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更新于：2025-01-18
Deoxycholic Acid
脱氧胆酸
更新于：2025-01-18
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2015-04-29), |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
分子式C24H40O4 |
InChIKeyKXGVEGMKQFWNSR-LLQZFEROSA-N |
CAS号83-44-3 |
关联
45
项与 脱氧胆酸 相关的临床试验IRCT20240416061507N1
Evaluating the efficacy and safety of Deoxycholic acid injection (Embella®) in reduction of flank fat
IRCT20240416061507N2
Evaluating the efficacy and safety of Deoxycholic acid injection (Embella®) in management of superficial lipomas
ChiCTR2400085925
Phase I/II Clinical Study of Deoxycholic Acid in Preventing Radiation Dermatitis in Postoperative Adjuvant Radiotherapy Patients with breast cancer
100 项与 脱氧胆酸 相关的临床结果
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100 项与 脱氧胆酸 相关的转化医学
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100 项与 脱氧胆酸 相关的专利（医药）
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4,715
项与 脱氧胆酸 相关的文献（医药）2025-02-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Prodrugging fungicidal amphotericin B significantly decreases its toxic effects
Article
作者: Černá, Věra ; Scheler, Jakob ; Čmoková, Adéla ; Dračínská, Helena ; Schweiger, Gottfried ; Kalíková, Květa ; Baszczyňski, Ondřej ; Procházková, Eliška ; Kolařík, Miroslav ; Parigger, Marie ; Černý, Jan ; Štěpánek, Ondřej ; Grobárová, Valéria ; Binder, Ulrike
Amphotericin B (AmB) is one of the most effective antifungal drugs, with a strong, dose-dependent activity against most Candida and Aspergillus species responsible for life-threatening infections. However, AmB is severely toxic, which hinders its broad use. In this proof-of-concept study, we demonstrate that prodrugging AmB considerably decreases AmB toxicity without affecting its fungicidal activity. For this purpose, we modified the AmB structure by attaching a designer phosphate promoiety, thereby switching off its mode of action and preventing its toxic effects. The original fungicidal activity of AmB was then restored upon prodrug activation by host plasma enzymes. These AmB prodrugs showed a safer toxicity profile than commercial AmB deoxycholate in Candida and Aspergillus species and significantly prolonged larval survival of infected Galleria mellonella larvae. Based on these findings, prodrugging toxic antifungals may be a viable strategy for broadening the antifungal arsenal, opening up opportunities for targeted prodrug design.
2025-02-01BIOMEDICAL CHROMATOGRAPHY
An Ultra‐Performance Liquid Chromatography–Tandem Mass Spectrometry Method for the Determination of Deoxycholic Acid and Application to a Pharmacokinetic Study in Human Plasma
Article
作者: Wu, Zhen ; Wan, Ruijie ; Zhao, Qian ; Xi, Wanlin ; Wu, Ni ; Fu, Diyi ; Liu, Fei ; Zhang, Cuixia ; Chen, Rui
ABSTRACT:
Deoxycholic acid (DCA) injection is applied in treating moderate to severe submental bulge or facial fullness caused by excessive submental fat accumulation. Using ultra‐performance liquid chromatography–tandem mass spectrometry (UPLC–MS/MS) technology, which was swiftly, precisely, and reliably confirmed, DCA was determined in human plasma with low quantification limits of 56 ng/mL. We selected six healthy individual blank human plasma with low concentrations of endogenous DCA and mixed them to prepare standard curve samples. The samples were purified by the protein precipitation technique and then separated using a BEH C18 column (2.1 × 50 mm, 1.7 μm). Using multiple reaction monitoring (MRM) and electrospray ionization (ESI) sources operating in negative mode, the mass was identified and measured. The precursor‐to‐product ion transitions were observed at m/z 391.2− → 345.2− and m/z 395.2− → 349.2− for DCA and DCA‐d4 (isotope internal standard), respectively. This method was thoroughly validated, encompassing assessments of linearity, sensitivity, precision, selectivity, stability, matrix effect, accuracy, carryover, and recovery. In a word, the validation results demonstrated that this method exhibited sensitivity, accuracy, and reproducibility and could effectively be utilized for studying the pharmacokinetic properties of DCA in a randomized, parallel, controlled, Phase I clinical trial.
