Drug Discovery Phases (4)

Lead Optimization — Prediction of Efficacy in Isolated Fresh Tissues

REPROCELL’s Predictive Drug Discovery provide an excellent first look at how your test compound will perform far in advance of being in the clinic.

lead_optimization_efficacy_1Our models can provide invaluable human efficacy data while your compounds are still in pre-clinical development; greatly increasing the predictability of your drug development, meaning ‘go’ or ‘no-go’ decisions can be made with confidence prior to expensive clinical studies.

Both healthy and diseased tissues are often freely available and enable researchers to make detailed ‘phase 0’ comparisons in select patient populations without the associated large costs. Human efficacy data adds significant value for investors and can be extremely useful when looking for expected secondary applications or repositioning of current compounds.

REPROCELL Bioptaoffers a range of validated assays across all therapeutic areas as well as a dedicated assay development team who are able to provide customised assays to meet your specific needs.The flow chart below shows a typical project at Biopta- note that the tissue type and endpoint is highly flexible, here, an example is shown using small blood vessels dissected from subcutaneous adipose tissues.

Efficacy data in living human tissues is a powerful method to demonstrate the value of your compounds:

  • For investors – confidence increased by early demonstration of human efficacy in the target patient group
  • Adds commercial value – reduces risk of phase II failure, which adds early stage value to the compounds
  • De-risks development – by selecting compounds with demonstrable human efficacy Accurately predict in vivo bioavailability and drug metabolism using human tissue, eliminating well-known differences between human and alternative model systems.

Determine the Potency of Your Drug

Compare the potency of your candidate drug versus other drugs on the market.

Small intestine ileum


Effect of inhibitors of chloride secretion in human ileum


Increase the Confidence of Your First-in-Man Dose Estimate

Measure compound permeability, transporter, or metabolic enzyme activity in human intestinal tissue in order to accurately predict in vivo bioavailability and drug metabolism.

  • Eliminate well-known differences between human and animal or cell models in bioavailability and metabolism by using human tissue.
  • In vitro human gut permeability correlates well to expected clinical absorption

Ussing chamber assay


In vitro human gut permeability correlates well to expected clinical absorption