Karolinska Development’s Umecrine Cognition has initiated patient enrolment in a Phase IIa clinical trial of its drug candidate GR3027 for the treatment of idiopathic hypersomnia, a type of sleep disorder.
GR3027 is a GABAA receptor modulating steroid antagonist (GAMSA) currently being developed to inhibit the activation of GABAA receptor by endogenous neuroactive steroids.
The Phase IIa trial includes an open-label part (Part A) designed to assess the safety, pharmacokinetics and tolerability of a single oral dose of GR3027 in six female subjects.
A prospective, double-blind, randomised, placebo-controlled cross-over Part B will be conducted after the Part A to evaluate the safety, tolerability, exposure and preliminary efficacy of several oral GR3027 doses in 14 male and female patients.
Umecrine Cognition CEO Magnus Doverskog said: "Excessive daytime sleepiness is a major concern from a medical and public health point of view, with a global prevalence of approximately 20%.
“We are excited to start exploring GR3027 in patients with idiopathic hypersomnia, a subset of patients with lifelong chronic sleeping disorders that severely affect their lives."
In addition to sleep disorders, GR3027 is currently being investigated for hepatic encephalopathy.
In experimental models, the GAMSA compound is reported to have restored various neurological impairments such as cognitive and sleep alternations.
GR3027 is reported to enter the CNS and reverse the inhibitory effects caused by the neurosteroid allopregnanolone on brain function in humans, making it a candidate for treating different sleep and cognitive conditions.