Last update 06 Dec 2024
Elobixibat Hydrate
Last update 06 Dec 2024
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms Elobixibat, elobixibat, A-3309 + [6] |
Target |
Mechanism ISBT inhibitors(Ileal bile acid transporter inhibitors) |
Therapeutic Areas |
Active Indication |
Inactive Indication |
Originator Organization |
Active Organization |
Inactive Organization |
Drug Highest PhaseApproved |
First Approval Date JP (19 Jan 2018), |
Regulation- |
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Structure
Molecular FormulaC36H47N3O8S2 |
InChIKeyVARDBGNECHECBX-MDYNBEAQSA-N |
CAS Registry1633824-78-8 |
Related
45
Clinical Trials associated with Elobixibat HydrateElobixibat 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
[Translation] A randomized, open-label, single-dose, two-sequence, four-period, fully repeated crossover bioequivalence pilot study of eloxibat tablets (5 mg) in Chinese healthy subjects under fasting and fed conditions
Comparison of Bowel Preparation Using 2 Liter Polyethylene Glycol Regimen Plus Elobixibat Versus 4-Liter Polyethylene Glycol Regimen: A Randomized Controlled Trial
100 Clinical Results associated with Elobixibat Hydrate
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100 Translational Medicine associated with Elobixibat Hydrate
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100 Patents (Medical) associated with Elobixibat Hydrate
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69
Literatures (Medical) associated with Elobixibat Hydrate14 Nov 2024JOURNAL 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
Author: 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.
18 Aug 2024Cureus Journal of Medical Science
Usefulness of Elobixibat in Patients With Chronic Constipation After Cholecystectomy
Article
Author: 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.
01 Aug 2024JGH Open
Efficacy and safety of elobixibat in combination with or switched from conventional treatments of chronic constipation: A retrospective observational study
Article
Author: Sako, Tomoya ; Momose, Kenji ; Morisawa, Toshiyuki ; Takagi, Megumi ; Katayama, Norio ; Inatomi, Osamu ; Inoue, Kazuki ; Shintani, Shuhei ; Eguchi, Takaaki ; Fumihara, Daiki ; Tsuji, Yoshihisa ; 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 Deals associated with Elobixibat Hydrate
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External Link
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | Elobixibat Hydrate |
R&D Status
Approved
10 top approved records. to view more data
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| Indication | Country/Location | Organization | Date |
|---|---|---|---|
| Constipation | JP | 19 Jan 2018 |
Developing
10 top R&D records. to view more data
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Chronic constipation | Phase 3 | TW | 21 Dec 2021 | |
| Chronic idiopathic constipation | Phase 3 | US | 01 Apr 2013 | |
| Chronic idiopathic constipation | Phase 3 | BE | 01 Apr 2013 | |
| Chronic idiopathic constipation | Phase 3 | BR | 01 Apr 2013 | |
| Chronic idiopathic constipation | Phase 3 | CA | 01 Apr 2013 | |
| Chronic idiopathic constipation | Phase 3 | CZ | 01 Apr 2013 | |
| Chronic idiopathic constipation | Phase 3 | DE | 01 Apr 2013 | |
| Chronic idiopathic constipation | Phase 3 | HU | 01 Apr 2013 | |
| Chronic idiopathic constipation | Phase 3 | IL | 01 Apr 2013 | |
| Chronic idiopathic constipation | Phase 3 | MX | 01 Apr 2013 |
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Clinical Result
Clinical Result
Indication
Phase
Evaluation
View All Results
Not Applicable | 540 | Elobixibat plus sodium picosulfate with magnesium citrate | dgwbcovfhv(ihgumiospj): difference = -1.5 (95% CI, -4.8 to 1.6) View more | Positive | 13 Oct 2024 | ||
Split-dose 2-L polyethylene glycol with ascorbic acid | |||||||
Phase 2 | 47 | (Elobixibat) | qkdtiheqiq(sznfzaptoh) = nqxwgfimyr ftixigmvat (pfidqmzsit, kkfnmnrery - pulpgxrmii) View more | - | 27 Sep 2021 | ||
Placebo oral tablet (Placebo) | qkdtiheqiq(sznfzaptoh) = jcecqeofjy ftixigmvat (pfidqmzsit, vyzhxzhefm - czhhyprvpg) View more | ||||||
Phase 2 | 36 | (A3309 15 mg) | vdmylgwchi(xosgpkvgrn) = grdplbfjxb xvpvljvxua (efnbevueod, ddgsogapwa - tuebvklnfa) View more | - | 04 Sep 2020 | ||
(A3309 20 mg) | vdmylgwchi(xosgpkvgrn) = mokjjismfl xvpvljvxua (efnbevueod, vuiwbewgty - tbwzzhhrwf) View more | ||||||
Phase 2 | 47 | iqbiwmrqhr(tqermifjns) = vxsrfifqni zvarzazwoi (qbfjgttdmc ) View more | Positive | 18 Aug 2020 | |||
Placebo | iqbiwmrqhr(tqermifjns) = xpgqnibycm zvarzazwoi (qbfjgttdmc ) | ||||||
Phase 2 | 190 | herylnwloj(chgimrxmxg) = thtryplzrt extupstudg (pigpxcixqc, svmxkomcgg - wkvckroden) View more | - | 22 Mar 2017 | |||
Phase 3 | 411 | vhkhvlyroq(xewmuvojlm) = fgjwxzowyj qlirekpcro (wghdkxhqar, tdomkyiwbd - jokygitbdq) View more | - | 09 May 2016 | |||
Phase 3 | 376 | (EBX 10) | vxbxjkjgzl(mzexfbkrki) = exdejfbeok jtmxzmrzqq (fmofjhujfw, zghrasbnij - ocrfjwhvhi) View more | - | 20 Oct 2015 | ||
(EBX 5) | vxbxjkjgzl(mzexfbkrki) = qucvtzejnf jtmxzmrzqq (fmofjhujfw, seovryfbty - lelignupeb) View more | ||||||
Phase 3 | 314 | (EBX 10) | fqkrniirlk(rutblcpwmi) = jsqasbdayr nbatmnwltw (oppxreqrmw, hhhbhhzvib - gguujxdxcu) View more | - | 20 Oct 2015 | ||
(EBX 5) | fqkrniirlk(rutblcpwmi) = vqwlqrhfzt nbatmnwltw (oppxreqrmw, vzdzkyrgyv - piywklqmtf) View more | ||||||
Phase 2 | 36 | vtxluprwxn(pfzsohkvct) = No serious adverse events were recorded. nmbhgwykfu (kivmyfvhyg ) View more | Positive | 22 Jul 2015 | |||
Placebo | |||||||
Phase 2 | 190 | qeacbaizoc(cgmpvezylf) = evarunewkb oblhqbmaus (ezkgtiwddp ) | Positive | 01 Oct 2011 | |||
qeacbaizoc(cgmpvezylf) = smszecdhqy oblhqbmaus (ezkgtiwddp ) |
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