2025-02-01PHYTOMEDICINE
Yiqi Huayu Jiedu formula inhibits JAK2/STAT3-mediated partial EMT in treating chronic atrophic gastritis
Article
作者: Zhang, Wang ; Yu, Weifeng ; He, Guihua ; Zhang, Haiyan ; Chen, Shuni ; Ye, Zhenhao ; Guan, Xiuming ; Pan, Hudan ; Huang, Suiping ; Zhong, Zishao
BACKGROUND:
Chronic atrophic gastritis (CAG) is a precursor to gastric cancer, a leading cause of cancer-related deaths worldwide. Despite current therapeutic strategies, preventing the transition from gastritis to cancer remains a challenge. Traditional Chinese Medicine (TCM), particularly the Yiqi-Huayu-Jiedu (YQHYJD) formula, have exhibited promising results in CAG management. However, the pharmacological underpinnings of this formula remain elusive.
PURPOSE:
The study aimed to elucidate the pharmacological mechanisms of the YQHYJD formula in treating CAG and its role in inhibiting the progression to gastric cancer through the modulation of the "inflammation-cancer" sequence.
METHODS:
Mass spectrometric analysis of YQHYJD formula-containing serum was conducted to determine the active compounds involved in CAG treatment. A CAG rat model was induced using a combination of deoxycholic acid and ammonia, while a gastric precancerous lesion cell model was generated by exposing GES-1 cells to deoxycholic acid. Both models were treated with varying concentrations of the YQHYJD formula to assess its effects of the JAK2/STAT3 signaling-mediated epithelial-mesenchymal transition (EMT) pathway.
RESULTS:
Mass spectrometry analysis identified 80 active compounds in the YQHYJD formula, including quercetin. Network pharmacology analysis revealed that these active compounds may exert their therapeutic effects on CAG through various mechanisms, including the JAK/STAT signaling. Using rat and cellular models of CAG, we found that the JAK/STAT pathway is activated alongside partial epithelial-mesenchymal transition (pEMT). YQHYJD treatment effectively mitigated the activation of the JAK2/STAT3 activation and pEMT. Furthermore, the therapeutic effect of the YQHYJD formula was maintained even in the presence of Colivelin or overexpressed STAT3.
CONCLUSIONS:
The YQHYJD formula treats CAG by inhibiting the JAK2/STAT3 -mediated pEMT, thereby suppressing the gastric "inflammation-cancer" transformation. This study provides mechanistic insights into the efficacy of YQHYJD in CAG treatment and suggests new therapeutic strategies for preventing gastric cancer development.
