Drug intelligence / Profile preview

(+)-α-dihydrotetrabenazine

Development stage
Unknown
Lead developer
Adeptio Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

(+)-α-Dihydrotetrabenazine is a stereochemically defined, small-molecule inhibitor of vesicular monoamine transporter 2 that reduces vesicular packaging and subsequent release of monoamine neurotransmitters, including dopamine. It is the pharmacologically active (+)-α metabolite associated with tetrabenazine and valbenazine, but is a distinct non-deuterated chemical entity from deutetrabenazine. Adeptio Pharmaceuticals is developing the compound as ADE513, including a Phase II program for tardive dyskinesia; the CTIS record for trial 2024-519105-35-00 identifies the study as Phase II and temporarily halted. The FDA has also granted orphan-drug designation to (+)-alpha-dihydrotetrabenazine for Huntington's disease, without orphan approval. ([precision.fda.gov](https://precision.fda.gov/ginas/app/ui/substances/IFRYDMLSGE))

Other names
(+)-α-DHTBZ(+)-DTBZRRR-dihydrotetrabenazine
02

Targets

VMAT2 (Vesicular monoamine transporter 2)

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