A wide variety of assays can provide important information on the Absorption, Distribution, Metabolism, and Excretion (ADME) properties of a therapeutic to understand potential liabilities and facilitate the selection of compounds to move forward into in vivo studies. Two critical physicochemical characteristics of compounds we can assess for you are solubility and plasma protein binding to better understand the concentration of unbound drugs that may be achievable in both in vitro assays and in vivo. Another critical early assessment is to evaluate metabolism by examining stability in hepatocytes or liver microsomes generated from these hepatic cells. Additional assays can evaluate the stability of your compound in multiple matrices - i.e., plasma, whole blood, urine, or simulated gastric or intestinal fluid. Finally, permeability can be assessed using a parallel artificial membrane permeability assay (PAMPA) and permeability and transporter-mediated efflux can be assessed with the Caco-2 permeability assay. Collectively, these assays can be used to screen out compounds with undesirable characteristics in order to select compounds that have a higher chance of moving forward to clinical success. Our analytical chemistry services, which are used to measure changes in these assays, are described in more detail here.

• Solubility
• Plasma protein binding
• Metabolic stability
  • Liver microsomal stability
  • Hepatocyte stability
• Matrix stability
  • Plasma
  • Whole blood
  • Urine
  • Simulated gastric or intestinal fluid
• Permeability and efflux
  • PAMPA
  • Caco-2 permeability assay