Valbenazine 是一种高度选择性的囊泡单胺转运蛋白 2 (VMAT2) 抑制剂,Ki为 110-190 nM,用于治疗迟发性运动障碍。
产品描述
Valbenazine, a highly selective vesicular monoamine transporter 2(VMAT2) inhibitor, is approved for the treatment of tardive dyskinesia.
体内活性
Valbenazine appeared to be well tolerated in adults with TD who received up to 48 weeks of treatment. In addition to long-term efficacy results, Suggest that valbenazine may be appropriate for the long-term management of TD regardless of underlying psychiatric diagnosis (SCHZ disorder or mood disorder)[1].
动物实验
The pooled long-term exposure (LTE) population included valbenazine-treated subjects from 3 studies: KINECT; KINECT 3; KINECT4. Safety assessments included adverse events (AEs), laboratory tests, vital signs, electrocardiograms (ECGs), and extrapyramidal symptom (EPS) scales. Psychiatric stability was monitored using the Positive and Negative Syndrome Scale (PANSS) and Calgary Depression Scale for Schizophrenia (CDSS) (SCHZ subgroup), as well as the Montgomery-?sberg Depression Rating Scale (MADRS) and Young Mania Rating Scale (YMRS) (mood subgroup). All data were analyzed descriptively[1].
Cas No.
1025504-45-3
分子式
C24H38N2O4
分子量
418.56
别名
NBI-98854
储存和溶解度
DMSO:50 mg/mL (119.45 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years