Deutetrabenazine
生产企业:Teva Pharmaceuticals
Deutetrabenazine is a vesicular monoamine transporter 2 inhibitor used for the symptomatic treatment of tardive dyskinesia and chorea associated with Huntington's disease.
Deutetrabenazine is a vesicular monoamine transporter 2 inhibitor used for the symptomatic treatment of tardive dyskinesia and chorea associated with Huntington's disease.
The precise mechanism of action of deutetrabenazine in mediating its anti-chorea effects is not fully elucidated. Deutetrabenazine reversibly depletes the levels of monoamines, such as dopamine, serotonin, norepinephrine, and histamine, from nerve terminals via its active metabolites. The major circulating metabolites are α-dihydrotetrabenazine [HTBZ] and β-HTBZ that act as reversible inhibitors of VMAT2. Inhibition of VMAT2 results in decreased uptake of monoamines into synaptic terminal and depletion of monoamine stores from nerve terminals . Deutetrabenazine contains the molecule deuterium, which is a naturally-occurring, nontoxic hydrogen isotope but with an increased mass relative to hydrogen . Placed at key positions, deuterium forms a stronger hydrogen bond with carbon that requires more energy for cleavage, thus attenuating CYP2D6-mediated metabolism without having any effect on the therapeutic target .
Deutetrabenazine is indicated in adults patients for the treatment of tardive dyskinesia and for chorea associated with Huntington's disease.
共 2 项相关疾病
每项发明一条,涵盖美国、欧洲、PCT 与中国的同族专利。