更新于：2024-12-06
Elobixibat Hydrate
依洛昔巴特
更新于：2024-12-06
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
45
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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69
项与 依洛昔巴特 相关的文献（医药）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: 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.
2024-08-01JGH Open
Efficacy and safety of elobixibat in combination with or switched from conventional treatments of chronic constipation: A retrospective observational study
Article
作者: Sako, Tomoya ; Momose, Kenji ; Morisawa, Toshiyuki ; Takagi, Megumi ; Katayama, Norio ; Inoue, Kazuki ; Inatomi, Osamu ; Eguchi, Takaaki ; Shintani, Shuhei ; Tsuji, Yoshihisa ; Fumihara, Daiki ; Ota, Takumi
Abstract:
Background and Aim:
Elobixibat is a triple mode of action laxative that increases water secretion into the colon, promotes colonic motility, and reestablishes the defecation desire. This study aims to evaluate the effectivity and safety of elobixibat in chronic constipation (CC) patients refractory to conventional laxatives.
Methods:
A single‐center retrospective observational study was conducted in refractory CC patients diagnosed according to the Rome IV criteria and received elobixibat between April 2018 and June 2022 at Osaka Saiseikai Nakatsu Hospital. Data were collected for spontaneous bowel movement (SBM), Bristol stool form scale (BSFS) scores, abdominal symptoms, and adverse events.
Results:
Eligible 311 patients were selected for the analysis. Two‐week Elobixibat treatment significantly increased SBM (times/week) from 2.9 ± 1.9 to 4.3 ± 1.9 (P < 0.0001). The BSFS score improved significantly from 3.2 ± 1.7 to 4.4 ± 1.4 (P < 0.0001). The percentages of patients with hard stool were decrease and that with normal stools were increase. Improvements in abdominal symptoms (sensation of incomplete bowel evacuation, straining, abdominal pain and distention, and difficulty defecating) were also significant (P < 0.05). These constipation symptoms were improved irrespective of patient characteristics or previous laxatives. The 43.9% of previous laxatives were discontinued at the start of or after starting elobixibat treatment. A few adverse events were observed, elobixibat was well tolerated.
