Drug intelligence / Profile preview

Ocinaplon

Development stage
Discontinued
Lead developer
DOV Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Ocinaplon is an investigational anxiolytic drug belonging to the pyrazolopyrimidine class. It was developed as a selective modulator of GABA-A receptors and exhibits a pharmacological profile similar to benzodiazepines but with greater selectivity for anxiolytic effects and reduced sedative or amnestic side effects[1][3][4]. Ocinaplon acts as a positive allosteric modulator at GABA-A receptors, with modest selectivity for subtypes containing the α2 subunit over those containing α1[1][7]. It was evaluated primarily for the treatment of generalized anxiety disorder (GAD), where it demonstrated efficacy in reducing anxiety symptoms without typical benzodiazepine-associated adverse effects such as sedation or dependence[5][6]. However, development was discontinued after cases of liver toxicity were observed during Phase III clinical trials[1][3].

Brand names
ocinaplon
Other names
ocinaplonCL 273547CL273547CL-273547
02

Targets

BZD site (GABA-A receptor benzodiazepine site)GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)

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