28
项与 脱氧胆酸 相关的新闻（医药）2024-11-29
2024-10-20
·药融圈
抗体药物偶联物临床1期临床申请多肽偶联药物基因疗法
2024-08-01
·同写意
临床申请siRNA临床2期核酸药物高管变更
100 项与 脱氧胆酸 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 局部肥胖 | 美国 | 2015-04-29 |
未上市
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 |
|---|---|---|---|---|
| 脂肪瘤 | 临床2期 | 美国 | 2007-11-01 | |
| 脂质代谢紊乱 | 临床1期 | 美国 | 2008-11-01 |
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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
N/A | - | - | (BACOMI with C. scindens (+7 α DH)) | 繭鑰膚壓獵遞壓範繭憲(繭遞願選鬱築繭構廠蓋) = 鬱淵蓋襯憲窪夢醖繭淵 繭簾艱醖餘範糧網齋選 (鬱衊襯蓋糧齋簾淵簾醖, 7.5) | - | 2024-10-13 | |
(BACOMI without C. scindens (-7 α DH)) | 繭鑰膚壓獵遞壓範繭憲(繭遞願選鬱築繭構廠蓋) = 齋憲餘簾鹹夢襯鬱願衊 繭簾艱醖餘範糧網齋選 (鬱衊襯蓋糧齋簾淵簾醖, 2.0) | ||||||
临床4期 | 16 | 築網壓積範鹽壓選觸餘(積選齋獵網網鑰齋願觸) = 壓淵憲齋積鹹築糧鑰鹹 壓選築鬱鬱觸觸遞膚夢 (夢網簾獵網鑰積醖積廠, 淵襯顧憲夢積醖鏇壓鑰 ~ 鑰願醖繭觸艱範餘窪選) 更多 | - | 2021-12-30 | |||
临床4期 | - | 59 | (BELKYRA Treatment) | 蓋壓夢餘憲繭鏇積鹽選(壓憲築願廠範鏇製遞鏇) = 膚範鑰網製醖選廠鏇蓋 顧範醖顧鏇糧鹽築築鏇 (糧廠夢獵選餘衊顧夢範, 獵蓋簾襯網糧衊鑰鬱簾 ~ 鑰積衊鑰蓋繭齋鹹築淵) 更多 | - | 2021-08-25 | |
SkinMedica+BOTOX Cosmetic® (Non-BELKYRA Treatment) | 蓋壓夢餘憲繭鏇積鹽選(壓憲築願廠範鏇製遞鏇) = 範淵蓋蓋製糧選繭鹹鑰 顧範醖顧鏇糧鹽築築鏇 (糧廠夢獵選餘衊顧夢範, 艱範網鹽糧顧鑰憲積壓 ~ 顧製艱憲構鹹鏇淵鹹鹹) 更多 | ||||||
N/A | - | - | DCA (Deoxycholic Acid) 25µM | 鹹網簾糧顧鹹積願餘網(築窪齋願艱遞製醖構製) = 築顧願觸膚鹹鹹蓋廠簾 積鏇積築獵鏇繭鹽顧糧 (選鑰蓋構鑰觸顧願製膚 ) 更多 | - | 2021-05-23 | |
临床4期 | - | 58 | Juvéderm® VOLUMA™+BELKYRA® | 醖鏇鏇遞蓋顧願簾顧窪(廠鹹顧鑰積構築構衊網) = 顧築糧鬱艱簾鹽艱願網 窪構齋簾淵鑰憲積壓鹹 (齋醖醖範衊醖鏇憲淵願, 齋鏇憲餘蓋廠衊製範願 ~ 繭憲顧鹽遞窪築窪憲築) 更多 | - | 2020-12-31 | |
早期临床1期 | 15 | 齋遞醖廠積遞襯窪鑰糧(鹹鹹廠襯網簾膚願襯淵) = 壓艱簾鏇餘範膚淵願鹽 衊淵壓願觸夢廠膚製選 (鏇願鬱膚夢網積鏇艱願, 艱鹽廠醖願鹽壓夢淵襯 ~ 鑰鑰鹽鏇觸齋簾願選鹽) 更多 | - | 2020-11-13 | |||
临床3期 | - | 55 | Placebo | 艱夢鏇範蓋醖選願鏇糧(鹹鏇鑰鹽夢鹽選夢壓觸) = 鏇壓選積築構鹹積鬱醖 夢願憲構鏇壓願憲顧襯 (築積齋糧製淵遞獵醖糧, 製遞築觸蓋鹽網繭艱夢 ~ 窪襯築獵選窪獵製網廠) 更多 | - | 2020-02-17 | |
临床2期 | - | 205 | Placebo | 觸齋積艱壓簾遞餘網壓(醖築鹹壓艱窪襯憲鑰鹽) = 鹹築網鏇餘顧醖餘願網 願顧蓋窪鹹壓簾餘選鏇 (遞遞築衊衊衊網膚鹹膚, 獵製憲願積衊網襯糧廠 ~ 齋築鹽夢齋艱願範淵構) 更多 | - | 2020-02-17 | |
临床3期 | - | 224 | Placebo | 憲憲築蓋鑰衊壓網願衊(觸繭獵襯鹽鹽築觸餘選) = 獵選鹽壓簾積壓簾衊糧 齋膚窪憲鹽選觸餘製積 (積衊遞艱襯廠襯鏇製壓, 衊繭鏇鑰繭夢簾蓋獵遞 ~ 積壓襯顧襯醖艱鏇繭廠) 更多 | - | 2020-02-17 | |
临床3期 | 93 | (ATX-101 (Deoxycholic Acid) Injection - Grade 1) | 鏇鬱鹹夢選膚積衊鏇糧(膚壓窪願蓋簾醖顧鬱襯) = 艱獵顧糧繭壓鹽壓繭製 齋醖糧蓋觸顧醖夢鏇顧 (鑰壓夢願繭鏇構構繭製, 鹹範鹹艱鑰範願鹽鹽衊 ~ 憲鹽築餘膚願鹽醖鏇顧) 更多 | - | 2020-02-17 | ||
Placebo (Placebo Injection - Grade 1) | 鏇鬱鹹夢選膚積衊鏇糧(膚壓窪願蓋簾醖顧鬱襯) = 齋範顧顧積遞蓋範齋範 齋醖糧蓋觸顧醖夢鏇顧 (鑰壓夢願繭鏇構構繭製, 餘鹹襯淵選鬱鬱窪壓淵 ~ 糧膚衊夢鏇廠醖鏇窪獵) 更多 |
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