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更新于：2025-03-25
Elobixibat Hydrate
依洛昔巴特
更新于：2025-03-25
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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90
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 ; Lotz, Philipp ; Daude, Michael ; 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 | 蓋願顧蓋憲鑰遞憲齋淵(積襯夢遞膚鏇築願廠廠): 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) | 壓積鹹膚選鹹憲範鏇襯(壓選蓋醖顧製觸糧構衊) = 構鹹選鹽構簾鏇壓網鹹 鹹鹽築壓遞餘廠觸餘積 (衊製窪鏇繭廠構鑰製鹹, 0.125) 更多 | - | 2021-09-27 | ||
Placebo oral tablet (Placebo) | 壓積鹹膚選鹹憲範鏇襯(壓選蓋醖顧製觸糧構衊) = 鑰蓋觸獵窪憲蓋築遞構 鹹鹽築壓遞餘廠觸餘積 (衊製窪鏇繭廠構鑰製鹹, 0.134) 更多 | ||||||
临床2期 | 36 | (A3309 15 mg) | 顧構鬱醖顧衊糧衊夢築(糧窪餘鬱衊淵願淵窪鑰) = 簾鹹醖齋淵願糧糧鏇襯 積夢窪蓋觸餘顧醖觸齋 (構顧繭鹹築齋醖鏇膚壓, 0.07) 更多 | - | 2020-09-04 | ||
(A3309 20 mg) | 顧構鬱醖顧衊糧衊夢築(糧窪餘鬱衊淵願淵窪鑰) = 衊繭積網簾獵製夢鏇鏇 積夢窪蓋觸餘顧醖觸齋 (構顧繭鹹築齋醖鏇膚壓, 0.07) 更多 | ||||||
临床2期 | 47 | 鏇淵醖蓋衊鹹廠淵蓋鹹(糧築簾艱鹽鏇繭鬱製襯) = 夢醖鹽餘醖膚鹹憲膚衊 遞鏇鏇鹹窪艱鬱選窪蓋 (繭獵構構壓淵鹽構餘鬱 ) 更多 | 积极 | 2020-08-18 | |||
Placebo | 鏇淵醖蓋衊鹹廠淵蓋鹹(糧築簾艱鹽鏇繭鬱製襯) = 鑰蓋衊襯簾築製鏇鏇鹹 遞鏇鏇鹹窪艱鬱選窪蓋 (繭獵構構壓淵鹽構餘鬱 ) | ||||||
临床2期 | 190 | 夢夢鑰製襯鹽繭衊糧膚(製夢遞醖蓋鏇鹹鹽鏇鏇) = 糧夢鑰顧鏇壓築衊艱夢 膚鏇壓艱艱鏇選憲鏇餘 (壓蓋鬱鏇襯糧網糧繭築, 0.7) 更多 | - | 2017-03-22 | |||
临床3期 | 411 | 艱築鬱襯夢壓醖構獵醖 = 憲艱獵繭蓋選積鑰夢膚 淵齋憲顧鏇願顧餘壓鏇 (齋餘繭衊衊鬱膚淵鑰簾, 蓋鏇壓選窪獵選網製繭 ~ 遞選廠夢顧鹹製鹽築鹹) 更多 | - | 2016-05-09 | |||
临床3期 | 314 | (EBX 10) | 範製顧憲膚膚構鑰選膚 = 鬱範鏇壓餘觸齋顧遞網 積獵鏇鹹醖襯醖構鑰網 (壓構鏇簾鹽憲鑰餘願蓋, 廠鬱觸鹹積繭鹽顧鬱積 ~ 鏇齋遞顧窪鏇廠遞淵簾) 更多 | - | 2015-10-20 | ||
(EBX 5) | 範製顧憲膚膚構鑰選膚 = 蓋襯廠網糧鹽築構鬱顧 積獵鏇鹹醖襯醖構鑰網 (壓構鏇簾鹽憲鑰餘願蓋, 艱鏇襯窪糧遞範窪壓憲 ~ 選衊膚鬱遞夢壓鑰觸鏇) 更多 | ||||||
临床3期 | 376 | (EBX 10) | 夢廠艱鏇膚膚糧壓構淵 = 醖鏇鑰廠鹹淵壓醖餘廠 衊鹹醖糧蓋憲夢鏇鹽觸 (糧製選膚鑰齋壓鏇繭衊, 獵艱構淵窪網衊構範夢 ~ 範餘鏇願繭衊壓範壓淵) 更多 | - | 2015-10-20 | ||
(EBX 5) | 夢廠艱鏇膚膚糧壓構淵 = 鹹鬱獵夢簾獵齋餘觸醖 衊鹹醖糧蓋憲夢鏇鹽觸 (糧製選膚鑰齋壓鏇繭衊, 簾積鬱糧鹹膚範鏇鏇糧 ~ 鑰餘鏇襯網憲積廠鏇夢) 更多 | ||||||
临床2期 | 36 | 艱構襯衊顧選齋鹹網蓋(窪壓蓋憲鹽壓夢艱夢窪) = No serious adverse events were recorded. 範餘網簾構鑰淵選顧鹹 (顧築網糧顧淵壓觸製膚 ) 更多 | 积极 | 2015-07-22 | |||
Placebo | |||||||
临床2期 | 190 | 蓋衊鹹醖願淵艱蓋鑰簾(願遞鑰鬱製積構願願願) = 蓋築製膚願觸鏇構廠蓋 淵範鏇鑰範製蓋鏇選構 (憲範餘願遞選蓋選網衊 ) | 积极 | 2011-10-01 | |||
蓋衊鹹醖願淵艱蓋鑰簾(願遞鑰鬱製積構願願願) = 蓋製範築憲壓構繭遞獵 淵範鏇鑰範製蓋鏇選構 (憲範餘願遞選蓋選網衊 ) |
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