CF series
Select a pre-clinical candidate from the CF series for the treatment of leishmaniasis
last phase of drug development
updated 1 Mar 2022
The chemical starting points for the CF series were identified through screening of GlaxoSmithKline’s kinetoplastid compound collection, which identified a series of compounds with intermediate potency. Modulation of the core scaffold led to the CF-series compounds, which displayed promising levels of efficacy in mouse models of visceral leishmaniasis and were found to be suitable for progression to lead optimization. Optimization of the CF lead series led to compounds displaying increased potency against the L. infantum and L. donovani parasite strains. In addition, the pharmacokinetic profile of the compounds was significantly improved.
Project updates
2021
Despite significant progress, the project team encountered obstacles to achieving an adequate drug property profile with improved antimicrobial efficacy. In addition, the scope in the class was deemed exhausted based on more than 400 compounds made. For these reasons, the project team recommended termination of the project. The findings and mechanisms of action elucidated during this project will be analysed and published.
2020
Further optimization of the potency and metabolic stability of two sub-series continued; a pre-clinical candidate is expected to be delivered in 2021.
2019
Further optimization of the CF series lead-series has provided compounds displaying promising potency against L. infantum. Further optimization is ongoing to select additional compounds for in vivo testing.
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