapies for insomnia.

Abstract

INTRODUCTION:

Insomnia is typified by a difficulty in sleep initiation, maintenance and/or quality (non-restorative sleep) resulting in significant daytime distress.

AREAS COVERED:

This review summarizes the available efficacy and safety data for drugs currently in the pipeline for treating insomnia. Specifically, the authors performed MEDLINE and internet searches using the keywords 'Phase II' and 'insomnia'. The drugs covered target GABAA (zaleplon-CR, lorediplon, EVT-201), orexin (filorexant, MIN-202), histamine-H1 (LY2624803), serotonin 5-HT2A (ITI-007), melatonin/serotonin5-HT1A (piromelatine) and melatonin (indication expansions of prolonged-release melatonin and tasimelteon for pediatric sleep and circadian rhythm disorders) receptors.

EXPERT OPINION:

Low-priced generic environments and high development costs limit the further development of drugs that treat insomnia. However, the bidirectional link between sleep and certain comorbidities may encourage development of specific drugs for comorbid insomnia. New insomnia therapies will most likely move away from GABAAR receptors' modulation to more subtle neurological pathways that regulate the sleep-wake cycle.

• Authors: Nava Zisapel
• Journal: Expert opinion on investigational drugs (Expert Opin Investig Drugs) Vol. 24 Issue 3 Pg. 401-11 (Mar 2015) ISSN: 1744-7658 [Electronic] England
• PMID: 25423562 (Publication Type: Journal Article, Review)

Chemical References

• Drugs, Investigational
• GABA Modulators
• Hypnotics and Sedatives
• Receptors, GABA-A

Topics

• Clinical Trials, Phase II as Topic
• Drug Design
• Drugs, Investigational (adverse effects, pharmacology, therapeutic use)
• GABA Modulators (adverse effects, pharmacology, therapeutic use)
• Humans
• Hypnotics and Sedatives (adverse effects, pharmacology, therapeutic use)
• Receptors, GABA-A (drug effects, metabolism)
• Sleep Initiation and Maintenance Disorders (drug therapy, physiopathology)