BIO-MD™ Prodrug Technology
Unlike currently approved opioid pill/tablet formulation approaches, the molecular structure of Ensysce Bioscienes’ novel prodrug technology provides a ‘chemical barrier’ to parenteral abuse as well as the extended-release profile. A representative BIO-MD™ opioid prodrug structure is shown here.
The prodrug delivery handle decreases the affinity of the molecule for the opioid receptor, decrease its permeability into the central nervous system, and reducing its opioid effects, until activated. The drug remains intact when it is taken by any non-oral route eliminating its effect when injected, snorted, or smoked. Below is a diagram of the activity receptor.
BIO-MD™ opioids are bioactivated molecular delivery systems. When administered orally, trypsin in the gastrointestinal tract starts the activation and releases the first amino acid portion of the prodrug. The pharmacokinetic profile is controlled by a second reaction providing either an immediate or extended release product. Common methods of tampering, do not release effective amounts of active opioids with our BIO-MD™ products. .
Our BIO-MD™ abuse-resistant opioid prodrug technology is protected by issued and pending patents in the United States and internationally that cover compositions of matter, methods of manufacture, and methods of use. Our patent estate provides broad protection of our proprietary technology, and will protect our morphone-class prodrugs and codone-class prodrugs until at least 2027 and 2030, respectively.
Early-stage clinical trials were conducted with PF329, our proprietary, extended-release prodrug of hydromorphone. In two phase 1 studies, PF329 has demonstrated excellent safety, dose proportionality, and a clinically beneficial extended release profile.
Fisher et al, First-in-Man Evaluation of HM Prodrug, an Abuse-Resistant Prodrug of Hydromorphone, Journal of Pain 2012;13:7
Our proprietary BIO-MD™ prodrug technology is broadly applicable to classes of drugs used in indications other than pain management. Studies conducted in animals confirm the release characteristics of several other medications based upon the BIO-MD™ platform, including extended- and immediate-release versions of dexamphetamine, a drug that is used for the treatment of ADD and ADHD.