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@ARTICLE{Rosenthal:280285,
author = {Rosenthal, Liana S and Farag, Mena and Aziz, N Ahmad and
Bang, Jee},
title = {{V}esicular monoamine transport inhibitors: current uses
and future directions.},
journal = {The lancet},
volume = {406},
number = {10503},
issn = {0140-6736},
address = {London [u.a.]},
publisher = {Elsevier},
reportid = {DZNE-2025-00940},
pages = {650 - 664},
year = {2025},
abstract = {Advancements over the past decade in understanding
vesicular monoamine transporter 2 (VMAT2) inhibitors
highlight their key role in the treatment of movement and
neuropsychiatric disorders. VMAT2 is crucial for packaging
neurotransmitters such as serotonin, dopamine, and
norepinephrine into synaptic vesicles, facilitating their
release and reuptake in synaptic transmission. VMAT2
inhibitors, such as tetrabenazine, deutetrabenazine, and
valbenazine, show therapeutic efficacy in managing
hyperkinetic movement disorders, including Huntington's
disease, tardive dyskinesia, and Tourette's syndrome. These
inhibitors modulate excessive synaptic activity by reducing
neurotransmitter storage and release. Genetic variations,
particularly in the cytochrome P450 enzyme family, influence
VMAT2 inhibitor metabolism, necessitating personalised
dosing to optimise efficacy and minimise adverse events.
Recent studies have provided further structural insights
into VMAT2 inhibition mechanisms, paving the way for the
development of inhibitors with enhanced potency and
selectivity. Leveraging pharmacogenetics for precision
medicine and exploring VMAT2 inhibition in broader
therapeutic contexts could revolutionise treatment
frameworks for neurological and psychiatric conditions.},
subtyp = {Review Article},
keywords = {Humans / Vesicular Monoamine Transport Proteins:
antagonists $\&$ inhibitors / Vesicular Monoamine Transport
Proteins: metabolism / Tetrabenazine: analogs $\&$
derivatives / Tetrabenazine: therapeutic use /
Tetrabenazine: pharmacology / Huntington Disease: drug
therapy / Movement Disorders: drug therapy / Valine: analogs
$\&$ derivatives / Vesicular Monoamine Transport Proteins
(NLM Chemicals) / Tetrabenazine (NLM Chemicals) / SLC18A2
protein, human (NLM Chemicals) / deutetrabenazine (NLM
Chemicals) / valbenazine (NLM Chemicals) / Valine (NLM
Chemicals)},
cin = {AG Aziz},
ddc = {610},
cid = {I:(DE-2719)5000071},
pnm = {354 - Disease Prevention and Healthy Aging (POF4-354)},
pid = {G:(DE-HGF)POF4-354},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:40783291},
doi = {10.1016/S0140-6736(25)01072-4},
url = {https://pub.dzne.de/record/280285},
}