Drug intelligence / Profile preview

GSK598809 + ethanol

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

GSK598809 + ethanol refers to the simultaneous administration of GSK598809, a potent and selective dopamine D3 receptor antagonist, and ethanol (alcohol). GSK598809 is under investigation as a novel treatment for substance dependence disorders, including alcoholism and other addictions. It works by blocking dopamine D3 receptors, which are implicated in the reinforcing effects of addictive substances. Studies have investigated the safety, tolerability, pharmacokinetic interactions, and CNS effects of co-administering GSK598809 (typically 175 mg oral dose) with ethanol (administered intravenously at a target blood concentration of 0.6 g/L) in healthy volunteers. The combination is generally well tolerated in healthy subjects, with effects of the two drugs mainly additive and no significant synergistic safety concerns[1][3]. Key side effects of GSK598809 include headache, dizziness, somnolence, and elevated prolactin. Ethanol can potentiate the CNS effects, but the pharmacokinetic interaction is relatively minor. The interaction is primarily studied to assess use in populations with substance use disorders (notably alcohol use disorder)[1][3][5][9].

02

Targets

DRD3 (Dopamine receptor D3)GABRR (GABA-A receptor subunit rho)

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