Lead Optimization

Lead optimization is a core strength within Charles River. We are able to consistently deliver high-quality development candidates (over 70 since 2001) within industry standard timelines, including the data required to support progression into investigational new drug (IND) studies. A significant percentage of the 70 candidates identified have progressed to clinical proof-of-concept, illustrating their high quality. In addition, the first drug on the market resulting from a collaboration with Charles River's medicinal chemistry group was announced in July 2014.

Our efficiency is achieved through the integration of key disciplines, such as assay development and screening, computer-aided drug design, ADME/PK and pharmaceutical sciences, into project teams with many years of experience in tackling the problems associated with converting leads into candidates. An additional aid to efficient decision making during this phase of a project is the use of translational biomarkers, which are employed whenever possible.

We also have many years of experience in providing medicinal chemistry services in joint project teams with a variety of pharmaceutical and biotechnology companies.

This collaborative approach to our partners' drug discovery programs is reflected in patent applications (where our scientists appear as joint inventors on client projects) and in our publications. Wherever possible, we encourage our scientists to publish, present and defend posters, and present orally at conferences.

Lead Optimization Deliverables

  • Compounds with maximized potency and selectivity plus minimized toxicity
  • Compounds with evidence of target or pathway engagement in human systems
  • Human dose predictions
  • Patent filings
  • Generation of a preclinical candidate meeting agreed criteria

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Medicinal Chemistry

Highly experienced medicinal chemists with a track record of delivering candidates to clients.

DMPK

In vitro and in vivo discovery pharmacokinetics can be performed in-house at Charles River.