Epsiprantel, a new tapeworm remedy. Preliminary efficacy studies in dogs and cats

Manger, Brian R.; Brewer, M. D.

doi:10.1016/0007-1935(89)90038-9

Cited by 14 publications

(5 citation statements)

References 3 publications

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“…For treatment of cestode and trematode infections, praziquantel (PZQ) is the drug of choice against most species [7]. For cestode-treatment, the alternatives available are epsiprantel that is exclusively applied in animals, and niclosamide, whose marketing status is currently discontinued [4,8]. PZQ is generally very well tolerated, even though it tastes bitter.…”

Section: Introductionmentioning

confidence: 99%

Development of a movement-based in vitro screening assay for the identification of new anti-cestodal compounds

Ritler¹,

Rufener²,

Sager³

et al. 2017

PLoS Negl Trop Dis

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Intestinal cestodes are infecting millions of people and livestock worldwide, but treatment is mainly based on one drug: praziquantel. The identification of new anti-cestodal compounds is hampered by the lack of suitable screening assays. It is difficult, or even impossible, to evaluate drugs against adult cestodes in vitro due to the fact that these parasites cannot be cultured in microwell plates, and adult and larval stages in most cases represent different organisms in terms of size, morphology, and metabolic requirements. We here present an in vitro-drug screening assay based on Echinococcus multilocularis protoscoleces, which represent precursors of the scolex (hence the anterior part) of the adult tapeworm. This movement-based assay can serve as a model for an adult cestode screen. Protoscoleces are produced in large numbers in Mongolian gerbils and mice, their movement is measured and quantified by image analysis, and active compounds are directly assessed in terms of morphological effects. The use of the 384-well format minimizes the amount of parasites and compounds needed and allows rapid screening of a large number of chemicals. Standard drugs showed the expected dose-dependent effect on movement and morphology of the protoscoleces. Interestingly, praziquantel inhibited movement only partially within 12 h of treatment (at concentrations as high as 100 ppm) and did thus not act parasiticidal, which was also confirmed by trypan blue staining. Enantiomers of praziquantel showed a clear difference in their minimal inhibitory concentration in the motility assay and (R)-(-)-praziquantel was 185 times more active than (S)-(-)-praziquantel. One compound named MMV665807, which was obtained from the open access MMV (Medicines for Malaria Venture) Malaria box, strongly impaired motility and viability of protoscoleces. Corresponding morphological alterations were visualized by scanning electron microscopy, and demonstrated that this compound exhibits a mode of action clearly distinct from praziquantel. Thus, MMV665807 represents an interesting lead for further evaluation.

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Section: Introductionmentioning

confidence: 99%

Development of a movement-based in vitro screening assay for the identification of new anti-cestodal compounds

Ritler¹,

Rufener²,

Sager³

et al. 2017

PLoS Negl Trop Dis

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“…Liver flukes from the genus Fasciola are insensitive to PZQ and epsiprantel [ 2 , 26 , 27 ]. Human fascioliasis is refractory to treatment by PZQ [ 28 , 29 ].…”

Section: Introductionmentioning

confidence: 99%

“…Fasciola TRPM PZQ provides a clear molecular explanation for the insensitivity of these liver flukes to PZQ. Liver flukes from the genus Fasciola are insensitive to PZQ and epsiprantel [2,26,27]. Human fascioliasis is refractory to treatment by PZQ [28,29].…”

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confidence: 99%

Progress interrogating TRPMPZQ as the target of praziquantel

Marchant

2024

PLoS Negl Trop Dis

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The drug praziquantel (PZQ) has served as the long-standing drug therapy for treatment of infections caused by parasitic flatworms. These encompass diseases caused by parasitic blood, lung, and liver flukes, as well as various tapeworm infections. Despite a history of clinical usage spanning over 4 decades, the parasite target of PZQ has long resisted identification. However, a flatworm transient receptor potential ion channel from the melastatin subfamily (TRPMPZQ) was recently identified as a target for PZQ action. Here, recent experimental progress interrogating TRPMPZQ is evaluated, encompassing biochemical, pharmacological, genetic, and comparative phylogenetic data that highlight the properties of this ion channel. Various lines of evidence that support TRPMPZQ being the therapeutic target of PZQ are presented, together with additional priorities for further research into the mechanism of action of this important clinical drug.

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“…In veterinary medicine, control of D. caninum involves treating dogs and cats with praziquantel 5 or epsiprantel 6 alone, or in combination with other anthelmintics for broadspectrum coverage. [7][8][9][10] Praziquantel is also used to treat human D. caninum infections after parasitological identification of the cestode.…”

Section: Introductionmentioning

confidence: 99%

Praziquantel Resistance in the Zoonotic Cestode Dipylidium caninum

Chelladurai

Kifleyohannes

Scott

et al. 2018

The American Journal of Tropical Medicine and Hygiene

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is a cosmopolitan cestode infecting dogs, cats, and humans. Praziquantel is a highly effective cestocidal drug and resistance in adult cestodes has not been reported. From 2016 to 2018, a population of dogs with cestode infections that could not be eliminated despite multiple treatments with praziquantel or epsiprantel was identified. Cases of were clinically resistant to praziquantel and could not be resolved despite increasing the dose, frequency, and duration of treatment. Resistant isolates were identified and characterized by sequencing the 28S, 12S, and voltage-gated calcium channel beta subunit genes. Cases were only resolved following treatment with nitroscanate or a compounded pyrantel/praziquantel/oxantel product. Clinicians should be aware of this alarming development as treatment options for cestodes are limited in both human and veterinary medicine.

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Epsiprantel, a new tapeworm remedy. Preliminary efficacy studies in dogs and cats

Cited by 14 publications

References 3 publications

Development of a movement-based in vitro screening assay for the identification of new anti-cestodal compounds

Development of a movement-based in vitro screening assay for the identification of new anti-cestodal compounds

Progress interrogating TRPMPZQ as the target of praziquantel

Praziquantel Resistance in the Zoonotic Cestode Dipylidium caninum

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