Neurocrine Biosciences, Inc. announced the initiation of a Phase 1 clinical study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of investigational compound NBI-1140675 in healthy adult participants. NBI-1140675 is an investigational, oral, selective second-generation small molecule inhibitor of the vesicular monoamine transporter 2 (VMAT2) in development for the potential treatment of certain neurological and neuropsychiatric conditions.  

"We are focused on extending our bench of VMAT2 inhibitors in development, building on our successful discovery and development of valbenazine for the treatment of tardive dyskinesia and chorea in Huntington's disease," said Eiry W. Roberts, M.D., Chief Medical Officer at Neurocrine Biosciences. "NBI-1140675 is an internally discovered, highly potent, selective VMAT2 inhibitor with the potential to provide differentiated benefit in treating certain neurological and neuropsychiatric conditions."

NBI-1140675 joins NBI-1065890 as a second-generation VMAT2 inhibitor undergoing evaluation by Neurocrine in Phase 1 clinical studies. VMAT2 inhibitors have been clinically validated as effective treatments for hyperkinetic movement disorders, playing an important role in presynaptic dopamine storage and release. Neurocrine successfully developed and received U.S. Food and Drug Administration approval in 2017 for valbenazine, a selective VMAT2 inhibitor, for use as the first drug ever developed for the treatment of tardive dyskinesia. In 2023, the company received FDA approval for valbenazine as a treatment for chorea associated with Huntington's disease. Valbenazine is in Phase 3 clinical studies as an adjunctive treatment with antipsychotics for schizophrenia and as a treatment for dyskinetic cerebral palsy.