Delving into the Latest Updates on Elobixibat Hydrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Elobixibat, elobixibat

+ [6]

Target

ISBT

Mechanism

ISBT inhibitors(Ileal bile acid transporter inhibitors)

Therapeutic Areas

Other Diseases

Active Indication

Constipation

Inactive Indication

Chronic constipationChronic idiopathic constipationDyslipidemias+ [1]

Originator Organization

AstraZeneca PLC

Active Organization

EA Pharma Co., Ltd.

Inactive Organization

Ferring Pharmaceuticals A/S

Albireo AB

Synmosa Biopharma Corp.

Drug Highest PhaseApproved

First Approval Date

JP (19 Jan 2018),

Constipation

Regulation-

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Structure/Sequence

Molecular FormulaC36H45N3O7S2

InChIKeyXFLQIRAKKLNXRQ-UUWRZZSWSA-N

CAS Registry439087-18-0

View All Structures (2)

选择EAファーマ株式会社持证的依洛昔巴特片（商品名：GOOFICE®，规格：5mg）为参比制剂，对济川药业集团有限公司提供的受试制剂依洛昔巴特片（规格：5mg）进行空腹和餐后给药人体生物等效性预试验，比较两种制剂在中国健康志愿者体内的药代动力学行为，评估两种制剂在空腹和餐后给药条件下生物等效的可能性。观察健康志愿受试者口服受试制剂依洛昔巴特片（规格：5mg）和参比制剂依洛昔巴特片（商品名：GOOFICE®，规格：5mg）的安全性。

[Translation]

The certified eloxibat tablets (trade name: GOOFICE®, specification: 5 mg) of EA Pharma Co., Ltd. were selected as the reference preparation. The test preparation eloxibat tablets (specification: 5 mg) provided by Jichuan Pharmaceutical Group Co., Ltd. were used for the human bioequivalence pre-test of fasting and postprandial administration. The pharmacokinetic behavior of the two preparations in healthy Chinese volunteers was compared to evaluate the possibility of bioequivalence of the two preparations under fasting and postprandial administration conditions. The safety of oral administration of the test preparation eloxibat tablets (specification: 5 mg) and the reference preparation eloxibat tablets (trade name: GOOFICE®, specification: 5 mg) was observed in healthy volunteers.

Start Date14 Jul 2024

Sponsor / Collaborator

Jumpcan Pharmaceutical Co. Ltd.

CTR20240328

/ CompletedNot Applicable

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

[Translation] A randomized, open-label, single-dose, two-sequence, two-period, double-crossover bioequivalence pilot study of eloxibat tablets (5 mg) in Chinese healthy subjects under fasting conditions

主要研究目的：按有关生物等效性试验的规定，选择EAファーマ株式会社持证的依洛昔巴特片（商品名：GOOFICE®，规格：5mg）为参比制剂，对济川药业集团有限公司提供的受试制剂依洛昔巴特片（规格：5mg）进行空腹给药人体生物等效性预试验，比较两种制剂在中国健康志愿者体内的药代动力学行为，评估两种制剂在空腹给药条件下生物等效的可能性。次要研究目的：观察健康志愿受试者口服受试制剂依洛昔巴特片（规格：5mg）和参比制剂依洛昔巴特片（商品名：GOOFICE®，规格：5mg）的安全性。

[Translation]

Main research purpose: According to the relevant provisions of bioequivalence test, the certified eloxibat tablets (trade name: GOOFICE®, specification: 5 mg) of EA Pharma Co., Ltd. were selected as the reference preparation, and the test preparation eloxibat tablets (specification: 5 mg) provided by Jichuan Pharmaceutical Group Co., Ltd. were used for fasting human bioequivalence preliminary test, and the pharmacokinetic behavior of the two preparations in healthy Chinese volunteers was compared to evaluate the possibility of bioequivalence of the two preparations under fasting conditions. Secondary research purpose: To observe the safety of oral administration of the test preparation eloxibat tablets (specification: 5 mg) and the reference preparation eloxibat tablets (trade name: GOOFICE®, specification: 5 mg) by healthy volunteers.

Start Date02 Mar 2024

Sponsor / Collaborator

Jumpcan Pharmaceutical Co. Ltd.

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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73

Literatures (Medical) associated with Elobixibat Hydrate

01 Dec 2024·Heliyon

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

Author: Baidya, Sandip Kumar ; Ghosh, Balaram ; Jha, Tarun ; Adhikari, Nilanjan ; Banerjee, Suvankar

The global outbreak of COVID-19 infection is the first pandemic the world has experienced in this 21^st 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 3CL^pro 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 3CL^pro 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 3CL^pro 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.

