Hit-to-Lead Optimization and Hit Expansion
Achieving a lead candidate is challenging. Charles River scientists will work closely with you to define the compound profile required, prioritize compounds for detailed evaluation, and interpret results from a customized screening cascade. This includes primary target discovery and cellular activity together with ADME/PK assessment and target engagement biomarker assay development.
Track Record of Candidates
Successful candidate development is directly related to the experience of scientists, investment in platform technologies and application of a translational approach. Check out our candidate delivery and patent track record by therapeutic area.
Will our next discovery be yours?
The Charles River chemistry team can guide key decisions at the hit generation and hit expansion stage by considering factors such as compound stability for in vivo studies, solubility, and other poor property issues, weak exposure in an animal, and off-target selectivity. As seen in the above chart, Charles River has an extensive track record of delivering high-quality lead series to our clients within agreed timelines across a broad range of target classes and therapeutic areas.
Hit-to-Lead Activities
Charles River is a hit-to-lead CRO, offering flexible, customized hit-to-lead services. Business models include stand-alone, fee-for-service pricing, and fully integrated solutions. Driven by your needs, projects may feature one or more of the following:
- Design and synthesis of new analogues for rapid SAR determination
- Increasing compound potency and selectivity
- Improvement of drug-like properties
- Applying CADD to generate binding hypotheses and to investigate SAR
- Early assessment of ADME properties
- Chemical synthesis
- Evaluation of target engagement biomarker assays
- Ranking of hits or hit series for lead optimization
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This eBook focuses on translational science and discovery partnerships that advance novel therapies through a collective momentum, leveraging efficiencies in drug discovery to accelerate nonclinical research and increase clinical success.
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Frequently Asked Questions (FAQs) About Hit-to-Lead
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How long should a hit-to-lead program take?
Timelines and costs of a hit2lead will vary from program to program. It is possible to reduce hit-to-lead timelines by factors such as prediction of drug-like properties, assessment of intellectual property (IP), increasing compound potency and selectivity, and assessment of solubility and other key attributes.
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What hit-to-lead optimization services does Charles River offer?
Charles River is a comprehensive drug discovery CRO, offering hit generation, hit expansion and hit-to-lead optimization services including in vitro biology, DMPK, in vivo pharmacology, pharmaceutics/formulation, and safety assessment. Our teams of project managers, biologists, and chemists work together to progress compound candidates to clinic. This collaborative, integrated approach to drug discovery ensure programs maximize turnaround times without compromising quality.
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Do you provide fee-for-service (FFS) and full-time equivalent (FTE) services?
Yes. As a flexible drug discovery CRO, we offer many different business models to suit client timelines and budgets. In addition to stand-alone fee-for-service pricing models, our hit-to-lead services are available as part of a fully integrated solution. During any point in the drug discovery workflow, our scientists are ready to work with you to progress your program quickly and efficiently.
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What is the advantage of using one CRO for hit identification, hit-to-lead, and lead optimization?
When using a single CRO from hit ID all the way through to IND, clients have one project team working to get the compound candidate quickly and efficiently through each phase. The team regularly assesses progress, predicts problems, and develops a plan for solving those problems. The project team is instrumental when moving from in vitro studies to in vivo studies and critically important with the transition from the discovery to the safety phase.
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What is the difference between a hit and a lead in drug discovery?
A hit is any compound that has binding activity to the biological target. A lead is a compound with pharmacological activity that still needs to be optimized for therapeutic effect and safety profile.