更新于：2024-11-04
Ansofaxine Hydrochloride
盐酸托鲁地文拉法辛
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 4-Methylbenzoate desvenlafaxine hydrochloride、Anshufaxine hydrochloride、ansofaxine + [8] |
作用机制 多巴胺重摄取抑制剂、NET抑制剂(去甲肾上腺素转运蛋白抑制剂)、5-羟色胺重摄取抑制剂 |
治疗领域 |
非在研适应症- |
原研机构 |
在研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2022-11-01), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C24H32ClNO3 |
InChIKeyBVWFJKQJRNSYCR-UHFFFAOYSA-N |
CAS号916918-84-8 |
关联
30
项与 盐酸托鲁地文拉法辛 相关的临床试验评价盐酸托鲁地文拉法辛缓释片（若欣林®）治疗中国抑郁症患者长期有效性及安全性研究（RESTORE研究）
A Multicenter, Randomized Withdrawal, Double-blind, Parallel, Placebo-controlled Design Clinical Trial of Toludesvenlafaxine Hydrochloride Extended-Release Tablets
Efficacy and Safety of Toludesvenlafaxine Hydrochloride Sustained-release Tablets Versus Venlafaxine Hydrochloride Sustained-release Tablets in Patients With Major Depression Disorder: a Multicentre, Open-label, Parallel-group, Randomised Controlled Trial
100 项与 盐酸托鲁地文拉法辛 相关的临床结果
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100 项与 盐酸托鲁地文拉法辛 相关的转化医学
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100 项与 盐酸托鲁地文拉法辛 相关的专利（医药）
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15
项与 盐酸托鲁地文拉法辛 相关的文献（医药）2024-07-01European journal of nuclear medicine and molecular imaging
PET/CT study of dopamine transporter (DAT) binding with the triple reuptake inhibitor toludesvenlafaxine in rats and humans
Article
作者: Shen, Yifeng ; Huang, Zhiwei ; Xie, Fang ; Wu, Junhao ; Wei, Yumei ; Guan, Yihui
PURPOSE:
Toludesvenlafaxine is a recently developed antidepressant that belongs to the triple reuptake inhibitor class. Despite the in vitro evidence that toludesvenlafaxine inhibits the reuptake of serotonin (5-HT), norepinephrine (NE) and dopamine (DA), there is no in vivo evidence that toludesvenlafaxine binds to DAT and increases DA level, a mechanism thought to contribute to its favorable clinical performance.
METHODS:
Positron emission tomography/computed tomography (PET/CT) was used to examine the DAT binding capacity in healthy rats and human subjects and microdialysis was used to examine the striatal DA level in rats. [18F]FECNT and [11C]CFT were used as PET/CT radioactive tracer for rat and human studies, respectively.
RESULTS:
In rats, 9 mg/kg of toludesvenlafaxine hydrochloride (i.v.) followed by an infusion of 3 mg/kg via minipump led to the binding rate to striatum DAT at 3.7 - 32.41% and to hypothalamus DAT at 5.91 - 17.52% during the 45 min scanning period. 32 mg/kg oral administration with toludesvenlafaxine hydrochloride significantly increased the striatal DA level with the AUC0 - 180 min increased by 63.9%. In healthy volunteers, 160 mg daily toludesvenlafaxine hydrochloride sustained-release tablets for 4 days led to an average occupancy rates of DAT at 8.04% ± 7.75% and 8.09% ± 7.00%, respectively, in basal ganglion 6 h and 10 h postdose.
CONCLUSION:
These results represent the first to confirm the binding of toludesvenlafaxine to DAT in both rats and humans using PET/CT, and its elevation of brain DA level, which may help understand the unique pharmacological and functional effects of triple reuptake inhibitors such as toludesvenlafaxine.
CLINICALTRIALS:
GOV IDENTIFIERS:
NCT05905120. Registered 14 June 2023. (retrospectively registered).
2023-05-10Translational psychiatry
A phase 3, multicenter, double-blind, randomized, placebo-controlled clinical trial to verify the efficacy and safety of ansofaxine (LY03005) for major depressive disorder.
