Tecnologías para licenciar

Compounds for malaria treatment

Advantages

  • High activity in vitro including chloroquine- and artemisinin-resistant lines.
  • New chemical family with no other antimalarial drugs described and new mechanismof action.
  • Theranostic agent for malaria (it turns fluorescent when entering the parasite) promoting its use in diagnostics tools.
  • Quick and easy synthesis (2 steps) from commercially available sources.
  • High stability. The compounds have a long shelf life (months) at room temperature.

Intellectual Property

  • ISGlobal (40 %), Institute of Bioengineering of Catalonia (40 %), and University of Barcelona (20 %) share joint ownership.
  • PCT application submitted 21st October 2022.
  • Excellent perspectives to be granted after EESR and ISR positive evaluation reports.
  • Entering national phases in Europe, the USA, India, China, Brazil, ARIPO and Nigeria.

Reference

UBTT0434-E

Contact

ISGlobal:
Oscar Casado:  innovation@isglobal.org

University of Barcelona:
Rosa Vázquez: rvazquez@fbg.ub.edu

Unmet clinical need

  • Malaria is still a major global health problem. According to WHO, in 2021, it caused 619,000 deaths, mainly children under five years old and pregnant women.
  • The parasite can kill within 24 hours of symptom onset if left untreated.
  • The main threat to malaria elimination is the evolution by the parasite of resistance to every drug deployed against it.
  • New drugs with new MoA, representing a new chemical class and good therapeutic index are urgently needed to overcome resistance issues.

Technology description

  • Potent Antimalarial. Family of compounds around YAT2150 (HIT compound) possess high in vitro activity and quite a good selectivity index:
Compound
IC50 (nM)
CC50 (µM)*
SI
(Selectivity Index)
YAT2150
90
3.4
37.8
PRC25
47
4.8
102
EMA377
59
57
956
*CC50: Cytotoxic Concentration

 

  • Irresistible antimalarial drug. No resistant P. falciparum strains emerged in vitro after 60 days of cross-resistance assessment in P. falciparum lines.
  • Preliminary data suggests that YAT2150 will be active against all Plasmodium species causing malaria targeting protein aggregation, which is essential for the viability of the parasite.
  • YAT2150 has a low teratogenic index (TI) in the zebrafish model (1.15), significantly below that of artemisinin controls (2.04).

Current stage of development

  • We are currently completing the Hit-to-Lead stage (TRL 3).
  • Presently preparing in vivo experiments in a murine model of malaria and identifying proteins interacting with, or being affected by YAT2150.
  • Transmission-blocking potential in mosquitoes to be assessed in the following months.
  • OUR ASK: CO-DEVELOPMENT, LICENSE AGREEMENT and/or INVESTMENT.

 

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Tags: Life Sciences, Salud y ciencias de la vida

 

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