일루카도린

일루카도린 속성

일루카도린 C화학적 특성, 용도, 생산

개요

Eluxadoline, originally developed by Janssen and currently marketed by Allergan (formerly Actavis), was approved in May 2015 by the FDA for the treatment of diarrhea-predominant irritable bowel syndrome (IBS-D). Eluxadoline, an orally dosed agent, employs a unique mechanism for IBS-D treatment, as it functions simultaneously as a μ- and κ-opioid receptor agonist and a δ- opioid receptor antagonist, leading to a first-in-class therapy for treatment of IBS-D. Specifically, in animal studies, eluxadoline was found to interact with opioid receptors in the gut, inhibiting neurogenically mediated secretion and reducing intestinal contractility. Additionally, the treatment led to a decrease in stress-induced acceleration of upper GI transit without causing rebound constipation, earning its mark as a first-line therapeutic treatment for IBS-D. In two phase III clinical trials of over 2400 patients with IBS-D, patients taking eluxadoline showed a greater improvement toward the end point (≥30% improvement from their baseline IBS-D score on at least 50% of days treated with eluxadoline) compared to patients treated with placebo.

용도

Eluxadoline is an orally-active drug used to reduce symptoms of irritable bowel syndrome such as diarrhea and abdominal pain.

정의

ChEBI: An amino acid amide obtained by the formal condensation of the carboxy group of 4-carbamoyl-2,6-dimethyl-L-phenylalanine with the secondary amino group of 2-methoxy-5-({[(1S)-1-(4-phenylimidazol-2-yl)ethyl]amino}methyl)ben oic acid. It has mixed opioid receptor activity and is used for treatment of irritable bowel syndrome with diarrhoea.

Pharmacokinetics

Following oral administration of 100 mg VIBERZI in healthy subjects, the Cmax of eluxadoline was approximately 2 to 4 ng/mL, and AUC was 12 to 22 ng. h/mL. Eluxadoline has approximately linear pharmacokinetics with no accumulation upon repeated twice-daily dosing. The variability of eluxadoline pharmacokinetic parameters ranges from 51% to 98%.
Absorption: The absolute bioavailability of eluxadoline has not been determined. The median Tmax value was 1.5 hours (1 to 8 hours) under fed conditions and 2 hours (range: 0.5 to 6 hours) under fasting conditions.
The administration of VIBERZI with a high-fat meal that contained approximately 800 to 1000 total calories, with 50% of calories derived from fat content, decreased the Cmax of eluxadoline by 50% and AUC by 60%.
Distribution: Plasma protein binding of eluxadoline was 81%.
Elimination: The mean plasma elimination half-life of eluxadoline ranged from 3.7 hours to 6 hours.
Metabolism: The metabolism of eluxadoline is not established. There is evidence that glucuronidation can occur to form an acyl glucuronide metabolite.
Excretion: Following a single oral dose of 300 mg [14C] eluxadoline in healthy male subjects, 82.2% of the total radioactivity was recovered in feces within 336 hours and less than 1% was recovered in urine within 192 hours.

일루카도린 준비 용품 및 원자재

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일루카도린 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Protheragen-ING	+16313385890	info@protheragen-ing.com	United States	3868	58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.	+86-18600796368 +86-18600796368	sales@sjar-tech.com	China	444	58
Capot Chemical Co.,Ltd.	+86-（0）57185586718 +86-13336195806	sales@capot.com	China	29791	60
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1803	55
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21634	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32957	60
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29881	58
Nanjing Dolon Biotechnology Co.,Ltd.	18905173768	sales@dolonchem.com	CHINA	2972	58
Hangzhou Cyanochem Co., Ltd.	+86 17788583750	sales@cyanochem.com	CHINA	281	58
Beijing Yibai Biotechnology Co., Ltd	0086-182-6772-3597	sales04@yibaibiotech.com	CHINA	419	58

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