Glycoside Prodrugs

Prodrugs can overcome the limitations of existing drugs, enabling a proprietary and highly differentiated product.  Prodrugs are medications or compounds that, after administration, are converted within the body into a pharmacologically active drug, which may already have a long history of clinical investigation and use.  When the reference drug already has independent verification of its safety and efficacy, the prodrug may be approved far more efficiently, while simultaneously being more marketable, due to its ability to eliminate unwanted side effects or undesirable commercial aspects.  As of 2015, there had been approximately 15 prodrugs that have been classified as blockbusters, which is defined as having achieved annual sales that exceeded $1 billion.

Targeted Delivery

Glycoside prodrugs, upon oral delivery, can target the intestinal tract, enabling targeted delivery of cannabinoids to this area for treatment of various gastrointestinal disorders, such as inflammatory bowel disease or narcotic bowel syndrome, a severe form of opiate-induced abdominal pain.  Targeted, or site-specific delivery of cannabinoids could enable potent local therapeutic effects while reducing or avoiding the systemic delivery of THC to the brain. Currently, the psychoactivity of THC limits the dose of cannabinoids that can be used for treatment of pain and inflammation. In addition, independently conducted studies have shown that glycosylated compounds can selectively target the brain and increase bioavailability.

Improved Taste & Tolerability

More water-soluble glycoside prodrugs can dramatically improve the taste and tolerability of oral formulations.  This can help ensure patients comply with physicians’ instructions, and that they do not develop lesions or sores in their mouth due to chronic use of oils or sprays that include high concentrations of harsh organic solvents like ethanol.

Improved Bioavailability

More stable glycoside prodrugs are able to pass through the acidic stomach environment unharmed.  Higher bioavailability may lead to improved therapeutic effects as well as safer and more reliable dosing.

Short Duration of Action

Sustained and delayed systemic release prodrugs could provide long-lasting and overnight relief within a convenient oral drug formulation.

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