Comparative Pharmacology
Head-to-head clinical analysis: AUSTEDO XR versus VALBENAZINE TOSYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUSTEDO XR versus VALBENAZINE TOSYLATE.
AUSTEDO XR vs VALBENAZINE TOSYLATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Deuterated tetrabenazine; inhibits vesicular monoamine transporter 2 (VMAT2), reducing dopamine and monoamine uptake into synaptic vesicles, thereby depleting presynaptic dopamine and other monoamines.
Valbenazine is a selective vesicular monoamine transporter 2 (VMAT2) inhibitor. By inhibiting VMAT2, it reduces the uptake of monoamines into synaptic vesicles, thereby decreasing presynaptic dopamine concentrations and mitigating dopaminergic hyperactivity associated with tardive dyskinesia.
Initial: 6 mg orally once daily. Titrate weekly by 6 mg/day increments to a maximum of 48 mg/day. Administer with food.
Initial dose: 6 mg orally twice daily; may increase to 12 mg twice daily based on response.
None Documented
None Documented
Deutetrabenazine: 9-10 hours; major active metabolites (α-HTBZ and β-HTBZ): 7-15 hours; allows twice-daily dosing for immediate-release, but AUSTEDO XR is once-daily.
The terminal elimination half-life of valbenazine is approximately 15–22 hours for the parent drug and 20–25 hours for its active metabolite, (+)-α-dihydrotetrabenazine (dihydrotetrabenazine). The long half-life supports once-daily dosing.
Primarily hepatic metabolism via CYP2D6 and CYP3A4; <5% excreted unchanged in urine; fecal excretion accounts for ~50% of metabolites.
Approximately 73% of the dose is excreted in feces (primarily as parent drug and metabolites) and 20% in urine. The major metabolites are valbenazine glucuronide and its acid metabolite.
Category C
Category C
VMAT2 Inhibitor
VMAT2 Inhibitor