Delving into the Latest Updates on Trimebutine Maleate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

2-Dimethylamino-2-phenylbutyl 3,4,5-trimethoxybenzoat, Modulon SR, Trimebutine

+ [11]

Target

Opioid receptors x mAChRs

Mechanism

Opioid receptors agonists(Opioid receptors agonists), mAChRs antagonists(Muscarinic acetylcholine receptor antagonists)

Therapeutic Areas

Digestive System Disorders

Active Indication

GastritisIrritable Bowel Syndrome

Inactive Indication-

Originator Organization-

Active Organization

Xinhe Yuansheng Pharmaceutical Co., Ltd.

Inactive Organization

Labopharm, Inc.

Drug Highest PhaseApproved

First Approval Date

JP (15 Feb 1984),

GastritisIrritable Bowel Syndrome

Regulation-

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Structure

Molecular FormulaC22H29NO5

InChIKeyLORDFXWUHHSAQU-UHFFFAOYSA-N

CAS Registry39133-31-8

View All Structures (2)

The goal of this clinical trial is to test the effectiveness of trimebutine and probiotics in treating Functional Abdominal Pain Disorders (FAPD) in a pediatric population. The main questions it aims to answer are: Is trimebutine effective in reducing the symptoms of FAPD in children? Are probiotics effective in reducing the symptoms of FAPD in children? Participants will be randomly assigned to one of three treatment groups (trimebutine/probiotics, probiotics/placebo, or trimebutine/placebo). Undergo measurements for pain and other relevant metrics at the start of the study, after 4 weeks, and after 8 weeks.
Researchers will compare the trimebutine/probiotics group to the probiotics/placebo and the trimebutine/placebo groups to see if there are significant differences in the efficacy of these treatments in reducing symptoms of FAPD in children.

Start Date01 Sep 2024

Sponsor / Collaborator

Unversity of Colima

CTR20242206 / CompletedNot Applicable

马来酸曲美布汀片人体生物等效性研究

[Translation] Study on the bioequivalence of trimebutine maleate tablets in healthy volunteers

本试验旨在研究单次空腹和餐后口服浙江诺得药业有限公司研制、生产的马来酸曲美布汀片（100 mg）的药代动力学特征；以田辺三菱製薬株式会社持证、生产的马来酸曲美布汀片（Cerekinon®，100 mg）为参比制剂，比较两制剂中药动学参数Cmax、AUC0-t、AUC0-∞，评价两制剂的人体生物等效性。

[Translation]

The purpose of this trial was to study the pharmacokinetic characteristics of trimebutine maleate tablets (100 mg) administered on an empty stomach and after meals in a single dose, administered by Zhejiang Node Pharmaceutical Co., Ltd.; Trimebutine maleate tablets (Cerekinon®, 100 mg) produced by the company are used as reference preparations. The pharmacokinetic parameters Cmax, AUC0-t, and AUC0-∞ of the two preparations are compared to evaluate the human bioequivalence of the two preparations. .

Start Date14 Jul 2024

Sponsor / Collaborator

Zhejiang NuoDe Pharmaceutical Co., Ltd.

CTR20234149 / CompletedNot Applicable

马来酸曲美布汀片在健康成年受试者中空腹状态下生物等效性试验

[Translation] Bioequivalence study of trimebutine maleate tablets in healthy adult subjects under fasting condition

主要目的：考察空腹条件下单次口服受试制剂马来酸曲美布汀片（规格：0.1 g）（浙江华海药业股份有限公司生产）与参比制剂马来酸曲美布汀片（商品名：Cerekinon，规格：100 mg）（田边三菱制药株式会社持证）在健康受试者体内的药代动力学特征，评价空腹条件下口服两种制剂的生物等效性。次要目的：考察受试制剂马来酸曲美布汀片和参比制剂马来酸曲美布汀片（Cerekinon）在健康受试者中的安全性。

[Translation]

Primary objective: To investigate the pharmacokinetic characteristics of the test preparation trimebutine maleate tablets (specification: 0.1 g) (produced by Zhejiang Huahai Pharmaceutical Co., Ltd.) and the reference preparation trimebutine maleate tablets (trade name: Cerekinon, specification: 100 mg) (certified by Mitsubishi Tanabe Pharma Co., Ltd.) in healthy subjects after a single oral administration under fasting conditions, and to evaluate the bioequivalence of the two preparations when taken orally under fasting conditions. Secondary objective: To investigate the safety of the test preparation trimebutine maleate tablets and the reference preparation trimebutine maleate tablets (Cerekinon) in healthy subjects.

Start Date08 Jan 2024

Sponsor / Collaborator

Zhejiang Huahai Pharmaceutical Co., Ltd.

100 Clinical Results associated with Trimebutine Maleate

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100 Translational Medicine associated with Trimebutine Maleate

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100 Patents (Medical) associated with Trimebutine Maleate

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243

Literatures (Medical) associated with Trimebutine Maleate

01 May 2024·Drug Development Research

In vitro and in silico investigation of FDA‐approved drugs to be repurposed against Alzheimer's disease

Article

Author: Akkaya, Didem ; Seyhan, Gökçe ; Barut, Burak ; Sari, Suat

AbstractAlzheimer's disease (AD), one of the main causes of dementia, is a neurodegenerative disorder. Cholinesterase inhibitors are used in the treatment of AD, but prolonged use of these drugs can lead to serious side effects. Drug repurposing is an approach that aims to reveal the effectiveness of drugs in different diseases beyond their clinical uses. In this work, we investigated in vitro and in silico inhibitory effects of 11 different drugs on cholinesterases. The results showed that trimebutine, theophylline, and levamisole had the highest acetylcholinesterase inhibitory actions among the tested drugs, and these drugs inhibited by 68.70 ± 0.46, 53.25 ± 3.40, and 44.03 ± 1.20%, respectively at 1000 µM. In addition, these drugs are bound to acetylcholinesterase via competitive manner. Molecular modeling predicted good fitness in acetylcholinesterase active site for these drugs and possible central nervous system action for trimebutine. All of these results demonstrated that trimebutine was determined to be the drug with the highest potential for use in AD.

