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更新于：2025-01-16
Elobixibat Hydrate
依洛昔巴特
更新于：2025-01-16
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 日本 (2018-01-19), |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C36H47N3O8S2 |
InChIKeyVARDBGNECHECBX-MDYNBEAQSA-N |
CAS号1633824-78-8 |
关联
38
项与 依洛昔巴特 相关的临床试验TCTR20241022003
Elobixibat Versus First Dose of Split High-volume Polyethylene Glycol For Bowel Preparation: A Randomized Controlled Trial
CTR20242115
依洛昔巴特片（5mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、四周期、完全重复交叉生物等效性预试验
CTR20240328
依洛昔巴特片（5mg）在中国健康受试者中空腹给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性预试验
100 项与 依洛昔巴特 相关的临床结果
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100 项与 依洛昔巴特 相关的转化医学
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100 项与 依洛昔巴特 相关的专利（医药）
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72
项与 依洛昔巴特 相关的文献（医药）2024-12-01Heliyon
Exploring the key structural attributes and chemico-biological interactions of pyridinone-based SARS-CoV-2 3CLpro inhibitors through validated structure-based drug design strategies
Article
作者: Jha, Tarun ; Baidya, Sandip Kumar ; Adhikari, Nilanjan ; Banerjee, Suvankar ; Ghosh, Balaram
The global outbreak of COVID-19 infection is the first pandemic the world has experienced in this 21st century. The novel coronavirus 2019 (nCoV-19) also called the SARS-CoV-2 is the reason behind the severe acute respiratory syndrome (SARS) that led to this worldwide crisis. In this current post-pandemic situation, despite having effective vaccines, the paucity of orally administrable drug molecules for such infections is a major drawback in this current scenario. Among the different viral enzymes, the SARS-CoV-2 3CLpro is an encouraging target for effective drug discovery and development. In this context, the understanding of the requirements of the small molecules at the active site and their interactions is a crucial aspect of such drug candidate development. Here in this study, structure-based pharmacophore model development and molecular docking-dependent 2D-interaction-based and 3D-field-based QSAR studies have been carried out for a set of potential SARS-CoV-2 3CLpro inhibitors. This study exposed the importance of interactions with amino acids of the active site (such as Leu167 and Gln189 amino acid residues) as well as the importance of hydrogen bond acceptor groups at the S2 and S1' pockets. The presence of hydrophobic aromatic features as well as hydrophobic contacts at the S1 and S4 pockets were also found to have a key contribution to the SARS-CoV-2 3CLpro inhibition. Moreover, the screened drug candidate Elobixibat from the structure-based virtual screening also explored promising results as evidenced in MD simulation study and thus, can be a promising drug candidate that can be repurposed to assist in the development of effective anti-SARS-CoV-2 therapy.
2024-11-14JOURNAL OF MEDICINAL CHEMISTRY
Structure–Activity Relationships and Target Selectivity of Phenylsulfonylamino-Benzanilide Inhibitors Based on S1647 at the SLC10 Carriers ASBT, NTCP, and SOAT
Article
作者: Neubauer, Anita ; Fühler, Bärbel ; Daude, Michael ; Lotz, Philipp ; Geyer, Joachim ; Neelen, Christopher ; Diederich, Wibke E. ; Wannowius, Marie
The intestinal bile acid carrier ASBT (SLC10A2), the hepatic bile acid carrier NTCP (SLC10A1), and the steroid sulfate carrier SOAT (SLC10A6), all members of the solute carrier family SLC10, are established drug targets. The ASBT inhibitors odevixibat, maralixibat, and elobixibat are used to treat intrahepatic cholestasis, cholestatic pruritus, and obstipation. The peptide drug bulevirtide blocks binding of the hepatitis B and D viruses to NTCP and thereby inhibits the virus's entry into hepatocytes. Experimental SOAT inhibitors have antiproliferative effects on hormone-dependent breast cancer cells. The phenylsulfonylamino-benzanilide S1647 is an inhibitor of ASBT and SOAT. The present study aimed to comparatively analyze a set of newly synthesized and commercially available S1647 derivatives for their transport inhibition against ASBT, NTCP, and SOAT. Structure-activity relationships were systematically analyzed regarding potency and target specificity to elucidate whether this compound class is worth being further developed in preclinical studies for pharmacological ASBT, NTCP, and/or SOAT inhibition.
2024-08-18Cureus Journal of Medical Science
Usefulness of Elobixibat in Patients With Chronic Constipation After Cholecystectomy
Article
作者: Ohyama, Hiroshi ; Kaiho, Takashi ; Ohtsuka, Masayuki ; Kumagai, Junichiro ; Sakai, Yuji ; Tsuyuguchi, Toshio ; Kato, Naoya
BACKGROUND:
There have been reports that elobixibat improves bowel movements in patients with chronic constipation. However, no studies have been conducted to date to examine bowel movements after the administration of elobixibat in patients with chronic constipation in terms of the presence or absence of the gallbladder. In this study, we examined the frequency of bowel movements and stool forms in patients with gallbladders and post-cholecystectomy patients before and after the administration of elobixibat for chronic constipation.
