To assess the safety and efficacy of deutetrabenazine (Teva Neuroscience, Inc, Parsippany, NJ), a vesicular monoamine transporter 2 inhibitor, in children and adolescents with TS. Methods: Alternatives for Reducing Tics in TS (ARTISTS) open-label extension (OLE) (NCT03567291) was a 54-week, gl...
Here we report cryo-electron microscopy structures of the human vesicular monoamine transporter VMAT2 in complex with the antichorea drug tetrabenazine, the antihypertensive drug reserpine or the substrate serotonin. Remarkably, the two drugs use completely distinct inhibition mechanisms. Tetrabenazine binds...
Here, we report a 3.1 resolution cryo-electron microscopy (cryo-EM) structure of VMAT2 complexed with tetrabenazine (TBZ), a non-competitive inhibitor used in the treatment of Huntington's chorea. We find TBZ interacts with residues in a central binding site, locking VMAT2 in an oc...
Here we describe cryo-electron microscopy structures of human VMAT2 complexed with serotonin and three clinical drugs at 3.5–2.8 Å, demonstrating the structural basis for transport and inhibition. Reserpine and ketanserin occupy the substrate-binding pocket and lock VMAT2 in cytoplasm-facing and...
(VMAT-2) inhibitor deutetrabenazine for the treatment of Tourette syndrome. A total of 158 children and adolescents were enrolled across 52 sites in 10 countries. Participants were randomized to high-dose deutetrabenazine (up to 48 mg per day, adjusting for weight and cytochrome P450 2D6 status;...
Research results from a study into Luye Pharma’s in-house developed LY03015, a next-generation vesicular monoamine transporter 2 (VMAT2) inhibitor, were recently published in the European Journal of Medicinal Chemistry, an authoritative international journal with a high impact factor, published by ...
Coffey et al1 report the results of Alternatives for Reducing Tics in Tourette syndrome (ARTISTS 2), a phase 3, randomized, double-blind, placebocontrolled, parallel-group, fixed-dose study of the reversible vesicular monoamine transporter 2 (VMAT-2) inhibitor deutetrabenazine for the treatment of...
A new method of treating schizophrenia and schizophrenic emotional disorder is provided by administering a pharmaceutical composition comprising an antipsychotic compound and a VMAT2 inhibitor to a subject in need thereof. The present disclosure shows that combinations of antipsychotics and VMAT2 inhibitors...
a new method of treating the disease of the patient currently receiving antipsychotic drugs and medicinal compositions useful in the treatment of neuropsychiatric disorders such as schizophrenia are provided.More specifically, the methods described herein include administering antipsychotic and VMAT2 inhibitors...
A new method of treating schizophrenia and schizophrenic emotional disorder is provided by administering a pharmaceutical composition comprising an antipsychotic compound and a VMAT2 inhibitor to a subject in need thereof. The present disclosure shows that combinations of antipsychotics and VMAT2 inhibitors...