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Eluxadoline

Eluxadoline Struktur
864821-90-9
CAS-Nr.
864821-90-9
Englisch Name:
Eluxadoline
Synonyma:
CS-2329;EOS-61916;Eluxadolin;Eluxadoline;API-Diarrhea;JNJ 27018966;The yi lu Lin;Eluxadoline 13CD4;Eluxadoline (Viberzi);Eluxadoline(JNJ 27018966)
CBNumber:
CB12723517
Summenformel:
C32H35N5O5
Molgewicht:
569.65
MOL-Datei:
864821-90-9.mol

Eluxadoline Eigenschaften

Schmelzpunkt:
>180°C (dec.)
Siedepunkt:
834.2±65.0 °C(Predicted)
Dichte
1.284±0.06 g/cm3(Predicted)
storage temp. 
Refrigerator
L?slichkeit
DMSO (Slightly), Methanol (Slightly)
Aggregatzustand
Solid
pka
4.01±0.10(Predicted)
Farbe
White to Off-White
InChIKey
QFNHIDANIVGXPE-FNZWTVRRSA-N
SMILES
C(O)(=O)C1=CC(CN(C(=O)[C@@H](N)CC2=C(C)C=C(C(N)=O)C=C2C)[C@H](C2NC(C3=CC=CC=C3)=CN=2)C)=CC=C1OC
CAS Datenbank
864821-90-9
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
DEA Controlled Substances CSCN: 9725
CAS SCH: IV
NARC: N
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H361 Kann vermutlich die Fruchtbarkeit beeintr?chtigen oder das Kind im Mutterleib sch?digen. Reproduktionstoxizit?t Kategorie 2 Warnung P201, P202, P281, P308+P313, P405,P501
Sicherheit
P201 Vor Gebrauch besondere Anweisungen einholen.
P202 Vor Gebrauch alle Sicherheitshinweise lesen und verstehen.
P281 Vorgeschriebene pers?nliche Schutzausrüstung verwenden.
P308+P313 BEI Exposition oder falls betroffen: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen.
P405 Unter Verschluss aufbewahren.
P501 Inhalt/Beh?lter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

Eluxadoline Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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.

Verwenden

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

Definition

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.

Pharmakokinetik

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.

Eluxadoline Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Eluxadoline Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 174)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
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 474 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 32956 60
career henan chemical co
+86-0371-86658258 +8613203830695
sales@coreychem.com China 29880 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

  • JNJ 27018966
  • Eluxadoline
  • 5-(((S)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)-N-((S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl)propanamido)methyl)-2-methoxybenzoic acid
  • Eluxadolin
  • API-Diarrhea
  • Benzoic acid, 5-[[[(2S)-2-amino-3-[4-(aminocarbonyl)-2,6-dimethylphenyl]-1-oxopropyl][(1S)-1-(5-phenyl-1H-imidazol-2-yl)ethyl]amino]methyl]-2-methoxy-
  • CS-2329
  • Eluxadoline (Viberzi)
  • EOS-61916
  • 5-(((S)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)-N-((S)-1-(5-phenyl-1H-imidazol-2-yl)ethyl)propanamido)methyl)-2-methoxybenzoic acid
  • Eluxadoline(JNJ 27018966)
  • Eluxadoline 13CD4
  • The yi lu Lin
  • 5-{[(2S)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)-N-[(1S)-1-(5-phenyl-1H-imidazol-2-yl)ethyl]propanamido]methyl}-2-methoxybenzoic acid
  • 864821-90-9
  • API
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