A strategic discovery roadmap towards high-quality leads and drug development candidates for kinetoplastid diseases. Part 2: from molecule to confirmed hit

Abstract

Given the medical importance and challenges related to kinetoplastid diseases, a strategic roadmap is needed for the identification of high-quality leads and drug development candidates. Within the aim to deliver more compelling proof-of-concept read-outs, this part proposes a systematic flow-chart of laboratory experiments and decision criteria, focusing on African trypanosomiasis, Chagas disease and visceral and cutaneous leishmaniasis. Next to precision experimental design and reporting, an overview is provided of various complementary laboratory models reproducing kinetoplastid infection and disease. Technical aspects of conventional in vitro and in vivo approaches and, more recently, in silico methods are presented with reference to specific preclinical R&D stages from 'hit finding' to 'profiling of a confirmed hit', covering the expertise areas of medicinal chemistry, primary pharmacology, (eco)toxicology, pharmacokinetics and pharmaceutics (Figure 1).

Published in

Journal of Antimicrobial Chemotherapy
2026, volume: 81, number: 4, article number: dkag110

SLU Authors

• Thoré, Eli

  • Department of Wildlife, Fish and Environmental Studies, Swedish University of Agricultural Sciences
    
  • University of Namur

• Bertram, Michael

  • Department of Wildlife, Fish and Environmental Studies, Swedish University of Agricultural Sciences
    
  • Monash University
  • Stockholm University

UKÄ Subject classification

Medicinal Chemistry
Pharmacology and Toxicology

Publication identifier

• DOI: https://doi.org/10.1093/jac/dkag110

Permanent link to this page (URI)

https://res.slu.se/id/publ/146665