New therapeutic approaches to identifying molecules for opioid abuse treatment

NIH RePORTER · NIH · R43 · $256,220 · view on reporter.nih.gov ↗

Abstract

Project Summary Collaborations Pharmaceuticals Inc. is a small business focused on developing treatments for difficult to treat diseases. The ongoing overreliance on opioids for chronic pain despite their poor ability to improve function has contributed to a significant and alarming epidemic of opioid overdose deaths and addictions in recent years. Despite the overwhelming addiction crisis, few therapies exist, and with low efficacy. Thus, a critical unmet need is an effective and safe treatment for opioid abuse disorders. Recent research has suggested that psychedelics are also capable of reducing drug-dependence, including opioid abuse, and that serious adverse effects are extremely rare. This drug abuse cessation is linked to the induction of neuritogenesis and increased neuroplasticity, a hallmark of psychedelics. While the psychedelic experience and neuroplasticity induction appear interlinked, several analogs of psychedelics have been proposed which induce neuroplasticity and drug- avoidance while seemingly lacking the psychedelic experience. Although few in number, these analogs have been named “psychoplastogens” and are promising candidates for treatment of opioid drug abuse. The de- coupling of the psychedelic experience and neuroplasticity induction is linked to receptor specificity as psychoplastogens are specific to 5HT2A. Here, we propose to use a combination of generative machine learning models with our extensive experience of supervised machine models to generate new analogs of psychedelics that will have improved 5-HT2A specificity, ADME properties, and are easily synthesizable to rapidly expand the pool of known psychoplastogens, significantly increasing potential therapeutic options for opioid abuse treatment.

Key facts

NIH application ID
10385998
Project number
1R43DA055419-01
Recipient
COLLABORATIONS PHARMACEUTICALS, INC.
Principal Investigator
SEAN EKINS
Activity code
R43
Funding institute
NIH
Fiscal year
2022
Award amount
$256,220
Award type
1
Project period
2022-04-15 → 2024-04-14