Article
作者: Chen, Jindong ; Xie, Shiping ; Di, Xiaolan ; Xu, Xiufeng ; Yang, Dong ; Zhou, Yunfei ; Wang, Huaning ; Jiang, Zhiwei ; Li, Yi ; Yang, Chanjuan ; Luo, Jiong ; Li, Lehua ; Zhang, Kerang ; Zhang, Hongyan ; Tian, Feng ; Lv, Shuyun ; Li, Huafang ; Chen, Zhenhua ; Wang, Yiming ; Mi, Weifeng ; Tian, Jingwei ; Wu, Bin ; Yi, Qizhong ; Zhong, Hua ; Wang, Guoqiang
Major depressive disorder (MDD) is the most prevalent form of depression and is becoming a great challenge for public health and medical practice. Although first-line antidepressants offer therapeutic benefits, about 35% of depressed patients are not adequately treated, creating a substantial unmet medical need. A multicenter, double-blind, randomized, placebo-controlled phase 3 clinical trial was conducted in patients with MDD in China to assess the efficacy and safety of ansofaxine (LY03005), a potential triple reuptake inhibitor of serotonin, norepinephrine, and dopamine. Eligible 588 MDD patients were included and randomly assigned (1:1:1) to 8-week treatment with ansofaxine 80 mg/day(n = 187), ansofaxine 160 mg/day(n = 186), or placebo(n = 185). The primary efficacy endpoint was the Montgomery-Åsberg Depression Rating Scale (MADRS) total score change from baseline to the end of the study. Safety indexes included adverse events, vital signs, physical examination, laboratory tests, 12-lead electrocardiogram (ECG), and evaluation of suicide tendency and sexual function. Significant differences were found in mean changes in MADRS total score at week 8 in the two ansofaxine groups (80 mg, -20.0; 160 mg, -19.9) vs. placebo (-14.6; p < 0.0001). All doses of ansofaxine were generally well-tolerated. Treatment-emergent adverse events (TEAEs) were reported by 137 (74.46%) patients in ansofaxine 80 mg group, 144 (78.26%) patients in ansofaxine 160 mg and 125 (67.93%) patients in the placebo group. The incidence of treatment-related adverse events (TRAEs) was 59.2% (109 patients), 65.22% (120 patients) in the 80, 160 mg ansofaxine groups, and 45.11% (83 patients) in the placebo group. The initial results of this trial indicate that ansofaxine at both the 80 mg/day and 160 mg/day was effective and safe in adult patients with MDD. ClinicalTrials.gov Identifier: NCT04853407.
2023-05-01Journal of affective disorders
A multicenter, randomized, double-blind, duloxetine-controlled, non-inferiority trial of desvenlafaxine succinate extended-release in patients with major depressive disorder
Article
作者: Lyu, Nan ; Xu, Xiufeng ; He, Shunqiang ; Wang, Qian ; Fu, Bingbing ; Li, Junqing ; Zou, Shaohong ; He, Ruifeng ; Wang, Zhiqiang ; Li, Lehua ; Hu, ZhenYu ; Pan, Xiaoyue ; Zhao, Jinghua ; Zhao, Qian ; Li, Shuang ; Zhao, Jingyuan ; Lu, Zheng ; Li, Yi ; Huang, Guangbiao ; Wang, Gang ; Tan, Yunlong ; Wei, Bo ; Zhang, Xuehua ; Guo, Hua ; Chen, Ce ; Pan, Zhenyu ; Li, Keqing ; Yang, Chuang ; He, Hongbo ; Li, Hengfen ; Wang, Xueyi ; Wang, Wenqiang ; Xu, Xiangdong
BACKGROUND:
Desvenlafaxine and duloxetine are selective serotonin and norepinephrine reuptake inhibitors. Their efficacy has not been directly compared using statistical hypotheses. This study evaluated the non-inferiority of desvenlafaxine extended-release (XL) to duloxetine in patients with major depressive disorder (MDD).
METHODS:
In this study, 420 adult patients with moderate-to-severe MDD were enrolled and randomly assigned (1:1) to receive 50 mg (once daily [QD]) of desvenlafaxine XL (n = 212) or 60 mg QD of duloxetine (n = 208). The primary endpoint was evaluated using a non-inferiority comparison based on the change from baseline to 8 weeks in the 17-item Hamilton Depression Rating Scale (HAMD17) total score. Secondary endpoints and safety were evaluated.
RESULTS:
Least-squares mean change in HAM-D17 total score from baseline to 8 weeks was -15.3 (95% confidence interval [CI]: -17.73, -12.89) in the desvenlafaxine XL group and - 15.9 (95% CI, -18.44, -13.39) in the duloxetine group. The least-squares mean difference was 0.6 (95% CI: -0.48, 1.69), and the upper boundary of 95% CI was less than the non-inferiority margin (2.2). No significant between-treatment differences were found in most secondary efficacy endpoints. The incidence of the most common treatment-emergent adverse events (TEAEs) was lower for desvenlafaxine XL than for duloxetine for nausea (27.2% versus 48.8%) and dizziness (18.0% versus 28.8%).
LIMITATIONS:
A short-term non-inferiority study without a placebo arm.
CONCLUSIONS:
This study demonstrated that desvenlafaxine XL 50 mg QD was non-inferior to duloxetine 60 mg QD in efficacy in patients with MDD. Desvenlafaxine had a lower incidence of TEAEs than duloxetine did.
100 项与 盐酸托鲁地文拉法辛 相关的药物交易
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 抑郁症 | 中国 | 2022-11-01 |
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临床3期 | - | 鏇廠襯觸艱襯鑰鏇範繭(窪願壓構膚選鬱壓廠夢) = 若欣林®在治疗8周末的蒙哥马利-艾斯伯格抑郁量表（MADRS）总分较基线的变化显著优于安慰剂 遞齋築窪膚築獵鏇夢獵 (製繭憲齋範憲艱構鑰積 ) 更多 | 积极 | 2022-12-06 | |||
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