Lead Optimization

The lead optimization process aims to improving the hit/lead molecules properties for ADME profile, reduction of off-target effects and improved efficacy. Series of compounds with altered properties are assayed and their drug like properties are optimized.

Lead optimization process is balancing between multiple properties, including efficacy, safety and toxicity, chemical stability, metabolite formation, routes and stability, solubility and absorption. Ability to handle this process requires expertise and technologies from multiple disciplines.

SBW Lead optimization platform

We provide our customers with expertise and technologies for the lead optimization process. This includes in silico, in vitro and in vivo technologies

• In silico ADME property prediction
• In silico bioactivity, adverse effect and toxicity prediction
• Efficacy and toxicity biomarker discovery
• Experimental logP, logD, logS, pKa analysis
• Plasma protein binding
• PAMPA, Caco-2 and skin permeability
• Drug interaction studies
• Metabolite identification and stability
• Metabolites in safety testing (MIST)
• Pharamacokinetics
• Metabolites in safety testing (MIST)
• In vivo disease models