Neurocrine Launches Phase 1 Trial of Novel VMAT2 Inhibitor for Neurological Disorders
• Neurocrine Biosciences initiates Phase 1 clinical study of NBI-1140675, a second-generation VMAT2 inhibitor, evaluating safety and pharmacokinetics in healthy adults.
• The new compound builds on Neurocrine's success with valbenazine, which received FDA approval for tardive dyskinesia in 2017 and Huntington's disease chorea in 2023.
• NBI-1140675 joins NBI-1065890 in Neurocrine's pipeline of next-generation VMAT2 inhibitors, targeting various neurological and neuropsychiatric conditions.
Neurocrine Biosciences has launched a Phase 1 clinical trial to evaluate NBI-1140675, its novel second-generation vesicular monoamine transporter 2 (VMAT2) inhibitor, marking a significant step in expanding its neuroscience portfolio. The study will assess the compound's safety, tolerability, and pharmacokinetic profile in healthy adult participants.
The oral, selective small molecule inhibitor represents Neurocrine's latest advancement in VMAT2 inhibitor development, building upon their established expertise in this therapeutic area. VMAT2 inhibitors have demonstrated clinical efficacy in treating hyperkinetic movement disorders by modulating presynaptic dopamine storage and release.
Dr. Eiry W. Roberts, Chief Medical Officer at Neurocrine Biosciences, emphasized the strategic importance of the program: "We are focused on extending our bench of VMAT2 inhibitors in development, building on our successful discovery and development of valbenazine. 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."
Neurocrine's expertise in VMAT2 inhibition is well-established. The company's first-generation VMAT2 inhibitor, valbenazine, achieved FDA approval in 2017 as the first treatment specifically developed for tardive dyskinesia. The drug subsequently received approval in 2023 for treating chorea associated with Huntington's disease. Currently, valbenazine is undergoing Phase 3 clinical studies for additional indications, including as an adjunctive treatment with antipsychotics for schizophrenia and as a treatment for dyskinetic cerebral palsy.
NBI-1140675 represents part of Neurocrine's broader strategy to develop next-generation VMAT2 inhibitors. The compound joins NBI-1065890, another second-generation VMAT2 inhibitor already in Phase 1 clinical studies, demonstrating the company's commitment to advancing multiple candidates in this therapeutic class.
The development of these new compounds reflects Neurocrine's continued focus on addressing unmet needs in neurological and neuropsychiatric disorders. The company's approach leverages its deep understanding of neuroscience and the interconnections between brain and body systems to develop targeted therapeutics for complex neurological conditions.

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Neurocrine Biosciences (NasdaqGS:NBIX) Begins Phase 1 Study Of New VMAT2 Inhibitor For Neurological Conditions
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Neurocrine Biosciences initiates trial of VMAT2 inhibitor in healthy adults
finance.yahoo.com · Mar 6, 2025
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Neurocrine begins Phase 1 clinical study of NBI-1140675
markets.businessinsider.com · Mar 5, 2025
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Neurocrine Biosciences initiates trial of VMAT2 inhibitor in healthy adults
clinicaltrialsarena.com · Mar 6, 2025