Us2.ai receives FDA clearance for Us2.v2,transforming…

SAN DIEGO, Feb. 29, 2012 /PRNewswire/ -- BrainCells Inc., a leading biotechnology company developing novel compounds for the treatment of central nervous system (CNS) diseases, announced today that the Phase 1 single ascending dose (SAD) study of BCI-838 has been successfully completed and that the company has initiated the Phase 1 multiple ascending dose (MAD) study. The SAD study evaluated BCI-838 for safety, tolerability, pharmacokinetics and food effect in healthy male subjects.  Single oral doses of BCI-838 up to 900 mg were administered and the drug was well tolerated.  No serious adverse events were reported and all adverse events were mild in intensity, transient, and resolved without sequelae.

"BCI-838's biological activity mimics that of ketamine, an intravenous anesthetic, which has been shown to be efficacious in treating patients with TRD.   Since ketamine is associated with a number of unwanted side effects such as short-term dissociation and psychosis, safer compounds that act in a similar fashion promise to revolutionize the way the disease is managed for these patients," said Robert Williamson, Chief Executive Officer.

BCI-632 increases synaptic glutamate by inhibiting the mGlu2/3 auto-receptor, which is located predominantly at the pre-synaptic site.  As in the case of ketamine, the long-lasting efficacy of BCI-632 can be blocked by either inhibition of AMPA receptors, mTOR or the BDNF signaling pathway. In contrast to ketamine, BCI-632 does not cause psychosis or dissociative effects. In addition, BCI-632 also stimulates serotonin release and, after chronic dosing, hippocampal neurogenesis.

"BCI-838 is an oral prodrug for the active compound BCI-632 that is an mGluR2/3 antagonist," said John Hutchinson, Ph.D. Senior Vice President of Research.  "BCI-632 has been shown to work acutely in a range of animal models of depression, anxiety, cognition and Alzheimer's disease."