30 Apr 2024·Journal of Neurogastroenterology and Motility

Effect of Trimebutine and Rifaximin on Breath Hydrogen and Methane by Glucose Breath Test in Patients With Functional Bloating: A Randomized Double-blind Clinical Trial

Article

Author: Paik, Chang-Nyol ; Kim, Yeon-Ji ; Song, Do Seon ; Lee, Ji Min ; Jo, Ik Hyun

Background/AimsDrugs that stabilize intestinal motility may improve the efficacy of nonabsorbable antibiotics, such as rifaximin, against small intestinal bacterial overgrowth (SIBO). We compared the efficacy of rifaximin alone with that of its combination with trimebutine maleate against SIBO.MethodsWe performed a randomized double-blind placebo-controlled trial (https://cris.nih.go.kr, no. KCT0004836) that included patients with functional bloating, no constipation, and SIBO using the hydrogen (H₂)-methane (CH₄) glucose breath test (GBT). Patients were randomized into 2 groups in a 1:1 ratio, namely rifaximin (1200 mg/day) + trimebutine maleate (600 mg/day) group and rifaximin + placebo group, for 2 weeks. Patients completed a symptom questionnaire and underwent a GBT at baseline and at 1 month after treatment withdrawal. The primary outcome was SIBO eradication. The secondary outcomes included changes in the concentrations of exhaled gases, symptoms, and presence of adverse events.ResultsThe complete eradication rate of SIBO was 35.9% (14/39) in the rifaximin group, and 34.1% (14/41) in the combined group with no significant differences. In both groups, no significant differences were observed in GBT profiles before and after the treatment, respectively. However total breath H₂ and CH₄ concentration were conspicuously decreased in the combined group after treatment. The combined group exhibited substantial relief of bloating. The adverse events were similar in the 2 groups.ConclusionWhile the combination therapy was not superior over rifaximin alone for SIBO eradication, it improves the symptom of bloating with numerically reducing the concentration of breath H₂/CH₄.

24 Apr 2024·Biological and Pharmaceutical Bulletin

Fentanyl Analogs Exert Antinociceptive Effects <i>via</i> Sodium Channel Blockade in Mice

Article

Author: Takagi, Miho ; Takahashi, Hideyo ; Arita, Hironobu ; Ogawa, Natsuki ; Kasai, Satoka ; Yoshizawa, Kazumi ; Takahashi, Yukino ; Makino, Kosho

The formalin test is one approach to studying acute pain in rodents. Similar to formalin, injection with glutamate and veratrine can also produce a nociceptive response. This study investigated whether opioid-related compounds could suppress glutamate- and veratrine-induced nociceptive responses in mice at the same dose. The administration of morphine (3 mg/kg), hydromorphone (0.4 mg/kg), or fentanyl (0.03 mg/kg) suppressed glutamate-induced nociceptive response, but not veratrine-induced nociceptive response at the same doses. However, high doses of morphine (10 mg/kg), hydromorphone (2 mg/kg), or fentanyl (0.1 mg/kg) produced a significant reduction in the veratrine-induced nociceptive response. These results indicate that high doses are required when using morphine, hydromorphone, or fentanyl for sodium channel-related neuropathic pain, such as ectopic activity. As a result, concerns have arisen about overdose and abuse if the dose of opioids is steadily increased to relieve pain. In contrast, trimebutine (100 mg/kg) and fentanyl analog isobutyrylfentanyl (iBF; 0.1 mg/kg) suppressed both glutamate- and veratrine-induced nociceptive response. Furthermore, nor-isobutyrylfentanyl (nor-iBF; 1 mg/kg), which is a metabolite of iBF, suppressed veratrine-induced nociceptive response. Besides, the optimal antinociceptive dose of iBF, unlike fentanyl, only slightly increased locomotor activity and did not slow gastrointestinal transit. Cancer pain is a complex condition driven by inflammatory, neuropathic, and cancer-specific mechanisms. Thus, iBF may have the potential to be a superior analgesic than fentanyl.

100 Deals associated with Trimebutine Maleate

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External Link

KEGG	Wiki	ATC	Drug Bank
D01500	Trimebutine Maleate	A03AA05	DB09089

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Gastritis	JP	-	15 Feb 1984
Irritable Bowel Syndrome	JP	-	15 Feb 1984

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Irritable Bowel Syndrome	Phase 1	CA	Labopharm, Inc.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


WJOG11318B (ESMO2021)	Phase 2	Hormone receptor positive HER2 negative breast cancer	-	Bifidobacterial	(rzxaovemdx) = bzuwlbvvfb styhgtwyku (zffzvwwowd ) View more	-	16 Sep 2021
				Bifidobacterial and Trimebutine Maleate	(rzxaovemdx) = upbikinztl styhgtwyku (zffzvwwowd ) View more