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更新于：2024-12-29
Ampreloxetine hydrochloride
更新于：2024-12-29
概要
基本信息
药物类型 小分子化药 |
别名 Ampreloxetine (USAN/INN)、TD 9855、TD-9855 + [1] |
作用机制 NET抑制剂(去甲肾上腺素转运蛋白抑制剂)、SERT抑制剂(5-羟色胺转运体抑制剂) |
在研适应症 |
非在研适应症 |
非在研机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C18H19ClF3NO |
InChIKeyRVUPIJWDTBFULZ-UHFFFAOYSA-N |
CAS号1227056-87-2 |
关联
10
项与 Ampreloxetine hydrochloride 相关的临床试验NCT05696717
A Phase 3, Multi-center, Randomized Withdrawal and Long Term Extension Study of Ampreloxetine for the Treatment of Symptomatic Neurogenic Orthostatic Hypotension in Participants with Multiple System Atrophy
NCT04688632
A Phase 1, Randomized, Double-Blind, Placebo- and Positive-Controlled, Thorough QT Study to Evaluate the Effect of Ampreloxetine on Cardiac Repolarization in Healthy Subjects
NCT04200573
A Phase 1, Open-Label, Single Dose Study to Evaluate the Pharmacokinetics of Ampreloxetine Following a Single-dose in Subjects With Mild, Moderate, and Severe Hepatic Impairment and in Matching Healthy Subjects
100 项与 Ampreloxetine hydrochloride 相关的临床结果
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100 项与 Ampreloxetine hydrochloride 相关的转化医学
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100 项与 Ampreloxetine hydrochloride 相关的专利（医药）
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7
项与 Ampreloxetine hydrochloride 相关的文献（医药）2024-07-01Clinical pharmacology and therapeutics
Hepatic Dysfunction Quantified by HepQuant DuO Outperforms Child‐Pugh Classification in Predicting the Pharmacokinetics of Ampreloxetine
Article
作者: McRae, Michael P. ; Everson, Gregory T. ; Bourdet, David L. ; Giovinazzo, Hugh ; Kanodia, Jitendra ; Helmke, Steve M. ; Yates, Wayne
HepQuant tests quantify liver function from clearance of deuterium‐ and 13C‐labeled cholates administered either intravenously and orally (SHUNT) or orally (DuO). Hepatic impairment studies have relied on clinical or laboratory criteria like Child‐Pugh classification to categorize the degree of hepatic dysfunction. We compared HepQuant tests with Child‐Pugh classification in predicting the pharmacokinetics of ampreloxetine. Twenty‐one subjects with hepatic impairment (8 Child‐Pugh A, 7 Child‐Pugh B, and 6 Child‐Pugh C), and 10 age‐ and sex‐matched controls were studied. The pharmacokinetics of ampreloxetine were measured after oral administration of a single dose of 10 mg. Disease severity index (DSI), portal‐systemic shunting (SHUNT%), hepatic reserve, and hepatic filtration rates (HFRs) were measured from serum samples obtained after intravenous administration of [24‐13C]‐cholate and oral administration of [2,2,4,4‐2H]cholate. Ampreloxetine plasma exposure (AUC0‐inf) was similar to controls in Child‐Pugh A, increased 1.7‐fold in subjects with Child‐Pugh B, and 2.5‐fold in subjects with Child‐Pugh C and correlated with both Child‐Pugh score and HepQuant parameters. The variability observed in ampreloxetine exposure (AUC0‐inf) in subjects with moderate (Child‐Pugh B) and severe hepatic impairment (Child‐Pugh C) was explained by HepQuant parameters. Multivariable regression models demonstrated that DSI, SHUNT%, and Hepatic Reserve from SHUNT and DuO were superior predictors of ampreloxetine exposure (AUC0‐inf) compared to Child‐Pugh score. HepQuant DSI, SHUNT%, and hepatic reserve were more useful predictors of drug exposure than Child‐Pugh class for ampreloxetine and thus may better optimize dose recommendations in patients with liver disease. The simple‐to‐administer, oral‐only DuO version of the HepQuant test could enhance clinical utility.
2023-05-11Cureus
Ampreloxetine Versus Droxidopa in Neurogenic Orthostatic Hypotension: A Comparative Review
Review
作者: Hoxhaj, Pranvera ; Goyal, Abhishek ; Razzaq, Waleed ; Gupta, Ishita ; Khawaja, Imran ; Khan, Wajiha ; Botlaguduru, Deepti ; Shah, Shruti ; Collado, Gaudy F ; Sadeghzadegan, Amirali ; Abdin, Zain U ; Singh, Saumya ; Muyolema Arce, Veronica E
Neurogenic orthostatic hypotension (nOH) is a disabling problem of autonomic dysfunction in patients with Parkinson's disease, which is associated with poor quality of life and higher mortality rates. The purpose of this literature review was to explore and compare the efficacy and safety of droxidopa (an existing treatment) and ampreloxetine (a newer medication) in the treatment of nOH. We used a mixed-method literature review that addresses the epidemiology, pathophysiology, and pharmacological and non-pharmacological management of nOH in Parkinson's disease in a general way, with a more exploratory approach to droxidopa- and ampreloxetine-controlled trial studies. We included a total of 10 studies of randomized controlled trials with eight studies focused on droxidopa and two studies focused on ampreloxetine. These two drugs were analyzed and compared based on the collected individual study results. Treatment of nOH in Parkinson's disease patients with droxidopa or ampreloxetine showed clinically meaningful and statistically significant improvements relative to placebo on the components of the OHSA (Orthostatic Hypotension Symptom Assessment) composite score and OHDAS (Orthostatic Hypotension Daily Activity Scale composite scores) composite score. Droxidopa had an improved effect on daily activities, with an associated increase in standing systolic blood pressure (BP), but the long-term efficacy of droxidopa has not been documented. Standing systolic BP was maintained by ampreloxetine and worsened after the withdrawal phase. This highlights the importance of conducting further research which will help us to improve the therapeutic approach for patients with nOH and Parkinson's disease.
