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Lead optimisation

Fine-tuning lead compounds for optimal performance

Through suitable design–make–test cycles, we can improve the profiles of your lead compound via multiparameter optimisations. Our scientists work collaboratively across therapeutic research functions to increase on-target activity, improve molecular properties, examine efficacy with in vivo animal models and conduct safety profiling, while ensuring that tractable large-scale syntheses are in place.  

Scientist running a reaction under an inert atmosphere

Integrated lead optimisation workflow 

During lead optimisation, we aim for improved potency, selectivity and DMPK properties by developing efficient synthetic routes to key lead sub-structures. Our scale-up labs synthesise advanced intermediates for late-stage functionalisation. Co-located discovery pharmacology researchers assess lead compounds through pharmacological assays, in vitro PK and toxicology profiling. With extensive in vitro and in vivo data, we use data mining to refine safety and selectivity profiles. Our experienced medicinal chemists have successfully brought leads into the clinic, handling patenting, synthesis and coordination for preclinical studies. 

 
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