Alternatives to Praziquantel for the Prevention and Control of Schistosomiasis Thomas Spangenberg* Cite This: ACS Infect. Dis. 2021, 7, 939-942 Read Online ACCESS Metrics & More Article Recommendations ABSTRACT: Schistosomiasis, a neglected tropical disease provoked by infection with parasitic blood flukes of the genus Schistosoma,affects almost 240 million people worldwide, and more than 700 million people live in endemic areas. However, 40 years after the approval of praziquantel as an anthelmintic drug, the pipeline is nearly empty, and no other therapeutic alternative has reached the market. In its roadmap to “eliminate Schistosomiasis as a public health problem by 2030”, the World Health Organization calls for the development of new therapeutic interventions. A viewpoint on the learnings from praziquantel research as well as shaping the next generation of drugs is shared. S chistosomiasis or Bilharzia is a neglected tropical disease provoked by infection with parasitic blood flukes of the genus Schistosoma (Figure 1). The disease causes significant morbidity and mortality in subtropical and tropical regions of the world. In 2018, estimates show that at least 290.8 million people required preventive treatment, out of which 97.2 million had been treated with praziquantel (PZQ), an essential medicine for the treatment of helminths infections such as schistosomiasis (Figure 2). 1 The structure stems from a library of compounds originally developed by Merck (formerly E. Merck) as potential antipsychotics and then provided to Bayer for testing against worm parasites. This repurposing exercise led to the discovery of EMBAY-8440 in 1972, which was further codeveloped by both companies to become praziquantel, an anthelmintic drug approved in 1980. Forty years later, the pipeline is nearly empty, and no other therapeutic option to treat schistosomiasis has reached the market. Recently, in its roadmap to “eliminate Schistosomiasis as a public health problem by 2030”, the World Health Organization (WHO) calls for the development of new interventions, including alternatives to PZQ. 2 ■ WHY DOES THE COMMUNITY NEED TREATMENT ALTERNATIVES? With the WHO recommended dose of 40 mg/kg, PZQ achieved cure rates (CR) of 73.6% (S. hematobium), 76.4% (S. mansoni), Special Issue: Gut Pathogens Received: July 30, 2020 Published: August 21, 2020 Figure 1. Schistosoma spp lifecycle and opportunities for therapeutic inervention. Figure 2. Structure of (R)-praziquantel. Viewpoint pubs.acs.org/journal/aidcbc © 2020 American Chemical Society 939 https://dx.doi.org/10.1021/acsinfecdis.0c00542 ACS Infect. Dis. 2021, 7, 939−942 Downloaded via 171.243.71.223 on July 26, 2023 at 04:23:06 (UTC). See https://pubs.acs.org/sharingguidelines for options on how to legitimately share published articles.
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