Drug intelligence / Profile preview

O2P

Development stage
Preclinical
Lead developer
Elysium Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

O2P (Oral Overdose Protection) is a protease-activated prodrug of an opioid antagonist, such as naloxone, being developed by Elysium Therapeutics. It is designed to be co-formulated with prescription opioids to serve as a safety mechanism against oral overdose. The drug utilizes Elysium's Synthetic Enzyme-Activated Prodrug (SEAP) technology, which relies on the digestive enzyme trypsin to cleave the prodrug and release the active antagonist. In a standard therapeutic dose, the amount of antagonist released is negligible and does not interfere with the opioid's analgesic properties. However, in the event of an oral overdose, the increased quantity of the prodrug leads to the release of sufficient antagonist to block opioid receptors, thereby preventing respiratory depression and death. This mechanism is specifically designed to protect against oral ingestion and is not intended to interfere with the intended therapeutic use of the opioid.

Other names
Oral Overdose Protection
02

Targets

KOR (Kappa opioid receptor)PRSS1 (Trypsin family)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)

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