Coeruleus: Perking up the Morning After

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Background

According to a recent report by US health officials, 8.5 million Americans used prescription sleep aids in the last month. However, this is just a fraction of those suffering from some form of sleep disorder which affects approximately 50 to 70 million Americans.

The most common prescription sleep aids (including: Ambien, Lunesta, Sonata) are selective Gamma-aminubutyric acid (GABA) receptor agonists. What this means is that these medications function on receptors in the brain which reduce alertness and impart relaxation. They are indeed targeted specific to a subset of GABA receptors implicated in promoting sleep. This effect is highly effective and useful during the initiation of sleep but when it continues into the morning it can be problematic.

Photo Credit: Jacob Lab @ Univ. Pittsburgh

Photo Credit: Jacob Lab @ Univ. Pittsburgh

Recently, Sleep-aid drugs have become a new focus of the FDA due to concerns that they may impart a hangover effect. New evidence confirms this worry and shows that the effects of sleep-aids can persist well into the next day after use. Effects of these medications can significantly reduce alertness which is especially hazardous during the morning’s commute.

What can be done?

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Since the effects of these drugs are mainly focused on initiating sleep an ideal solution would be a drug that reverses their effects the next morning. One such drug currently on the market for other indications is Flumazenil. Flumazenil functions as a GABA receptor ANTAGONIST meaning it blocks activity at the same receptor that is activated bysleep aids reversing their sedative effect.

The challenge however lies in delivery. All current formulations of Flumazenil have very low oral bioavailability making them effecting only when given intravenously. This challenge in the delivery of this drug impedes its use for those suffering from morning hangovers, who understandably are not likely to be willing to give themselves injections each morning. This is of course until Coeruleus Ltd, an Israeli startup, devised a solution in it’s unique formulation.

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What does Coeruleus do?

Coeruleus’ innovation lies in a platform for sublingual delivery of drugs which currently are solely available in intravenous formats due to insufficient solubility . With their solution they boast an increase in the solubility of flumazenil of over 120 fold.

What makes Coeruleus unique?

Capitalizing on this increase in solubility, they devised a sublingual spray (FLUMUP) that when taken under the tongue can reverse the lingering effects of sleep aids. In doing so , they provide the most convenient solution to a very challenging problem.

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Future applications

Since their proprietary technology platform is focused on increasing solubility it can be applied to other drugs facing similar challenges in sublingual delivery.

My Two Cents

Given the popularity of prescription sleep aids for sleep disorders, there is clear demand for a remedy to the hangover they cause. Currently it satisfies an unmet need in a growing market that was estimated in 2011 to be 637 million dollars monthly packs, i.e. a blockbuster with a forecast sales of more than $1B/year. Since their formulation is created with approved inactive FDA compounds and their strategy to reformulate actively prescribed medications they will face fewer regulatory hurdles.  The company is  currently looking to secure additional funding to push development of their product further through stage II clinical trials. If they continue to optimize the user-friendliness of their product Coeruleus Ltd is a company to keep an eye on.

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