生物活性

• 靶点	Enkephalinase IC50:4.5μM

• 描述Racecadotril, via its active metabolite thiorphan, is an inhibitor of the enzyme neutral endopeptidase (NEP, EC 3.4.24.11), thereby increasing exposure to NEP substrates including enkephalins and atrial natriuretic peptide (ANP). Upon oral administration racecadotril is rapidly and effectively converted into the active metabolite thiorphan, which does not cross the blood-brain-barrier^[3]. Orally administered Racecadotril (100 mg/kg) shows efficacy in a rat model of castor oil-induced diarrhea^[4]. Racecadotril is used in the treatment of acute diarrhoea. It prevents the degradation of endogenous opioids (enkephalins), thereby reducing hypersecretion of water and electrolytes into the intestinal lumen. In well controlled trials, racecadotril had efficacy similar to that of loperamide and was generally as effective as loperamide-oxide. In well controlled trials, racecadotril had efficacy similar to that of loperamide and was generally as effective as loperamide-oxide^[5]. Racecadotril is more efficacious than other treatments except for loperamide and has a tolerability similar to placebo and better than loperamide^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02125604	Relapsing-Remitting Multiple S... more >>clerosis Collapse <<	Phase 4	Completed	-	Germany ... more >> Research Site Augsburg, Germany Research Site Bamburg, Germany Research Site Bayreuth, Germany Research Site Berlin, Germany Research Site Bochum, Germany Research Site Bonn, Germany Research Site Erbach, Germany Research Site Erlangen, Germany Research Site Freiburg, Germany Research Site Hamburg, Germany Research Site Leipzig, Germany Research Site Marburg, Germany Research Site Minden, Germany Research Site Mittweida, Germany Research Site Munchen, Germany Research Site Munster, Germany Research Site Osnabruck, Germany Research Site Potsdam, Germany Research Site Siegen, Germany Collapse <<
  NCT03005821	Diarrhea	Not Applicable	Recruiting	September 30, 2019	China, Guangdong ... more >> Dongguan Kanghua Hospital Recruiting Dongguan, Guangdong, China, 523080 Contact: Lingjia Yin, Physician    8613112843921    632608836@qq.com Collapse <<
  NCT00940290	-	-	Completed	-	-

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• 参考文献

• [1] Marion Eberlin, Tobias Muck, et al. A Comprehensive Review of the Pharmacodynamics, Pharmacokinetics, and Clinical Effects of the Neutral Endopeptidase Inhibitor Racecadotril. Front Pharmacol. 2012; 3: 93.

  [2] Wu HT, Chang CK, et al. Increase of plasma insulin by racecadotril, an inhibitor of enkephalinase, in Wistar rats. Horm Metab Res. 2010 Apr;42(4):261-7.

  [3] Eberlin M, Mück T, Michel MC. A comprehensive review of the pharmacodynamics, pharmacokinetics, and clinical effects of the neutral endopeptidase inhibitor racecadotril. Front Pharmacol. 2012 May 30;3:93

  [4] Griggs DW, Prinsen MJ, Oliva J, Campbell MA, Arnett SD, Tajfirouz D, Ruminski PG, Yu Y, Bond BR, Ji Y, Neckermann G, Choy RK, de Hostos E, Meyers MJ. Pharmacologic Comparison of Clinical Neutral Endopeptidase Inhibitors in a Rat Model of Acute Secretory Diarrhea. J Pharmacol Exp Ther. 2016 May;357(2):423-31

  [5] Matheson AJ, Noble S. Racecadotril. Drugs. 2000 Apr;59(4):829-35; discussion 836-7

  [6] Eberlin M, Chen M, Mueck T, Däbritz J. Racecadotril in the treatment of acute diarrhea in children: a systematic, comprehensive review and meta-analysis of randomized controlled trials. BMC Pediatr. 2018 Apr 3;18(1):124

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