更新于：2024-04-26
Berberine Ursodeoxycholate
小檗碱熊去氧胆酸盐
更新于：2024-04-26
概要
基本信息
原研机构 |
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)临床3期 |
特殊审评快速通道 (美国)、孤儿药 (美国) |
结构
分子式C44H57NO8 |
InChIKeyFHZVFXJRSFLYDY-FUXQPCDDSA-M |
CAS号1868138-66-2 |
关联
18
项与 小檗碱熊去氧胆酸盐 相关的临床试验一项在轻度、中度肝功能损害患者与匹配的肝功能正常受试者中评价HTD1801药代动力学的I期、单次给药、开放标签研究
一项评价HTD1801在患有进展至肝纤维化的非酒精性脂肪性肝炎（NASH）伴2型糖尿病或糖尿病前期的成人患者中的多中心、随机、双盲、安慰剂对照 IIb期研究（CENTRICITY研究）
评价HTD1801胶囊在二甲双胍治疗后血糖控制不佳的2型糖尿病患者中有效性和安全性的多中心、随机、双盲、安慰剂平行对照Ⅲ期临床研究
100 项与 小檗碱熊去氧胆酸盐 相关的临床结果
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100 项与 小檗碱熊去氧胆酸盐 相关的转化医学
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100 项与 小檗碱熊去氧胆酸盐 相关的专利（医药）
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4
项与 小檗碱熊去氧胆酸盐 相关的文献（医药）2022-11-01American Journal of Gastroenterology
Berberine Ursodeoxycholate for the Treatment of Primary Sclerosing Cholangitis: The Search for the Elusive Pharmacologic Holy Grail Will Need to Continue
Article
作者: Yoshida, Eric M
Abstract:
Effective pharmacologic treatment of primary sclerosing cholangitis (PSC) remains elusive. Ursodeoxycholic acid (UDCA) is known to improve liver biochemistry, specifically serum alkaline phosphatase, in patients with PSC but has not been shown to favourably alter the natural history. Similarly, many immunomodulatory medications have been studied for the treatment of PSC, but none has been demonstrated to be of unequivocal benefit. In this issue of the Journal, a pilot study of a ursodeoxycholate berberine salt vs placebo is reported. Although improvement in serum alkaline phosphatase is reported, without a control arm with UDCA monotherapy, it is not possible to determine whether this study drug is beneficial over UDCA by itself. More study in the PSC therapeutic arena is needed.
2022-11-01American Journal of Gastroenterology
A Randomized, Dose-Finding, Proof-of-Concept Study of Berberine Ursodeoxycholate in Patients With Primary Sclerosing Cholangitis
Article
作者: Gunn, Nadege ; Harrison, Stephen A ; Landis, Charles ; Liberman, Alexander ; Eksteen, Bertus ; Forman, Lisa ; Sundaram, Vinay ; Kowdley, Kris V ; Levy, Cynthia ; Hirschfield, Gideon M ; Di Bisceglie, Adrian M
INTRODUCTION::
Primary sclerosing cholangitis (PSC) is a fibroinflammatory disease of the bile ducts leading to cirrhosis and hepatic decompensation. There are no approved pharmaceutical therapies for PSC. Berberine ursodeoxycholate (HTD1801) is an ionic salt of berberine and ursodeoxycholic acid with pleiotropic mechanisms of action.
METHODS::
An 18-week proof-of-concept study was conducted to assess the safety and efficacy of HTD1801 in PSC. This study had three 6-week periods: (i) a placebo-controlled period, (ii) a treatment extension period, and (iii) a randomized treatment withdrawal period. The primary end point was change from baseline in alkaline phosphatase (ALP) at week 6.
