Lead Optimization

Drugabilis lead optimization tests includes:

  • Early routine screening: thermodynamic aqueous solubility, chemical stability in solution
  • Equilibrium aqueous solubility versus pH, ionic strength, temperature
  • Solubility in FASSIF (Fasted State Simulated Intestinal Fluid)
  • Solubility in FESSIF (Fed State Simulated Intestinal Fluid)
  • Solubility in solvents
  • Material chromatographic profile
  • Chemical stability assessment of bulk API under various stress conditions (light, temperature, humidity)
  • pKa of soluble and insoluble compounds
  • logP (shake flask method and screening by a chromatographic method)
  • Screening methodology design and set-up, at request, for early assessment of specific properties...

Any other specific physicochemical characterisation testing set may be designed at request, in order to secure, at each step of a given research program, that series selection, lead optimisation, candidate selection or formulation development will have taken drug-like properties and drugability criteria into account.