Fine-tuning a lead to have good potency, selectivity, and other DMPK properties is the goal during lead optimization. We start by developing robust, good yielding routes to access key lead sub-structures. Our scale-up laboratories—also located in the same building—play a pivotal role by synthesizing advanced intermediates that can be utilized in, for example, late-stage functionalizations.
Co-located in Berlin, NUVISAN’s discovery pharmacology researchers characterize new chemical derivatives in a range of pharmacological assays to assess potency and selectivity. Promising lead compounds are characterized with in vitro PK and in vitro metabolite profiling; in vitro toxicology helps to ensure that lead compounds have favorable initial safety end points. Our life science datasets contain billions of in vitro and in vivo data points, and data mining approaches are regularly utilized to further establish that lead compounds have good selectivity and safety profiles.
The medicinal chemists on our team have brought multiple leads into the clinic and have significant experience managing the nuances of these inherently complex activities. From novelty searches to patent drafting, as well as coordination of synthesis scale-up activities, we are ready to bring good lead compounds into in vivo pharmacology and toxicology studies en route to your preclinical candidate!