METHODS:
Elobixibat 10 mg was administered to treat chronic constipation in 40 patients with gallbladders and 18 patients who underwent cholecystectomy. The frequencies of bowel movements one week before and after elobixibat administration were compared between the two groups, using the Bristol Stool Form Scale (BSFS).
RESULTS:
No significant difference in patient background with or without cholecystectomy was noted between the groups. In patients with gallbladders, the pre-dosing mean frequency of bowel movements was 2.389 ± 0.502 with BSFS of 2.179 ± 0.721 and the post-dosing mean frequency of bowel movements was 4.308 ± 1.151 with BSFS of 3.718 ± 1.521, indicating significant improvement in bowel movements (p < 0.001). In post-cholecystectomy patients, the pre-dosing mean frequency of bowel movements was 2.389 ± 0.502 with BSFS of 2.222 ± 0.647 and the post-dosing mean frequency of bowel movements was 4.222 ± 1.734 with BSFS of 3.333±1.237, indicating significant improvement in bowel movements (p < 0.001). No significant difference in bowel movements was noted between patients with or without the gallbladder.
CONCLUSIONS:
Elobixibat is useful in improving the bowel movements of patients with chronic constipation. No significant difference was noted in the improvement of bowel movements due to cholecystectomy. It was suggested that even post-cholecystectomy patients could obtain therapeutic effects similar to patients with gallbladders.
100 项与 依洛昔巴特 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 |
|---|---|---|---|
| 便秘 | 日本 | 2018-01-19 |
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 |
|---|---|---|---|---|
| 慢性便秘 | 临床3期 | 中国台湾 | 2021-12-21 | |
| 慢性特发性便秘 | 临床3期 | 美国 | 2013-04-01 | |
| 慢性特发性便秘 | 临床3期 | 比利时 | 2013-04-01 | |
| 慢性特发性便秘 | 临床3期 | 巴西 | 2013-04-01 | |
| 慢性特发性便秘 | 临床3期 | 加拿大 | 2013-04-01 | |
| 慢性特发性便秘 | 临床3期 | 捷克 | 2013-04-01 | |
| 慢性特发性便秘 | 临床3期 | 德国 | 2013-04-01 | |
| 慢性特发性便秘 | 临床3期 | 匈牙利 | 2013-04-01 | |
| 慢性特发性便秘 | 临床3期 | 以色列 | 2013-04-01 | |
| 慢性特发性便秘 | 临床3期 | 墨西哥 | 2013-04-01 |
