Drug intelligence / Profile preview

R-ABS01-113

Development stage
Preclinical
Lead developer
Johns Hopkins Drug Discovery
Modality
Small Molecules
Administration
Oral
01

Overview

R-ABS01-113 is a small molecule dopamine D3 receptor (D3R) antagonist developed for the treatment of opioid use disorder (OUD). It is the (R)-enantiomer of the racemic compound (±)-ABS01-113 and a structural analog of the D3R partial agonist VK4-40, featuring a fluorine substitution at the 3-position of the linking chain. Developed by researchers at the National Institute on Drug Abuse (NIDA) and Johns Hopkins Drug Discovery, R-ABS01-113 exhibits high binding affinity (Ki = 0.37 nM) and selectivity for D3R over D2R. Preclinical studies in rodent models have demonstrated its ability to reduce heroin self-administration and cue-induced reinstatement of drug-seeking behavior. The compound is characterized by excellent oral bioavailability and significant blood-brain barrier penetration.

02

Targets

DRD3 (Dopamine receptor D3)

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