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Blake Insomnia Therapeutics inc (OTCMKTS:BKIT) is using beta blockers to reduce stress and make people sleep better

By: | Tags: | Comments: 0 | January 4th, 2017

This company may have tackled one of the most underserved areas of US healthcare with its novel approach

In the mid 1960s, a pharmacologist called James Black synthesized what has now become regarded as the first clinically significant beta blockers, propranolol and pronethalol. Many consider this event to be one of the most important contributions to the medical field of the 20th century, and the drug class has since grown to become one of the most widely prescribed in the developed world. Around 200 million prescriptions for beta blockers are filed every year in the US alone.

It’s big business, but it’s not without its downsides. The drugs have associated with them a host of pretty serious side effects, and these side effects are highly variable person to person. In other words, it’s very difficult for a physician to adequately prepare a patient for the side effects, as they don’t know how the drug might affect the individual. Additionally, there are a number of different types of beta blocker, each of which affects the patient in a slightly different way. The core mechanism of action (MOA) for the class is to reduce blood pressure by blocking the effects of the hormone epinephrine, also known as adrenaline, and in turn, slowing the heart rate. There are other actions, however, that vary depending on the type of blocker used. Some increase triglycerides and a decrease high-density lipoprotein, which can lead to heart attacks. Others can block signs of low blood pressure in diabetic patients, and can mask potential diabetes related complications. Others inhibit the release of melatonin, which translates to a bad nights sleep and resulting fatigue.

Where are we going with this?

Well, the benefit of beta blockers outweighs the side effects, as demonstrated by the hundreds of millions of US prescriptions filed annually. A satellite sector, therefore, has sprung up alongside the beta blocker sector; one that develops and sells treatments that counter the side effects of the drug class. GlaxoSmithKline plc (ADR) (NYSE:GSK), for example, markets Lunesta as a counter to the fatigue associated with a beta blocker regimen. Pain killers are routinely administered to counter the potential for migraines. Never before, however, has a company developed a beta blocker that incorporates both the MOA of a beta blocker, and treats one of the primary side effects, concurrently.

Until now, that is.

Blake Insomnia Therapeutics Inc (OTCMKTS:BKIT) is developing a drug called Zleepax, which is designed to treat stress related insomnia using the MOA that underpins beta blockers and takes advantage of one of the properties of the beta blocker element to improve sleep. Early beta blockers (which are still widely used, and often preferred over later generations) inhibit the nighttime release of melatonin, as mentioned above. A third generation of beta blockers, of which the most commonly prescribed is called Nebivolol, doesn’t inhibit nighttime melatonin. Studies have Nebivolol to have no impact on sleep, and in turn, residual daytime fatigue. Blake Insomnia Therapeutics has taken these studies a step further, and asked this question: what if you took a third generation beta blocker, and gave it to someone who suffers from stress related insomnia? Further, what if you combined the beta blocker with another insomnia drug, to enhance the impact of the major active ingredient (the beta blocker)? The vasodilative property of the beta blocker should reduce stress, which should improve sleep and tackle fatigue. At the same time, there’s no melatonin inhibition.

It is these two questions that underpin Zleepax. Blake Insomnia has filed a patent that covers the use of beta blockers such as Nebivolol—alone or in combination with other anti-insomnia drugs—for the treatment of stress-related insomnia.

What’s next for the company? One of the major advantages of this sort of treatment is that it’s based on ingredients that are Generally Recognized as Safe (GRaS) in the US and Europe. Any drugs based on GRaS compounds (and that don’t introduce a new ingredient) are eligible to skip early stage phase I testing, which a company would normally undertake to demonstrate safety before advancing a drug into a wider patient population. Phase I tests are small, but they can be costly and take time, so the ability to skip this element of the development pathway is a real benefit for Blake Insomnia, and in turn, its shareholders.

So the next step is to take Zleepax into phase II testing. The company plans to undergo a phase II to demonstrate that the drug improves sleep in the target population (i.e. those patients with stress-related insomnia, likely with a control arm taking placebo. There’s already evidence in place that points at clinical benefit, but it’s at the close of a phase II, when a company has top line in hand that compounds earlier evidence, that markets really start to take notice. The phase II, therefore, is an important step for Blake Insomnia in getting this asset to commercialization. Beyond that, US and European pivotals should underpin registration applications to the FDA and the EMA respectively.

What are the risks as a shareholder?

This is development stage biotechnology, so as always, shareholders need to be aware of the impact of any capital raises on their holdings. With the phase I skipped, however, the impact is mitigated somewhat. The company has reported that it is conducting a single digit million dollar raise, and that this round will cover the cost of the phase II entirely. With the data in hand from the phase II, a subsequent raise should be on good terms and easy to conduct. There’s also the potential that the data may not come out as representative of the hypothesis that the early data suggests. In other words, the drug may not work. These are GraS compounds, however and there’s plenty of evidence already in place that points to clinical benefit.

written by Eli Altmann