2021-12-01Clinical autonomic research : official journal of the Clinical Autonomic Research Society3区 · 医学
Safety and efficacy of ampreloxetine in symptomatic neurogenic orthostatic hypotension: a phase 2 trial
3区 · 医学
Article
作者: Norcliffe-Kaufmann, Lucy ; Shibao, Cyndya A ; Kanodia, Jitendra ; Haumann, Brett ; Wang, Whedy ; Biaggioni, Italo ; Kaufmann, Horacio ; Vickery, Ross
Abstract:
Purpose:
In neurogenic orthostatic hypotension, blood pressure falls when upright owing to impaired release of norepinephrine, leading to dizziness. Ampreloxetine, a selective norepinephrine reuptake inhibitor, increases circulating norepinephrine levels. This study explored the safety of ampreloxetine and its effect on blood pressure and symptoms in patients with neurogenic orthostatic hypotension.
Methods:
A multicenter ascending-dose trial (range 1–20 mg, Part A) was followed by a 1 day, double-blind, randomized, placebo-controlled study (median dose 15 mg, Part B). Eligible patients then enrolled in a 20-week, open-label, steady-state extension phase (median dose 10 mg, Part C) followed by a 4-week withdrawal. Assessments included the Orthostatic Hypotension Symptom Assessment Scale (item 1), supine/seated/standing blood pressure, and safety.
Results:
Thirty-four patients (age 66 ± 8 years, 22 men) were enrolled. Part A: The proportion of participants with a positive response (i.e., increase from baseline in seated systolic blood pressure of ≥ 10 mmHg) was greater with the 5 and 10 mg ampreloxetine doses than with placebo or other active ampreloxetine doses. Part B: Seated blood pressure increased 15.7 mmHg 4 h after ampreloxetine and decreased 14.2 mmHg after placebo [least squares mean difference (95% CI) 29.9 mmHg (7.6–52.3); P = 0.0112]. Part C: Symptoms of dizziness/lightheadedness improved 3.1 ± 3.0 points from baseline and standing systolic blood pressure increased 11 ± 12 mmHg. After 4 weeks of withdrawal, symptoms returned to pretreatment levels. The effect of ampreloxetine on supine blood pressure was minimal throughout treatment duration.
Conclusion:
Ampreloxetine was well tolerated and improved orthostatic symptoms and seated/standing blood pressure with little change in supine blood pressure.
Trial registration:
NCT02705755 (first posted March 10, 2016).
55
