Hit/Lead Compounds

The XenoGesis team can work with you to put together data packages for hit/lead compounds and for lead optimisation programmes.

Hit Identification / Lead Identification / Lead Optimisation Programmes

Typically, a data package for review will cover a broad range of compounds in less depth than a clinical candidate.

  • Potency
  • Lipophilicity
  • Molecular weight
  • Hepatocyte/microsome stability
  • Kinetic solubility for a selection of compounds

A further more detailed package covering one or two lead compounds would include:

  • In vivo PK in one or two pre-clinical species
  • Plasma protein binding & permeability
  • Some preliminary in vivo pharmacology
  • An understanding of the intended clinical use (indication, dose route) or target candidate profile

Deliverables

The data would be reviewed to explore the trends between in vitro and in vivo data and their relationship with potency and the physicochemical properties. The aim would be to identify the deficiencies in the lead compound(s) and, the likelihood that these could be addressed during a lead optimisation campaign. A proposal for a screening cascade to achieve this would be suggested.


Data Review

In general, we will assume all data provided is accurate. However, we can perform an in-depth review of raw data and reports if required.

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