Drug intelligence / Profile preview

LY2444296

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

LY2444296 is a selective, orally bioavailable, high-affinity, and relatively short-acting **kappa opioid receptor antagonist**. It has a Ki value of approximately 1 nM for the kappa opioid receptor (KOPR)[7][9]. The compound has shown promise in preclinical studies for reducing alcohol consumption and withdrawal symptoms in alcohol-dependent rodents[2][3][4][5][8], as well as attenuating escalated cocaine intake and associated negative affective states in animal models of cocaine self-administration and withdrawal[1][6]. It does not induce observable behavioral effects in non-dependent animals, suggesting a favorable safety profile in terms of acute pharmacological effects[2][3][5]. Research interest focuses on its potential for treating substance use disorders, particularly alcohol use disorder and cocaine addiction, by counteracting the negative emotional states and stress responses that promote relapse.

Other names
LY2444296LY-2444296LY 2444296FP3FBZFP-3FBZFP 3FBZ
02

Targets

KOR (Kappa opioid receptor)

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