VK4-116

VK4-116 is a novel, highly selective dopamine D3 receptor antagonist being developed primarily for the treatment of opioid use disorder (OUD). It acts by blocking dopamine D3 receptors, which are implicated in the brain's reward system and play a central role in drug-seeking behavior and relapse. Preclinical studies have shown that VK4-116 reduces self-administration and reinstatement of oxycodone use without diminishing its pain-relieving effects. Additionally, it has demonstrated efficacy in reversing cognitive deficits associated with chronic cocaine use in animal models. The compound exhibits favorable metabolic stability and safety profiles in vitro, with minimal off-target toxicity at therapeutic concentrations. VK4-116 is currently undergoing Phase 1 clinical trials to assess its safety, tolerability, and pharmacokinetics in healthy volunteers[1][2][3][5][7][8].