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.