A pilot study of Golexanolone, a new GABA-A receptor modulating steroid antagonist, in patients with covert hepatic encephalopathy

Golexanolone is a novel small molecule GABA-A receptor modulating steroid antagonist under development for treatment of cognitive and vigilance disorders due to allosteric over-activation of GABA-A receptors by neurosteroids. It restored spatial learning and motor coordination in animal models of hepatic encephalopathy (HE) and mitigated the effects of intravenous allopregnanolone in healthy adults in a dose-dependent fashion. Here we report golexanolone safety, pharmacokinetics (PK) and effects on the electroencephalogram (EEG), subjective sleepiness and cognitive performance in adult patients with cirrhosis.

Source: Journal of Hepatology - April 20, 2021 Category: Gastroenterology Authors: Sara Montagnese, Mette Lauridsen, Hendrik Vilstrup, Lisa Zarantonello, Geza Lakner, Sergey Fitilev, Igor Zupanets, Irina Kozlova, Elena Bunkova, Krzysztof Tomasiewicz, Jan Erik Berglund, Fredrik Rorsman, Hannes Hagstr öm, Stergios Kechagias, Carin Edmark Source Type: research