Home
Up

Lead identification and optimization

This process is used in discovery research to find and optimise the physicochemical, pharmacological, absorption-distribution-metabolism-excretion (ADME), toxicological properties of an active molecule.

At the end of the process one or more compounds having differentiated properties and fulfilling the desired Therapeutic Product Profile will be identified and scored against Standard of care, best in class and competitors.

Example of Development Candidate properties optimized during this phase of research

Property

Risk

Benefit

Potency

side effects

Lower dose, better formulability

Selectivity

Undesired effects

Unexpected advantages

Metabolism

Poor efficacy, variable efficacy

Active metabolites

Stability

Shelf life

Reduced development costs, easier development

Bioavailability

Higher doses, unecessary GI exposure

reduced costs, easier formulation

Physical form

Polymorphic change

Improves formulability and developability

Solubility

Complex formulation

Easier formulation

Chemical developability

Cost of goods too high

Supply chain

Faster and more robust development

Key Benefits

  • Define the development candidate properties
  • Identification of multiple lead compounds
  • Differentiation

 

     Hit Counter

For More Information Contact:

Innovative Solution di Biondi Stefano
via Copernico 22, 20016 Pero (MI), Italy
Tel: +39 02 36593963
FAX: +39 02 36593963
Internet: stefano.biondi@innovativesolution.it 

 

 

 

Send mail to stefano.biondi@innovativesolution.it with questions or comments about this web site.
Copyright 2010 Innovative Solution di Biondi Stefano