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Emerging compounds and therapeutic strategies to treat infections from Trypanosoma brucei: an overhaul of the last 5-years patents

Introduction: Human African Trypanosomiasis is a neglected disease caused by infection from parasites belonging to the Trypanosoma brucei species. Only six drugs are currently available and employed depending on the stage of the infection: pentamidine, suramin, melarsoprol, eflornithine, nifurtimox, and fexinidazole. Joint research projects were launched in an attempt to find new therapeutic options for this severe and often lethal disease.

Areas covered: After a brief description of the recent literature on the parasite and the disease, we searched for patents dealing with the proposal of new antitrypanosomiasis agents and, following the PRISMA guidelines, we filtered the results to those published from 2018 onwards returning suitable entries, which represent the contemporary landscape of compounds/strategies against Trypanosoma brucei. In addition, some relevant publications from the overall scientific literature were also discussed.

Expert opinion: This review comprehensively covers and analyzes the most recent advances not only in the discovery of new inhibitors and their structure-activity relationships but also in the assessment of innovative biological targets opening new scenarios in the MedChem field. Finally, also new vaccines and formulations recently patented were described. However, natural and synthetic compounds were analyzed in terms of inhibitory activity and selective toxicity against human cells.

Comments：

The introduction provides a brief overview of the current situation with regards to Human African Trypanosomiasis and the limited treatment options available. The review aims to explore recent developments in the discovery of new therapeutic options, including patents related to new antitrypanosomiasis agents, biological targets, vaccines, and formulations. The review also discusses the selectivity and toxicity of natural and synthetic compounds against human cells. Overall, the review provides a comprehensive analysis of the most recent advances in the field, providing valuable insights for researchers and healthcare professionals working on this disease.

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Decarboxylase