molecules of the month


irreversible trypanosomal topo. II inhibitor

efficacy in Chagas and sleeping sickness models

from phenotypic screen against trypanosomes

Science, June 29, 2023

Novartis (NITD), Emeryville, CA / Singapore

CT3, topoisomerase II, irreversible trypanosomal topo. II inhibitor, efficacy in Chagas and sleeping sickness models, from phenotypic screen against trypanosomes, Science, June 29, 2023, NOVARTIS (NITD), EMERYVILLE, CA / SINGAPORE
6 mins read

A Novel Class of Brain-Penetrant, Covalent Antiparasitic Drugs from Novartis Recently, Novartis disclosed a new class of brain-penetrant, covalent agents against kinetoplastid parasites in Science. Kinetoplastid parasites cause Chagas disease (T. cruzi), sleeping sickness (T. brucei), and leishmaniasis (Leishmania), but there are few effective treatment options, especially for infections in the brain (e.g. stage II sleeping sickness). Novartis’s cyanotriazoles have a novel mechanism of action that lead to rapid cures of trypanosomatid infections in mouse models of Chagas disease and sleeping sickness. This is a great example of a CNS-penetrant, non-acrylamide covalent drug with an interesting biological mechanism for activity and species selectivity discovered through phenotypic screening. Brain Penetration is Needed to Eradicate Kinetoplastid Parasite Infections The existing, decades-old treatments…

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