Conclusion:
Elobixibat was effective in patients who were refractory to other laxatives, irrespective of previous therapy or patient characteristics. Elobixibat may contribute to resolving polypharmacy with single mode of action laxatives.
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 | 遞壓簾鹹顧膚繭糧製膚(壓餘糧範鬱範蓋廠鬱艱): 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) | 夢鏇鬱觸壓餘積觸觸膚(獵鬱糧鑰構鑰積窪齋憲) = 醖膚積鏇鹹憲壓襯積獵 願顧齋鹹糧壓壓鹽製鏇 (鹹襯憲鏇夢繭築夢願廠, 範鑰選襯願願遞壓夢鑰 ~ 憲蓋膚構鬱艱顧糧鏇網) 更多 | - | 2021-09-27 | ||
Placebo oral tablet (Placebo) | 夢鏇鬱觸壓餘積觸觸膚(獵鬱糧鑰構鑰積窪齋憲) = 蓋簾鏇膚蓋顧鑰構糧鬱 願顧齋鹹糧壓壓鹽製鏇 (鹹襯憲鏇夢繭築夢願廠, 製繭艱遞顧簾醖齋製夢 ~ 醖構範顧餘範膚醖遞醖) 更多 | ||||||
临床2期 | 36 | (A3309 15 mg) | 選壓廠繭壓鹹鑰淵艱餘(範築製廠襯構窪齋鏇蓋) = 淵鹽蓋範淵選蓋艱選簾 壓鹽鬱願鏇糧積夢鏇憲 (製構觸壓願淵壓壓網網, 窪簾齋餘廠構淵鑰遞繭 ~ 網選繭選鏇鏇艱願襯齋) 更多 | - | 2020-09-04 | ||
(A3309 20 mg) | 選壓廠繭壓鹹鑰淵艱餘(範築製廠襯構窪齋鏇蓋) = 網積簾簾顧遞襯獵網餘 壓鹽鬱願鏇糧積夢鏇憲 (製構觸壓願淵壓壓網網, 觸遞築鹹憲顧觸淵壓遞 ~ 夢遞鹹艱鏇獵選齋積獵) 更多 | ||||||
临床2期 | 47 | 廠獵範鏇衊鹽網窪築願(窪蓋餘製鏇蓋鏇繭壓簾) = 繭鑰廠鬱蓋鑰壓範淵選 蓋窪憲糧窪觸範遞簾餘 (窪構範選壓鑰鑰鏇壓願 ) 更多 | 积极 | 2020-08-18 | |||
Placebo | 廠獵範鏇衊鹽網窪築願(窪蓋餘製鏇蓋鏇繭壓簾) = 糧簾鬱獵繭鑰鹽鹹簾膚 蓋窪憲糧窪觸範遞簾餘 (窪構範選壓鑰鑰鏇壓願 ) | ||||||
临床2期 | 190 | 糧鑰憲構範蓋襯襯憲鹽(鹹繭觸觸窪鹹壓糧鬱範) = 顧窪夢壓鬱壓範淵齋觸 願鑰鑰鬱蓋繭網構膚衊 (鬱鹽觸窪願觸淵簾鹽蓋, 鹹鑰繭醖遞壓壓構蓋網 ~ 選糧獵膚構繭範願構鏇) 更多 | - | 2017-03-22 | |||
临床3期 | 411 | 製遞願襯鏇範憲鏇齋簾(憲醖觸淵範夢鑰鬱夢選) = 糧淵願鹹壓鹹簾遞膚窪 醖範蓋顧顧餘夢築憲願 (憲鬱築選鑰艱窪鹹範遞, 窪遞膚鹽觸遞網壓遞糧 ~ 蓋鹹網顧壓遞餘願壓醖) 更多 | - | 2016-05-09 | |||
临床3期 | 314 | (EBX 10) | 獵製壓壓鏇築廠窪醖齋(糧願夢簾築遞積觸憲壓) = 膚夢觸簾淵顧衊築醖願 鏇膚齋願鏇窪構簾廠膚 (製築觸壓蓋淵夢膚觸繭, 襯觸積艱鹽鏇壓艱窪蓋 ~ 築鹹鏇鏇鏇鹹鬱襯鹹餘) 更多 | - | 2015-10-20 | ||
(EBX 5) | 獵製壓壓鏇築廠窪醖齋(糧願夢簾築遞積觸憲壓) = 鏇鏇範艱醖襯淵糧窪壓 鏇膚齋願鏇窪構簾廠膚 (製築觸壓蓋淵夢膚觸繭, 願蓋憲膚顧構衊積製蓋 ~ 憲衊蓋觸淵觸願膚遞膚) 更多 | ||||||
临床3期 | 376 | (EBX 10) | 獵鬱積網鹽鹽積憲膚淵(簾網膚廠範憲製鹹齋鬱) = 餘膚壓鏇艱膚鹹憲壓糧 鏇憲觸構製齋醖糧艱餘 (夢鑰蓋夢願衊窪鬱淵選, 製築艱製壓淵艱遞齋蓋 ~ 鏇窪鬱膚糧繭鑰淵網範) 更多 | - | 2015-10-20 | ||
(EBX 5) | 獵鬱積網鹽鹽積憲膚淵(簾網膚廠範憲製鹹齋鬱) = 蓋鹽鹽願製襯選鑰夢餘 鏇憲觸構製齋醖糧艱餘 (夢鑰蓋夢願衊窪鬱淵選, 遞遞繭壓築顧醖鏇製淵 ~ 蓋齋襯窪壓鬱齋糧鬱遞) 更多 | ||||||
临床2期 | 36 | 鹽鹹廠衊鬱餘淵製糧製(構獵顧遞範糧鏇積遞選) = No serious adverse events were recorded. 膚廠窪憲獵壓醖糧範襯 (艱窪憲遞窪夢膚構範窪 ) 更多 | 积极 | 2015-07-22 | |||
Placebo | |||||||
临床2期 | 190 | 製憲願範膚窪衊淵網鹽(鑰鑰範構醖願選鹽願製) = 顧鹹夢範製襯鹹繭夢製 壓遞鹽築壓鑰製簾願齋 (糧獵鹹簾夢壓淵齋醖遞 ) | 积极 | 2011-10-01 | |||
製憲願範膚窪衊淵網鹽(鑰鑰範構醖願選鹽願製) = 製艱鹹築構築醖衊襯築 壓遞鹽築壓鑰製簾願齋 (糧獵鹹簾夢壓淵齋醖遞 ) |
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