Tetrabenazine is a monoamine-depleting agent primarily used to treat hyperkinetic movement disorders such as Huntington's disease-related chorea. It works by reversibly inhibiting vesicular monoamine transporter type 2 (VMAT2), thereby reducing dopamine storage in nerve terminals and helping control involuntary movements. The drug was first synthesized in the late 1950s and introduced into clinical use in the 1960s in Europe as a treatment for movement disorders and certain psychiatric conditions. Over time, its role became more focused on neurological uses, particularly chorea, due to its targeted mechanism. After decades of use internationally, it gained formal approval in the United States by the U.S. Food and Drug Administration in 2008 specifically for Huntington’s disease-associated chorea, marking an important milestone in its therapeutic history.
