Long Duration, Novel Opioid Medical Countermeasure for Intramuscular Injection

Threats using chemical and biological weapons are ever-evolving and expanding in scope, underscoring the need for preparedness; therefore, the development and procurement of medical countermeasures is a high priority for the US. The high availability of synthetic opioids, such as fentanyl and its derivatives, is a threat to both the civilian and military communities. Currently, long acting opioid antagonists are available; however, none are available in cGMP formulations suitable for intramuscular/IM injection. In the event of exposure of military personnel and/or large numbers of civilians to weaponized opioids, an easily self-administered, long-acting opioid antagonist would be helpful in stabilizing victims in chaotic settings until they can receive medical attention. In this Phase I SBIR, Extend Biosciences proposes to demonstrate the feasibility of developing a long-acting opioid antagonist using its D-VITylation?? technology. Modification of a therapeutic with vitamin D allows binding to a long-lived serum protein, the vitamin D binding protein, which increases the half-life and bioavailability of the therapeutic. Combination of a D-VITylated, long-acting opioid antagonist with an IM autoinjector pen would result in a drug product that could be self-administered with little effort and logistical burden.