Neurocrine Biosciences Begins Phase 1 Trial of VMAT2 Inhibitor NBI-1140675 in Healthy Adults

7 March 2025
Neurocrine Biosciences, Inc., headquartered in San Diego, has announced the commencement of a Phase 1 clinical trial for its new investigational drug, NBI-1140675. This compound is an oral, selective, second-generation small molecule inhibitor targeting the vesicular monoamine transporter 2 (VMAT2). The goal of this trial is to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of NBI-1140675 in healthy adult participants, with an eye toward its potential use in treating various neurological and neuropsychiatric disorders.

Eiry W. Roberts, M.D., Chief Medical Officer at Neurocrine Biosciences, highlighted the company’s ongoing commitment to developing VMAT2 inhibitors. NBI-1140675 represents a promising addition to Neurocrine’s pipeline, building on the success of valbenazine, which was the first drug approved by the U.S. Food and Drug Administration (FDA) for the treatment of tardive dyskinesia. The company also recently secured FDA approval for valbenazine to treat chorea associated with Huntington's disease. The compound is currently in Phase 3 clinical trials as an adjunctive treatment with antipsychotics for schizophrenia and as a treatment for dyskinetic cerebral palsy. Unlike valbenazine, NBI-1140675 is designed as a highly potent, selective VMAT2 inhibitor, which could offer differentiated therapeutic benefits for patients with neurological and neuropsychiatric conditions.

Neurocrine Biosciences has been at the forefront of neuroscience-focused biopharmaceutical development for over three decades. The company is dedicated to creating treatments that address under-served needs in the domains of neurological, neuroendocrine, and neuropsychiatric disorders. Their diverse portfolio includes FDA-approved therapies for conditions such as tardive dyskinesia, chorea associated with Huntington's disease, classic congenital adrenal hyperplasia, endometriosis, and uterine fibroids. The latter two are being developed in collaboration with AbbVie. In addition, the company maintains a robust pipeline with several compounds in advanced stages of clinical development across their core therapeutic areas.

Neurocrine Biosciences places a strong emphasis on understanding the complex relationships between brain and body systems, leveraging this insight to develop treatments for challenging conditions. Their mission is to create transformative medicines that alleviate the burden of debilitating diseases, driven by a commitment to pioneering bold scientific advances.

NBI-1140675 is one of several VMAT2 inhibitors under evaluation by Neurocrine in Phase 1 clinical studies, alongside NBI-1065890. VMAT2 inhibitors have shown clinical efficacy in treating hyperkinetic movement disorders by modulating presynaptic dopamine storage and release. Neurocrine's continued research and development efforts in this area aim to expand therapeutic options for patients suffering from these challenging conditions, with the hope of offering new and more effective treatments.

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