The outbreak of novel coronavirus (SARS-CoV-2, formerly known as 2019-nCoV) has drawn global attention, prompting the urgent need to find specific and broad-spectrum antiviral drugs. With years of experience in structure-based drug design (SBDD), Creative Biostructure combines multidisciplinary drug discovery expertise to provide lead optimization services for coronavirus infection to support the discovery of effective preclinical antiviral drug candidates.
Importance of Lead Optimization in Drug DiscoveryOnce the most promising hit series is identified through the efforts of
hit to lead, the lead optimization phase of drug discovery will be entered. Lead optimization is a crucial process for finalizing preclinical drug candidates. It is a sophisticated iterative stage in drug discovery and development. The goal of this stage is to extensively optimize the biological activity and characterization of the lead series through specialized in vitro and in vivo screening funnels. Starting with identified potential lead compounds, toxicity, efficacy, stability, bioavailability, and other pharmacokinetic parameters are investigated to improve their target specificity, selectivity, and potency. This phase can provide lead molecules of better quality, and the optimized molecules have a high probability of success in clinical development.