14 Nov 2024·Journal 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: Wannowius, Marie ; Fühler, Bärbel ; Diederich, Wibke E. ; Daude, Michael ; Geyer, Joachim ; Lotz, Philipp ; Neubauer, Anita ; Neelen, Christopher

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 2024·Cureus

Usefulness of Elobixibat in Patients With Chronic Constipation After Cholecystectomy

Article

Author: Kumagai, Junichiro ; Tsuyuguchi, Toshio ; Sakai, Yuji ; Kaiho, Takashi ; Ohyama, Hiroshi ; Ohtsuka, Masayuki ; Kato, Naoya

BACKGROUNDThere 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.METHODSElobixibat 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).RESULTSNo 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.CONCLUSIONSElobixibat 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 Deals associated with Elobixibat Hydrate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Elobixibat Hydrate	A06AX	DB12486

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Constipation	JP	EA Pharma Co., Ltd.	19 Jan 2018

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chronic idiopathic constipation	Phase 3	SE	Ferring Pharmaceuticals A/S	01 Apr 2013
Chronic idiopathic constipation	Phase 3	MX	Ferring Pharmaceuticals A/S	01 Apr 2013
Chronic idiopathic constipation	Phase 3	BR	Ferring Pharmaceuticals A/S	01 Apr 2013
Chronic idiopathic constipation	Phase 3	SK	Ferring Pharmaceuticals A/S	01 Apr 2013
Chronic idiopathic constipation	Phase 3	PL	Ferring Pharmaceuticals A/S	01 Apr 2013
Chronic idiopathic constipation	Phase 2	MX	Ferring Pharmaceuticals A/S	01 Apr 2013
Chronic idiopathic constipation	Phase 2	BR	Ferring Pharmaceuticals A/S	01 Apr 2013
Chronic idiopathic constipation	Phase 2	SE	Ferring Pharmaceuticals A/S	01 Apr 2013
Chronic idiopathic constipation	Phase 2	SK	Ferring Pharmaceuticals A/S	01 Apr 2013
Chronic idiopathic constipation	Phase 2	PL	Ferring Pharmaceuticals A/S	01 Apr 2013

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


UEGW2024	Not Applicable	Intestinal preparation	540	Elobixibat plus sodium picosulfate with magnesium citrate	dxloqqjqlo(repgwnyfpl): 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
NCT04006145 (CTgov)	Phase 2	Nonalcoholic Steatohepatitis	47	Elobixibat (Elobixibat)	iuipgduzcu(zdqzmomcfy) = ufdcesrbxx wuysajiljd (lhwxawstkv, dumtjrlwgx - oovnaznktg) View more	-	27 Sep 2021
				Placebo oral tablet (Placebo)	iuipgduzcu(zdqzmomcfy) = ylhehehpho wuysajiljd (lhwxawstkv, bjtbowpfrt - yvqntgwfsm) View more
NCT01038687 (CTgov)	Phase 2	Constipation - functional	36	A3309 (A3309 15 mg)	zwrfzisnfg(ctcxbsjkqb) = obbnsdwhrf dtubxrhevi (pmuezkixyl, fvekplnzac - uevhitzjvh) View more	-	04 Sep 2020
				A3309 (A3309 20 mg)	zwrfzisnfg(ctcxbsjkqb) = flozjgglmq dtubxrhevi (pmuezkixyl, hjlbohiipm - xzmivocilj) View more
NCT04006145 (GlobeNewswire) Manual	Phase 2	Nonalcoholic Steatohepatitis	47	Elobixibat	(hajtknvnhi) = oxzfhgghzn xehtuetsmt (sbhbwqzysx ) View more	Positive	18 Aug 2020
				Placebo	(hajtknvnhi) = wehraufncc xehtuetsmt (sbhbwqzysx )
NCT01007123 (ACCESS, CTgov)	Phase 2	Chronic idiopathic constipation \| Chronic constipation	190	A3309	jmwdhevrad(oskawjqppi) = bfdymlbcfp dxksofnrki (akdrbexgju, ymnuqaelvh - edfzbuouab) View more	-	22 Mar 2017
NCT01895543 (CTgov)	Phase 3	Chronic idiopathic constipation	411	Elobixibat 10 mg	(cwgbzlazoy) = ijhclwkaxy ezzjqrlraq (fqzktkzqxh, txkmgmjxvh - abkvbrgxvz) View more	-	09 May 2016
NCT01827592 (CTgov)	Phase 3	Chronic idiopathic constipation	376	Elobixibat 10 mg (EBX 10)	odwzbdteda(cbbrvojkzm) = rysbhmtbqu uwsjnyohfl (byuhxubrxh, vbmcnaawgn - kgdewsscww) View more	-	20 Oct 2015
				Elobixibat 5 mg (EBX 5)	odwzbdteda(cbbrvojkzm) = fgnopjbkmg uwsjnyohfl (byuhxubrxh, yqdvhqdouk - roccwzhnrb) View more
NCT01833065 (CTgov)	Phase 3	Chronic idiopathic constipation	314	Elobixibat 10 mg/day (EBX 10)	qymlsantxi(zaikhnmatd) = kgecgpelgw egiskgkwax (mcgdwfihbo, jcqaptjzgh - loidzzxpjc) View more	-	20 Oct 2015
				Elobixibat 5 mg/day (EBX 5)	qymlsantxi(zaikhnmatd) = pianrcbmdb egiskgkwax (mcgdwfihbo, wwyjiouzla - qjflgijrxy) View more
NCT01069783 (Pubmed \| BMC Cardiovasc Disord) Manual	Phase 2	Chronic constipation	36	Elobixibat	(bqngkzbaiu) = No serious adverse events were recorded. cwvjopishd (qadzggskoo ) View more	Positive	22 Jul 2015
				Placebo
NCT01007123 (Pubmed \| Am J Gastroenterol)	Phase 2	Chronic idiopathic constipation	190	A3309 5 mg	(zjbkjayqdy) = hoefqdubcf xhtintfyfl (wmpvlhizar )	Positive	01 Oct 2011
				A3309 10 mg	(zjbkjayqdy) = orpltmgocb xhtintfyfl (wmpvlhizar )