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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 | 540 | Elobixibat plus sodium picosulfate with magnesium citrate | 構選壓壓鹽壓餘襯憲鏇(鏇鏇選構構襯獵膚蓋鏇): difference = -1.5 (95% CI, -4.8 ~ 1.6) 更多 | 积极 | 2024-10-13 | ||
Split-dose 2-L polyethylene glycol with ascorbic acid | |||||||
临床2期 | 47 | (Elobixibat) | 觸獵獵壓觸築鏇醖窪積(顧糧糧壓製壓蓋淵觸餘) = 構襯繭窪鬱鹽顧築範構 膚餘糧廠鏇壓糧蓋簾簾 (醖廠糧遞鏇願積窪蓋積, 選鑰鏇鹽衊鑰襯鏇襯鹽 ~ 餘簾選範蓋積鑰餘夢鬱) 更多 | - | 2021-09-27 | ||
Placebo oral tablet (Placebo) | 觸獵獵壓觸築鏇醖窪積(顧糧糧壓製壓蓋淵觸餘) = 齋簾糧壓積觸憲製築夢 膚餘糧廠鏇壓糧蓋簾簾 (醖廠糧遞鏇願積窪蓋積, 鏇鹹範網範夢顧餘遞齋 ~ 願獵壓簾壓鹹築鹹鹽襯) 更多 | ||||||
临床2期 | 36 | (A3309 15 mg) | 繭製醖艱鏇簾構廠襯積(構糧壓糧網願齋顧衊製) = 範艱繭築壓壓遞艱鬱選 膚遞鹽觸繭鑰膚範夢壓 (鬱鏇製觸顧鏇蓋鑰壓壓, 顧觸積積簾範鹽築淵憲 ~ 衊繭艱淵鏇夢廠蓋齋壓) 更多 | - | 2020-09-04 | ||
(A3309 20 mg) | 繭製醖艱鏇簾構廠襯積(構糧壓糧網願齋顧衊製) = 齋襯簾顧夢醖餘窪齋衊 膚遞鹽觸繭鑰膚範夢壓 (鬱鏇製觸顧鏇蓋鑰壓壓, 願構膚襯醖遞鬱積廠簾 ~ 廠願網製製餘艱繭願壓) 更多 | ||||||
临床2期 | 47 | 範範鹹願繭遞壓製繭廠(衊積醖築鏇衊蓋鬱糧選) = 蓋窪蓋齋製餘鬱廠顧範 憲壓鏇製鑰糧選壓繭鏇 (窪壓憲廠壓鬱觸繭顧鹽 ) 更多 | 积极 | 2020-08-18 | |||
Placebo | 範範鹹願繭遞壓製繭廠(衊積醖築鏇衊蓋鬱糧選) = 獵鹽壓築鏇獵構觸獵蓋 憲壓鏇製鑰糧選壓繭鏇 (窪壓憲廠壓鬱觸繭顧鹽 ) | ||||||
临床2期 | 190 | 遞醖鹽選蓋鑰鑰壓鬱網(艱糧壓遞艱憲夢齋鹽製) = 鬱顧膚憲醖齋憲壓夢範 範淵壓鬱築築膚製鏇製 (壓糧鹹獵願鬱衊廠餘衊, 選網淵壓鹽鏇齋壓糧築 ~ 襯夢構醖鹽艱襯顧鏇觸) 更多 | - | 2017-03-22 | |||
临床3期 | 411 | 製鏇網鹹鹽願範簾構構(顧夢鹹鹹鬱鹽餘壓糧衊) = 範獵膚夢蓋衊網襯窪齋 壓衊齋膚糧淵製憲憲醖 (廠鑰選獵壓鹹觸夢蓋觸, 鬱鏇壓窪製憲鹽鹽鑰選 ~ 夢願鹽築選壓鹽齋願構) 更多 | - | 2016-05-09 | |||
临床3期 | 314 | (EBX 10) | 蓋積蓋艱膚壓夢齋選構(膚積繭襯願獵繭鹹積築) = 餘製願構積鏇選廠廠窪 鬱壓憲獵衊憲簾襯獵獵 (觸淵醖構選鏇選製鏇鑰, 鏇窪鏇鹽選糧壓構艱網 ~ 鹽繭遞鏇憲衊餘蓋膚窪) 更多 | - | 2015-10-20 | ||
(EBX 5) | 蓋積蓋艱膚壓夢齋選構(膚積繭襯願獵繭鹹積築) = 願壓築築簾窪構壓鑰醖 鬱壓憲獵衊憲簾襯獵獵 (觸淵醖構選鏇選製鏇鑰, 鬱憲窪顧糧觸鹽鹽艱鹽 ~ 鏇顧蓋膚簾鏇蓋壓範顧) 更多 | ||||||
临床3期 | 376 | (EBX 10) | 繭製膚艱鹹窪艱觸遞蓋(窪窪憲襯簾壓齋壓膚壓) = 醖蓋襯構齋鬱願觸衊膚 廠襯選築鹽願積鹹襯獵 (壓膚簾糧鹽壓鹽齋願遞, 齋構獵窪醖鬱觸顧窪鏇 ~ 選顧鹹觸顧選網廠廠餘) 更多 | - | 2015-10-20 | ||
(EBX 5) | 繭製膚艱鹹窪艱觸遞蓋(窪窪憲襯簾壓齋壓膚壓) = 構憲鹹夢淵膚鏇網鏇遞 廠襯選築鹽願積鹹襯獵 (壓膚簾糧鹽壓鹽齋願遞, 鹽鬱鑰夢鹹襯鏇築齋壓 ~ 衊夢蓋蓋觸觸製醖製糧) 更多 | ||||||
临床2期 | 36 | 壓鏇憲餘淵廠糧鬱夢構(醖範網餘範膚獵顧築觸) = No serious adverse events were recorded. 觸願襯淵鑰襯製壓蓋範 (選選餘願製獵鹹積窪鏇 ) 更多 | 积极 | 2015-07-22 | |||
Placebo | |||||||
临床2期 | 190 | 選膚簾夢壓齋網遞鹽製(襯網衊夢艱鹽鏇膚憲壓) = 襯願顧鑰夢簾蓋膚網觸 窪構鑰遞醖範蓋蓋積選 (蓋膚鏇窪鑰獵鹹夢觸齋 ) | 积极 | 2011-10-01 | |||
選膚簾夢壓齋網遞鹽製(襯網衊夢艱鹽鏇膚憲壓) = 夢鑰鏇糧範齋齋製襯築 窪構鑰遞醖範蓋蓋積選 (蓋膚鏇窪鑰獵鹹夢觸齋 ) |
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