RESULTS::
Fifty-five patients were randomized and treated; 35 (64%) had inflammatory bowel disease and 22 (40%) had previously received ursodeoxycholic acid. Patients were initially randomized to placebo (n = 16), HTD1801 500 mg BID (n = 15), or HTD1801 1000 mg BID (n = 24). At baseline, mean (range) ALP values were 414 U/L (138–1,048), 397 U/L (237–773), and 335 U/L (122–882) for the placebo, HTD1801 500 mg BID, and HTD1801 1,000 mg BID groups, respectively. At week 6, a significant decrease in ALP was observed with HTD1801 (least square mean; HTD1801 500 mg BID = −53 U/L, P = 0.016; HTD1801 1000 mg BID = −37 U/L, P = 0.019) compared with placebo (98 U/L). ALP reductions were sustained through week 18 in those who remained on therapy, whereas ALP increased in those who crossed over to placebo during period 3. HTD1801 was generally well tolerated; 4 patients experienced serious adverse events, none attributed to HTD1801.
DISCUSSION::
HTD1801 is associated with significant improvement in ALP and warrants further study as a treatment for PSC.
2020-12-01Lipids in health and disease3区 · 医学
Pharmacokinetics and pharmacodynamics of HTD1801 (berberine ursodeoxycholate, BUDCA) in patients with hyperlipidemia
3区 · 医学
ArticleOA
作者: Watts, Gerald F ; Bai, Ru ; Di Bisceglie, Adrian M ; Yu, Meng ; Lavin, Philip ; Liu, Liping
Abstract:
Background:
Reduction in elevated serum cholesterol concentrations is important in the management of individuals at risk of atherosclerotic cardiovascular disease (ASCVD), such as myocardial infarction and thrombotic stroke. Although HMGCoA reductase inhibitors (“statins”) are frequently used for this purpose, a significant proportion of patients remain at increased residual risk of ASCVD as they do not adequately address some of the associated co-morbidities such as diabetes and fatty liver disease.
Methods:
A double-blind, randomized, placebo-controlled, dose ranging study was carried out that compared three doses of berberine ursodeoxycholate (BUDCA) to placebo in a cohort of subjects with a history of hypercholesterolemia and serum LDL cholesterol levels above 2.59 mmol/L (> 99.9 mg/dL). BUDCA was administered in two divided doses each day for 28 days. The primary endpoints of the study were safety and tolerability of this new compound, as well as its effect in lowering serum lipid and lipoprotein concentrations.
Results:
A total of 50 subjects were enrolled into three dose cohorts in this study. BUDCA was generally well tolerated, even at doses of 2000 mg per day (the highest dose group); there were no significant adverse effects reported and this highest dose was associated with significant reductions in LDL cholesterol. By day 28 and with the highest dose of BUDCA, there were significant reductions in the serum concentrations of total cholesterol by 8.2% (P = 0.0004) and LDL cholesterol by 10.4% (P = 0.0006), but no significant changes in triglyceride and HDL cholesterol concentrations.
Conclusions:
BUDCA is a new single molecular entity that has a significant but modest effect in safely lowering serum LDL-cholesterol concentrations in individuals with a history of hypercholesterolemia. It has a potential use for treating hypercholesterolemia in individuals who cannot take statins, and possibly as adjunctive to other agents, such as ezetimibe or bempedoic acid.
Trial registration:
The study was registered onClinicaltrials.gov(NCT03381287).
