Praziquantel – 50 Years of Research

Author:

Waechtler Andreas1,Cezanne Bertram1ORCID,Maillard David1ORCID,Sun Rui2,Wang Shaofang3,Wang Jihua3,Harder Achim4

Affiliation:

1. Central Process Development Department (EL-OTS) Merck KGaA Frankfurter Str. 250 64293 Darmstadt Germany

2. R&D Department Valiant Pharmaceutical Co. Ltd. Taiyuan Road No. 60, YEDA Yantai Shandong 264006 China

3. Technical Department Valiant Corporation Ltd. Wuzhishan Road No. 11, YEDA, Yantai Shandong 264006 China

4. Department WE Biology Institute of Biology Heinrich-Heine University Düsseldorf Universitätsstraße 1 40225 Düsseldorf Germany

Abstract

AbstractInvestigations on praziquantel (PZQ) started fifty years ago by a cooperation between Bayer AG and Merck KGaA. Until today PZQ is the drug of choice for schistosomiasis in human medicine and used in many combinations with antinematode drugs in veterinary medicine. The Sm.TRPMPZQ, a Ca2+ ‐permeable transient receptor potential (TRP) channel, has been discovered as primary target of PZQ during the last decade. Furthermore, there is a short overview of routes of large‐scale synthesis of racemic and pure (R)‐PZQ. Until now racemic PZQ is used in veterinary and human medicine. In 2012 the Pediatric Praziquantel Consortium started PZQ chemistry and process development of pure (R)‐PZQ for human application. It is hoped that (R)‐PZQ will become available for pediatric use soon. The knowledge of the binding pocket of PZQ in Sm.TRPMPZQ allows to design synthesis of PZQ‐derivatives of the next generation for a target‐site directed screening. A similar screening should also be started for Fasciola hepatica TRPMPZQ.

Funder

Global Health Innovative Technology Fund

Publisher

Wiley

Subject

Organic Chemistry,General Pharmacology, Toxicology and Pharmaceutics,Molecular Medicine,Drug Discovery,Biochemistry,Pharmacology

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