Kalytera has initiated a novel program for the treatment of acute and chronic pain through the development of a compound that consists of a cannabinoid conjugated with naproxen, a generic, non-steroidal, anti-inflammatory drug that is already approved for treatment of pain. The objective of Kalytera’s new program is to develop a potent, non-psychotropic, oral analgesic for intractable pain that will be safe and well tolerated.
By combining both molecules into a single drug, Kalytera has designed a next generation pain medication that may maximize the activation of the alpha3 glycine receptor pathway for treatment of intractable pain. To our knowledge, no company has introduced into the market an agent specifically targeting this receptor.
The initial route of administration will be oral, Kalytera will also seek to develop an intravenous formulation.
Structure of Naproxen
Potential for Complementary Mechanism of Action
The cannabinoid is designed to trigger the activation of a specialized protein in the spinal cord known as the alpha3 glycine receptor. When activated, the alpha3 glycine receptor may potently block pain signals from being sent to the brain.
Kalytera has engineered its compound to help ensure the alpha3 glycine receptor is activated by a second mechanism. This is achieved by attaching naproxen to the cannabinoid in a manner that allows it to detach in the spinal cord and block the synthesis of the pain-inducing prostaglandin molecule PGE2.
The combination of naproxen with the cannabinoid is crucial because PGE2 is known to shut down the alpha3 glycine receptor pathway.
Potential Advantages of Approach
We believe the cannabinoid/naproxen conjugate has potential to become a next generation pain medication, and, based on the potentially complementary methods of action of the cannabinoid and naproxen, there is reason to believe these molecules may have a synergistic effect in treatment of pain, as well as a superior safety profile compared with opioid analgesics. The promise of this novel compound is that the two active agents, the cannabinoid and naproxen, may provide effective pain reduction, without the risks of addiction or respiratory suppression that exist with opioid analgesics. We have also found a way to make this compound water soluble, which may allow for treatment of acute pain in in-patient settings, such as childbirth, short surgical procedures, and post-operative pain care.
CBD is a non-psychoactive cannabis compound that possesses therapeutic potential across a broad range of diseases and disorders and is being evaluated by Kalytera and other companies for treatment of several diseases and disorders.
Use of cannabinoids in the treatment of pain is supported by data from many studies. According to results of a systemic review of randomized controlled trials published in the Journal of Neuroimmune Pharmacology, cannabinoids have demonstrated significant analgesic effects and were well tolerated.
Current Treatment Methods for Pain
Current treatments for pain mainly include non-steroidal anti-inflammatory drugs (“NSAIDs”), such as naproxen, for mild to moderate pain, and opioids, such as morphine, for moderate to severe and chronic pain. Kalytera believes that its product will be suitable for mild to severe pain, without the risks of respiratory suppression and dependence associated with opioid analgesics.
According to a 2016 report by Transparency Market Research, the global pain management therapeutics market is projected to reach $83 billion by 2024.
Beetlebung Pharma, Ltd.
Patents for this compound have been filed in the U.S. and other jurisdictions, and Kalytera has obtained an exclusive, worldwide license for this compound from Beetlebung Pharma, Ltd., an Israeli-based pharmaceutical discovery company focused on cannabinoid-based therapeutics for the treatment of human disease (“BPL”).