Monepantel: the most studied new anthelmintic drug of recent years

Abstract

Monepantel (MOP), a new anthelmintic drug from a group of amino-acetonitrile derivatives, has been intensively studied during last years. Many authors examined this new drug from different perspectives, e.g. efficacy against different species and stages of parasites, mode of action, metabolism, pharmacokinetics, toxicity, resistance, ecotoxicity, etc. MOP is an anthelmintic for livestock (currently only sheep and goats), with molecular mode of action which is different to all other anthelmintics. MOP has a broad-spectrum of activity against gastrointestinal nematodes of sheep, including adults and L4 larvae of the most important species. The key feature of MOP is its full effectiveness against strains of nematodes resistant to benzimidazoles, levamisole, macrocyclic lactones and closantel. After oral administration, MOP is quickly absorbed into the bloodstream and quickly metabolized to MOP sulfone that has a similar efficacy as the parent molecule. Several other MOP metabolites formed in ovine hepatocytes were described. MOP and its metabolites are considered to be non-toxic to environment and its components, such as soil microflora, aquatic organisms, dung organisms, vegetation, etc. The aim of the presented review was not to collect all reported data but to bring an overview of various approaches in the study of MOP and to evaluate their principal results.

Comparison of biotransformation and efficacy of aminoacetonitrile anthelmintics in vitro

“…[25] Nowadays, the situation has become more problematic by increasing the occurrence of drug-resistant helminths. [14] In spite of this fact, only one representative of AADs, MOP, has been approved for veterinary practice which limits the choice for veterinarians. Contrary to other groups, only AADs are sufficiently effective against multi-resistant nematodes.…”

“…Contrary to other groups, only AADs are sufficiently effective against multi-resistant nematodes. [14] In spite of this fact, only one representative of AADs, MOP, has been approved for veterinary practice which limits the choice for veterinarians. Moreover, MOP is extensively biotransformed in sheep and induces CYPs activities in ovine liver [6,7,17] which increase a risk of drug-drug interactions and inter-individual differences in pharmacokinetics.…”

“…[11] This hypercontraction of body wall muscles leads to the paralysis, spasmodic contractions of the anterior portion of the pharynx and ultimately death of adult nematodes. [14] Since 2010, MOP has been used in the therapy of nematode infections in sheep mostly with success. [13] The present information about MOP has been reviewed recently.…”

“…[13] The present information about MOP has been reviewed recently. [14] Since 2010, MOP has been used in the therapy of nematode infections in sheep mostly with success. However, some cases of failure of MOP therapy have been recently reported.…”

Anthelmintics

“…It is effective against nematodes that show resistance to levamisole, ivermectin, or albendazole and derquantel [67][68][69]. It is effective against nematodes that show resistance to levamisole, ivermectin, or albendazole and derquantel [67][68][69].…”