生物活性

• 描述Tetrabenazine (TBZ; Xenazine) is a potent, selective, reversible depletor of monoamines from nerve terminals. TBZ inhibits the vesicular monoamine transporter type 2 which, in humans, is expressed nearly exclusively in the brain. TBZ is rapidly metabolized in the liver by carbonyl reductase to stereoisomers of hydrotetrabenazine, some of which are potent inhibitors of vesicular monoamine transporter type 2^[3]. Tetrabenazine, a monoamine depleter and dopamine receptor blocker, is a VMAT-inhibitor used for treatment of hyperkinetic movement disorder^[4]. Tetrabenazine (TBZ) depletes presynaptic dopamine in the CNS. TBZ is most effective in reducing chorea (including Huntington's disease associated chorea), tic associated with Tourette's syndrome and tardive dyskinesias^[5]. TBZ selectively depletes central monoamines by reversibly binding to the type 2 vesicular monoamine transporter. TBZ, at adjusted dosages of up to 100 mg/day, effectively lessens chorea in ambulatory patients with Huntington disease^[6]. Optimized nanoemulsion formulation of a tetrabenazine was robust and its delivery through nasal route is a viable alternative to other routes of administration for treatment of hyperkinesia associated with Huntington's disease^[7].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01734733	Parkinson's Disease	Phase 1 Phase 2	Active, not recruiting	April 29, 2019	New Zealand ... more >> Auckland City Hospital Auckland, New Zealand Collapse <<
  NCT01910480	Effect of Ketoconazole on the ... more >>PK of NBI-98854 in Healthy Subjects Collapse <<	Phase 1	Completed	-	United States, Arizona ... more >> Celerion Tempe, Arizona, United States, 85283 Collapse <<
  NCT02191358	-	-	Completed	-	United States, California ... more >> Dr. Michael Dao Garden Grove, California, United States, 92844 United States, Colorado Kaiser Permanente Colorado Denver, Colorado, United States, 80011 United States, Kentucky Gill Heart Institute Lexington, Kentucky, United States, 40508 United States, Maryland IRC Clinics Towson, Maryland, United States, 21204 United States, Massachusetts Internal Medicine & Cardiology Associates Fall River, Massachusetts, United States, 02720 Prima CARE Fall River, Massachusetts, United States, 02720 United States, Virginia Carilion Clinic Christiansburg, Virginia, United States, 24073 Collapse <<

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• 参考文献

• [1] Kenney C, Hunter C, et al. Long-term tolerability of tetrabenazine in the treatment of hyperkinetic movement disorders. Mov Disord. 2007 Jan 15;22(2):193-7.

  [2] Jankovic J, Beach J. Long-term effects of tetrabenazine in hyperkinetic movement disorders. Neurology. 1997 Feb;48(2):358-62.

  [3] Jankovic J, Clarence-Smith K. Tetrabenazine for the treatment of chorea and other hyperkinetic movement disorders. Expert Rev Neurother. 2011 Nov;11(11):1509-23

  [4] Ondo WG, Hanna PA, Jankovic J. Tetrabenazine treatment for tardive dyskinesia: assessment by randomized videotape protocol. Am J Psychiatry. 1999 Aug;156(8):1279-81

  [5] Fasano A, Bentivoglio AR. Tetrabenazine. Expert Opin Pharmacother. 2009 Dec;10(17):2883-96

  [6] Huntington Study Group. Tetrabenazine as antichorea therapy in Huntington disease: a randomized controlled trial. Neurology. 2006 Feb 14;66(3):366-72

  [7] Arora A, Kumar S, Ali J, Baboota S. Intranasal delivery of tetrabenazine nanoemulsion via olfactory region for better treatment of hyperkinetic movement associated with Huntington's disease: Pharmacokinetic and brain delivery study. Chem Phys Lipids. 2020 Aug;230:104917

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