MAY 06, 2021

Tweaked Version of Ketamine Could Solve the Opioid Crisis

WRITTEN BY: Annie Lennon

Medications that manage post-operative pain are some of the main entry points to opioid addiction and overdose in the US, which kills roughly 50,000 Americans each year. Alternatives for pain management are thus crucial to address this issue. 

Some have looked to ketamine, which was approved by the FDA in 1970 as an anesthetic. The drug has also recently gained popularity as an adjunct to psychotherapy due to its dissociative psychedelic effects at low doses. However, despite its increasing popularity, ketamine’s chemical profile has made using it for post-operative pain extremely difficult, thus limiting its adoption. 

This may soon change, though. Research-stage company Bexson Biomedical has just been granted a patent by the U.S. Patent and Trademark Office (USPTO). Their patent details an innovative ketamine formulation that can be delivered under the skin, or subcutaneously, at low doses via a wearable patch pump, similar to those worn by insulin-dependent diabetics.

Taken together, the formulation and pump are designed to address the key hurdles that have stood in the way of ketamine’s widespread use for managing post-operative pain. These include the drug’s very short half-life and poor oral bioavailability (how much of the drug reaches the bloodstream and thus can be used by the body) as well as the close clinical monitoring needed if given to patients intravenously (IV) at higher doses. 

While the active ingredient in their ketamine formulation is known as ‘racemic ketamine’, the ketamine used in clinics throughout the country, their first version—called BB106—has been tweaked in some critical ways.

They have increased its pH by around two points and tuned its osmolality, a measure of how much dissolved substance is in a liquid, to better suit subcutaneous tissue and thus reduce irritation upon being given to the patient. These changes should in turn increase ketamine’s bioavailability to almost match that of an IV infusion, which is 100% bioavailable. 

Improving the substance’s properties in this way means that pain control can be delivered for up to 24-hours with just a few milliliters of Bexson’s ketamine formulation. The small quantity needed also means that it can easily be delivered to patients via a discrete wearable patch pump. This both gives doctors greater flexibility in pain treatment, and patients better control over their pain. 

“Controlled, low-dose, subcutaneous delivery of ketamine can have several advantages for pain management. These include steady state capability (the ability of the body to regain its original/previous state), improved bioavailability, decreased metabolites and reduced off-target side effects,” wrote Jeffrey Becker, MD, co-founder and Chief Science Officer of Bexson Biomedical in an email correspondence with LabRoots

“This formulation technology may also be applied to a wide variety of other compounds. It can potentially optimize other therapies for subcutaneous delivery that cannot currently be delivered in this manner.”

Currently, Bexson is running preclinical studies needed to engage with the FDA and enable clinical trials for its ketamine formulation and wearable pump. Initially targeting their product to treat post-operative pain, should all go to plan, their first Phase 1 studies for BB106 should begin in the first half of 2022. After a further series of clinical trials, the treatment could be FDA-approved by 2026.


Sources: PR Newswire