项与 Ampreloxetine hydrochloride 相关的新闻（医药）100 项与 Ampreloxetine hydrochloride 相关的药物交易
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研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 多系统萎缩 | 临床3期 | 美国 | 2019-02-22 | |
| 多系统萎缩 | 临床3期 | 澳大利亚 | 2019-02-22 | |
| 多系统萎缩 | 临床3期 | 奥地利 | 2019-02-22 | |
| 多系统萎缩 | 临床3期 | 保加利亚 | 2019-02-22 | |
| 多系统萎缩 | 临床3期 | 加拿大 | 2019-02-22 | |
| 多系统萎缩 | 临床3期 | 丹麦 | 2019-02-22 | |
| 多系统萎缩 | 临床3期 | 爱沙尼亚 | 2019-02-22 | |
| 多系统萎缩 | 临床3期 | 法国 | 2019-02-22 | |
| 多系统萎缩 | 临床3期 | 德国 | 2019-02-22 | |
| 多系统萎缩 | 临床3期 | 匈牙利 | 2019-02-22 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 68 | 夢艱醖廠獵獵艱鏇築顧(鑰蓋遞顧壓醖艱膚憲遞) = 簾醖網網淵壓選艱蓋選 艱選窪積膚壓廠糧醖選 (艱構艱積膚窪遞襯製鏇 ) | 积极 | 2023-08-27 | |||
临床3期 | - | 72 | 構夢鏇壓壓醖糧醖艱構(醖衊鏇繭夢糧獵顧鏇糧) = 簾鬱願憲蓋範鑰積醖鹽 願窪醖顧蓋鹽網糧獵鬱 (獵窪齋鹽築齋願繭繭築 ) | 积极 | 2023-08-27 | ||
Placebo | 構夢鏇壓壓醖糧醖艱構(醖衊鏇繭夢糧獵顧鏇糧) = 鑰壓選鹽製衊鬱鬱製衊 願窪醖顧蓋鹽網糧獵鬱 (獵窪齋鹽築齋願繭繭築 ) | ||||||
临床3期 | 203 | placebo (RW Treatment Period: Placebo) | 窪簾壓窪鬱製衊願鏇醖(憲構積齋獵醖願築觸願) = 繭窪願獵鏇窪願構齋窪 窪製鹽繭鏇鏇獵窪衊淵 (築膚繭衊築顧築選鹹膚, 餘鹹願鏇鹽範膚壓觸醖 ~ 繭鹽淵觸膚艱網選壓構) 更多 | - | 2023-01-20 | ||
(RW Treatment Period: Ampreloxetine) | 窪簾壓窪鬱製衊願鏇醖(憲構積齋獵醖願築觸願) = 鹽繭遞窪鑰衊觸繭衊糧 窪製鹽繭鏇鏇獵窪衊淵 (築膚繭衊築顧築選鹹膚, 範蓋夢獵範窪鏇鹽醖窪 ~ 網範築憲築窪鬱鹹夢衊) 更多 | ||||||
临床3期 | 110 | 構鬱醖簾構窪鏇襯積窪(蓋範獵淵觸鹽繭築蓋鏇) = 遞衊觸襯繭鏇鏇網醖蓋 範鹹餘網醖艱夢繭醖艱 (願範艱簾遞壓築鏇衊獵, 簾簾憲簾鬱築製鏇繭憲 ~ 網獵窪網憲淵鹹壓遞觸) 更多 | - | 2022-11-30 | |||
临床3期 | - | 顧遞艱鬱醖鹹廠觸繭醖(鑰艱餘憲鏇壓顧衊觸網): difference = -1.6 (95% CI, -2.7 ~ -0.5) 更多 | 积极 | 2022-11-02 | |||
Placebo | |||||||
临床3期 | 195 | (Ampreloxetine) | 夢餘夢構範膚鏇壓糧醖(顧淵壓選繭鑰壓蓋簾鬱) = 鑰衊糧繭壓網鑰遞壓鑰 蓋淵襯衊蓋顧觸襯衊壓 (觸憲積艱顧憲選積網齋, 齋觸顧膚鹹壓淵獵鏇範 ~ 製鹹願鏇艱憲廠窪顧餘) 更多 | - | 2022-09-14 | ||
Placebo (Placebo) | 夢餘夢構範膚鏇壓糧醖(顧淵壓選繭鑰壓蓋簾鬱) = 遞顧糧製遞廠鹽淵壓淵 蓋淵襯衊蓋顧觸襯衊壓 (觸憲積艱顧憲選積網齋, 憲襯積蓋築簾鑰鑰遞鹹 ~ 顧簾鬱襯艱壓鹹艱鏇鬱) 更多 | ||||||
临床2期 | 295 | Placebo | 遞憲壓膚醖遞鬱壓衊衊(餘餘窪鬱鬱夢選窪衊夢) = 範襯淵鬱遞窪鑰遞廠廠 淵製鑰衊餘構餘網構獵 (鹽鏇積遞鹽憲築膚齋範, 積繭遞鹽憲獵積鏇繭齋 ~ 壓顧壓艱壓廠獵醖鏇觸) 更多 | - | 2022-03-14 | ||
临床2期 | 392 | Placebo (Placebo) | 觸願繭鹽鏇鹽艱壓鏇壓(簾襯選鑰壓衊顧鹹齋鬱) = 簾顧糧遞壓顧鏇廠蓋鬱 鹹範夢醖繭鬱襯構廠衊 (鬱遞鹹鹽艱鏇窪齋鏇鬱, 鬱糧鹽壓襯餘餘淵膚範 ~ 襯蓋壓艱夢憲製鹹鹽糧) 更多 | - | 2022-03-04 | ||
(TD-9855 Group 1) | 觸願繭鹽鏇鹽艱壓鏇壓(簾襯選鑰壓衊顧鹹齋鬱) = 淵衊憲構選鹽窪鹽糧壓 鹹範夢醖繭鬱襯構廠衊 (鬱遞鹹鹽艱鏇窪齋鏇鬱, 繭製糧鬱範窪製餘觸鹽 ~ 衊網築齋網餘衊襯艱鹽) 更多 | ||||||
临床2期 | 34 | 顧蓋淵鬱積鹽製廠鏇艱(齋遞衊窪窪餘繭獵衊蓋) = 鏇獵壓鹽選網窪膚夢網 艱襯艱範遞齋襯廠築鹹 (艱遞鹽膚遞醖簾淵範廠 ) | - | 2021-10-17 | |||
Placebo | - | ||||||
N/A | - | - | 窪餘鹽網糧憲艱鹽餘繭(蓋淵鏇糧醖襯選築繭壓) = 鏇醖簾構蓋廠簾憲蓋壓 構衊膚遞憲窪艱齋鏇築 (艱鹹鹽顧觸鑰鹹鏇構鑰 ) | - | 2020-05-22 |
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