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Peer-reviewedCC BY-NCJournal of Antimicrobial Chemotherapy

A strategic discovery roadmap towards high-quality leads and drug development candidates for kinetoplastid diseases. Part 3: from lead towards a drug development candidate

8 more authors

Abstract

Neglected tropical diseases such as leishmaniasis, Chagas disease, sleeping sickness and animal trypanosomiasis remain a significant global health challenge. This part of the roadmap outlines a streamlined path for progressing from lead identification to a drug development candidate, tailored to the specific needs of kinetoplastid infections. Besides the medicinal upscaling of synthesis, this review highlights key experiments in pharmacology in non-rodent species, toxicology, pharmacokinetics and pharmaceutics. These include but are not limited to early evaluation of safety using refined in vitro and in vivo methods to enhance predictive value, bioavailability and distribution to target tissues, and formulation strategies leveraging various delivery systems to optimize efficacy and safety. Environmental toxicity is also addressed proactively, for which in silico tools are presented. Collectively, this roadmap provides a practical, scalable approach to deliver high-quality drug candidates capable of addressing the urgent needs for kinetoplastid diseases (Figure 1).

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BibTeX
@article{hendrickx2026strategic,
  title = {{A strategic discovery roadmap towards high-quality leads and drug development candidates for kinetoplastid diseases. Part 3: from lead towards a drug development candidate}},
  author = {Sarah Hendrickx and Kayhan Ilbeigi and Eli Thoré and Michael Bertram and Estefanía Calvo-Alvarez and Sener Cintesun and Ana Isabel Olías-Molero and María Jesús Corral and Marta Mateo-Barrientos and Jérôme Estaquier and Sébastien Pomel and José María Alunda and Sheraz Gul and Katrien van Bocxlaer and Frédéric Frézard and Joana Tavares and Anabela Cordeiro da Silva and Maria Paola Costi and Louis Maes and Guy Caljon},
  journal = {Journal of Antimicrobial Chemotherapy},
  year = {2026},
  month = jun,
  doi = {10.1093/jac/dkag111},
  url = {https://hal.science/hal-05790237v1},
  note = {CC BY-NC},
}
RIS
TY  - JOUR
TI  - A strategic discovery roadmap towards high-quality leads and drug development candidates for kinetoplastid diseases. Part 3: from lead towards a drug development candidate
AU  - Sarah Hendrickx
AU  - Kayhan Ilbeigi
AU  - Eli Thoré
AU  - Michael Bertram
AU  - Estefanía Calvo-Alvarez
AU  - Sener Cintesun
AU  - Ana Isabel Olías-Molero
AU  - María Jesús Corral
AU  - Marta Mateo-Barrientos
AU  - Jérôme Estaquier
AU  - Sébastien Pomel
AU  - José María Alunda
AU  - Sheraz Gul
AU  - Katrien van Bocxlaer
AU  - Frédéric Frézard
AU  - Joana Tavares
AU  - Anabela Cordeiro da Silva
AU  - Maria Paola Costi
AU  - Louis Maes
AU  - Guy Caljon
PY  - 2026
DA  - 2026/06/05
JO  - Journal of Antimicrobial Chemotherapy
DO  - 10.1093/jac/dkag111
UR  - https://hal.science/hal-05790237v1
AB  - Neglected tropical diseases such as leishmaniasis, Chagas disease, sleeping sickness and animal trypanosomiasis remain a significant global health challenge. This part of the roadmap outlines a streamlined path for progressing from lead identification to a drug development candidate, tailored to the specific needs of kinetoplastid infections. Besides the medicinal upscaling of synthesis, this review highlights key experiments in pharmacology in non-rodent species, toxicology, pharmacokinetics and pharmaceutics. These include but are not limited to early evaluation of safety using refined in vitro and in vivo methods to enhance predictive value, bioavailability and distribution to target tissues, and formulation strategies leveraging various delivery systems to optimize efficacy and safety. Environmental toxicity is also addressed proactively, for which in silico tools are presented. Collectively, this roadmap provides a practical, scalable approach to deliver high-quality drug candidates capable of addressing the urgent needs for kinetoplastid diseases (Figure 1).
SN  - 0305-7453
SN  - 1460-2091
ER  -