71
项与 小檗碱熊去氧胆酸盐 相关的新闻（医药）2024-04-22
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100 项与 小檗碱熊去氧胆酸盐 相关的药物交易
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 2型糖尿病 | 临床3期 | 中国 更多 | |
| 原发性硬化性胆管炎 | 临床3期 | 全球 更多 | |
| 肝纤维化 | 临床2期 | 中国 更多 | |
| 非酒精性脂肪性肝炎 | 临床2期 | 美国 更多 | |
| 糖尿病前期 | 临床2期 | 中国 更多 |
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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2期 | 100 | 鹽醖顧膚淵蓋選壓鬱壓(製廠齋衊艱醖繭壓構壓) = 範願觸願餘鏇鹽窪網壓 齋築鹹簾鹹鑰衊築衊築 (構憲糧鏇餘觸夢網鬱簾 ) | - | 2023-06-21 | |||
临床1/2期 | 50 | Placebo to match 1000 mg HTD1801 (Placebo) | 簾網觸夢構鑰淵簾壓繭(壓鏇窪夢構夢獵壓蓋鹽) = 齋鏇夢憲鹹襯製鏇襯製 壓醖糧遞壓積獵製範觸 (膚糧艱淵製衊願艱餘願, 鹽廠鹽衊製簾製憲積夢 ~ 觸壓鏇鏇簾願鹹構蓋壓) 更多 | - | 2023-03-03 | ||
(HTD1801 250 mg BID) | 簾網觸夢構鑰淵簾壓繭(壓鏇窪夢構夢獵壓蓋鹽) = 築遞鏇夢願構願醖齋憲 壓醖糧遞壓積獵製範觸 (膚糧艱淵製衊願艱餘願, 築襯餘積鑰構餘願繭鹹 ~ 衊範網構獵糧鹹衊憲憲) 更多 | ||||||
临床2期 | 59 | Placebo | 築淵觸鬱網簾遞衊顧顧(網網鹹鹽壓選衊艱糧餘) = 顧簾廠鹹鹹網淵餘窪糧 選遞齋簾艱遞簾願醖膚 (簾餘淵壓遞醖廠衊醖積 ) | - | 2022-11-01 | ||
HTD1801 500 mg BID | 築淵觸鬱網簾遞衊顧顧(網網鹹鹽壓選衊艱糧餘) = 範築願蓋艱蓋鹽襯築願 選遞齋簾艱遞簾願醖膚 (簾餘淵壓遞醖廠衊醖積 ) | ||||||
N/A | - | 繭鏇鑰艱憲艱蓋衊遞夢(壓鬱鬱餘窪鹽觸夢醖繭) = substantially enhanced for HTD1801 across the pH range for BBR and at pH 6.5 for UDCA vs BBR-Cl or UDCA alone 膚廠簾憲鬱鬱觸簾憲鏇 (壓鏇範壓鏇蓋鹽願製憲 ) 更多 | - | 2022-06-25 | |||
临床2期 | 101 | (500mg HTD1801, Bid) | 衊製淵壓艱構簾範蓋鏇(壓餘遞顧蓋艱醖醖積簾) = 餘遞選膚範餘積餘壓顧 餘醖夢窪糧繭網鹹觸觸 (淵範築襯糧齋壓襯蓋鑰, 範夢壓製顧夢襯衊鹽鑰 ~ 蓋鏇憲衊憲鏇鹹夢網範) 更多 | - | 2021-12-29 | ||
(1000mg HTD1801, Bid) | 衊製淵壓艱構簾範蓋鏇(壓餘遞顧蓋艱醖醖積簾) = 窪顧糧願膚鹹餘憲範鏇 餘醖夢窪糧繭網鹹觸觸 (淵範築襯糧齋壓襯蓋鑰, 觸蓋淵遞繭願蓋願願艱 ~ 繭糧簾積簾積艱艱簾蓋) 更多 | ||||||
临床2期 | 100 | 夢鏇廠廠襯鹹遞窪壓艱(艱鏇築廠鹽願築鏇壓遞) = 鑰願膚選淵壓憲廠選鹹 窪齋鏇廠遞憲願窪鑰選 (願範壓鹹糧願壓願簾襯 ) | 积极 | 2021-09-17 | |||
Placebo | 夢鏇廠廠襯鹹遞窪壓艱(艱鏇築廠鹽願築鏇壓遞) = 鹹獵鹹艱築簾鏇襯夢遞 窪齋鏇廠遞憲願窪鑰選 (願範壓鹹糧願壓願簾襯 ) | ||||||
N/A | 50 | 餘糧遞壓築製觸夢鏇蓋(築壓餘膚簾簾廠壓遞窪) = 膚構願鏇鑰鹹醖鑰繭築 網範繭製齋製廠鑰糧齋 (憲範淵蓋構製憲醖製醖 ) 更多 | - | 2020-08-27 | |||
餘糧遞壓築製觸夢鏇蓋(築壓餘膚簾簾廠壓遞窪) = 醖鑰蓋獵繭醖製築膚淵 網範繭製齋製廠鑰糧齋 (憲範淵蓋構製憲醖製醖 ) 更多 |
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