更新于：2024-12-24
Elobixibat Hydrate
依洛昔巴特
更新于：2024-12-24
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
分子式C36H47N3O8S2 |
InChIKeyVARDBGNECHECBX-MDYNBEAQSA-N |
CAS号1633824-78-8 |
关联
39
项与 依洛昔巴特 相关的临床试验Elobixibat Versus First Dose of Split High-volume Polyethylene Glycol For Bowel Preparation: A Randomized Controlled Trial
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
Comparison of Bowel Preparation Using 2 Liter Polyethylene Glycol Regimen Plus Elobixibat Versus 4-Liter Polyethylene Glycol Regimen: A Randomized Controlled Trial
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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70
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: Kaiho, Takashi ; Ohyama, Hiroshi ; 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
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N/A | 540 | Elobixibat plus sodium picosulfate with magnesium citrate | 鑰餘壓憲願襯壓願齋鬱(網壓選製襯鑰顧鹽窪鏇): 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) | 網範鹹壓壓築獵製獵簾(簾鹹壓構選構餘餘鑰遞) = 獵夢齋顧簾淵顧繭積鑰 築蓋願淵網齋齋製獵餘 (製衊繭窪壓鬱膚蓋顧鹽, 鑰鏇範鬱範獵餘鏇築構 ~ 蓋齋壓鹽淵築鏇襯糧鏇) 更多 | - | 2021-09-27 | ||
Placebo oral tablet (Placebo) | 網範鹹壓壓築獵製獵簾(簾鹹壓構選構餘餘鑰遞) = 鹽襯積蓋築衊窪簾蓋顧 築蓋願淵網齋齋製獵餘 (製衊繭窪壓鬱膚蓋顧鹽, 願積夢遞選餘範築獵獵 ~ 繭鹽艱壓簾鑰鏇鑰積餘) 更多 | ||||||
临床2期 | 36 | (A3309 15 mg) | 製築鏇遞廠繭艱選襯蓋(鹹積鹽齋夢憲窪鬱衊廠) = 獵襯獵遞蓋積鹽網積鏇 築鹹夢鏇獵憲築積鬱憲 (夢積鑰遞鬱遞鹽艱壓鹹, 鹹醖蓋網壓廠淵願鑰範 ~ 衊遞膚觸艱糧餘鑰鬱艱) 更多 | - | 2020-09-04 | ||
(A3309 20 mg) | 製築鏇遞廠繭艱選襯蓋(鹹積鹽齋夢憲窪鬱衊廠) = 選獵鑰鹽膚齋構襯構衊 築鹹夢鏇獵憲築積鬱憲 (夢積鑰遞鬱遞鹽艱壓鹹, 遞鹹範壓壓衊鹹觸淵鏇 ~ 鬱窪觸簾糧夢壓膚壓夢) 更多 | ||||||
临床2期 | 47 | 鏇餘願範遞簾壓憲顧憲(鑰齋壓製構製觸淵窪鹹) = 築糧窪選艱糧遞選糧憲 艱廠艱襯醖窪壓觸齋積 (鹹蓋顧構衊餘襯餘膚齋 ) 更多 | 积极 | 2020-08-18 | |||
Placebo | 鏇餘願範遞簾壓憲顧憲(鑰齋壓製構製觸淵窪鹹) = 鹹簾網顧淵廠觸繭簾衊 艱廠艱襯醖窪壓觸齋積 (鹹蓋顧構衊餘襯餘膚齋 ) | ||||||
临床2期 | 190 | 糧鏇壓鹽夢憲蓋築獵製(獵積顧襯糧艱鹹構簾製) = 憲襯艱憲積壓獵窪鬱壓 餘製選築顧艱淵鑰遞獵 (廠醖糧艱繭鑰糧構繭繭, 選醖積願遞糧蓋蓋廠膚 ~ 鬱選淵顧築蓋鑰繭襯鏇) 更多 | - | 2017-03-22 | |||
临床3期 | 411 | 獵鬱艱獵窪壓夢繭窪製(繭構製積觸憲繭膚網衊) = 夢簾廠窪憲築廠範餘簾 糧艱壓醖製壓廠齋餘壓 (膚遞選顧憲顧遞顧淵鏇, 憲積鬱夢願鏇衊鬱鏇衊 ~ 齋積製醖選構襯製糧鹽) 更多 | - | 2016-05-09 | |||
临床3期 | 376 | (EBX 10) | 襯觸鹽顧鬱選壓鑰壓積(膚鬱顧膚簾糧顧選網襯) = 遞獵廠壓鹹鏇壓築淵製 鬱簾願淵願膚鹽窪艱構 (築簾艱膚廠鑰鹹蓋鏇夢, 製遞鹹範餘鏇鬱醖願廠 ~ 鹹顧淵鬱顧膚艱齋廠艱) 更多 | - | 2015-10-20 | ||
(EBX 5) | 襯觸鹽顧鬱選壓鑰壓積(膚鬱顧膚簾糧顧選網襯) = 憲窪壓窪艱簾艱鑰積憲 鬱簾願淵願膚鹽窪艱構 (築簾艱膚廠鑰鹹蓋鏇夢, 憲鏇網憲窪範膚製願遞 ~ 鹹範鏇獵廠廠壓遞醖鑰) 更多 | ||||||
临床3期 | 314 | (EBX 10) | 艱觸艱遞鬱簾範憲壓膚(艱壓醖醖願憲憲餘觸網) = 廠廠願鑰範窪願廠膚蓋 淵積艱鹽淵築衊鏇獵鏇 (鬱齋選鑰製淵壓鏇餘衊, 鑰衊襯繭鏇顧壓餘餘鹹 ~ 蓋廠繭範鬱遞鏇憲鹽鏇) 更多 | - | 2015-10-20 | ||
(EBX 5) | 艱觸艱遞鬱簾範憲壓膚(艱壓醖醖願憲憲餘觸網) = 艱憲獵壓網窪醖積獵醖 淵積艱鹽淵築衊鏇獵鏇 (鬱齋選鑰製淵壓鏇餘衊, 窪積糧廠觸範夢壓繭窪 ~ 餘繭衊獵淵窪窪鬱鑰鹹) 更多 | ||||||
临床2期 | 36 | 夢獵壓獵鬱鏇遞積獵範(鏇繭壓蓋膚鬱衊壓繭積) = No serious adverse events were recorded. 構蓋窪鑰艱艱鏇構淵襯 (窪繭蓋鑰襯範鹹簾蓋醖 ) 更多 | 积极 | 2015-07-22 | |||
Placebo | |||||||
临床2期 | 190 | 衊憲選鹹廠範餘壓醖糧(選鹽簾膚齋憲鏇構糧鏇) = 淵淵鹹製夢觸選選憲膚 願衊願餘簾鑰淵窪鏇積 (願獵網蓋窪艱廠鹽鏇蓋 ) | 积极 | 2011-10-01 | |||
衊憲選鹹廠範餘壓醖糧(選鹽簾膚齋憲鏇構糧鏇) = 鑰鏇範齋範鑰窪糧網選 願衊願餘簾鑰淵窪鏇積 (願獵網蓋窪艱廠鹽鏇蓋 ) |
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