Successful lead optimization in drug discovery requires knowledgeable and collaborative scientists at a CRO that regularly invests in technology. In order to give your small or large molecule the best chance to turn into a preclinical candidate, a rigorous approach to translational study design and risk mitigation is required.
Lead Optimization Services and Deliverables
In addition to optimizing the lead compound’s safety profile, researchers must develop a clear understanding of the mode of action, nature of the target, and establish the biological relevance of the animal species used in pharmacological studies, as well as explore potential differences between animal models and humans.
Among the lead selection and optimization services we offer, they include:
- Evidence of target or pathway engagement in human systems
- Human dose predictions
- Patent filings
- Studies to maximize potency and selectivity plus minimize toxicity
- Generating a preclinical candidate meeting agreed criteria
Lead Selection and Optimization
We offer a comprehensive suite of drug discovery services, and our lead optimization scientists work collaboratively with our target ID, hit identification, and hit-to-lead teams to offer a seamless solution for our clients.
Below is a partial list of guided lead optimization studies:
- Mechanism of action
- Appropriate LogP and LogD profiles
- Biochemical and functional potency
- Acceptable biochemical kinetics (on-off rates)
- Target engagement in vitro
- Selectivity profiling and optimization
- Potency distribution showing structure-activity relationship (SAR)
- Solubility profiling and optimization
- Permeability (Caco-2)
- Metabolic liabilities profile
- Human plasma protein binding ≤ 99%
- CYP450 inhibition
- hERG and chronic cytotoxicity screen
- Genotoxic liabilities profile
- Cerep® profile
- In vivo PK and ADME profile
- In vivo efficacy in appropriate animal models
- Translational biomarkers
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?
Path to Preclinical Candidate and Clinical Candidate Success
With years of laboratory experience, scientific expertise through publications and patents, and a proven track record conducting lead optimization programs, partnering with us can give your program a leg up on the competition. Having already worked on 85% of drugs currently on the market, find out how we can turn your small and large molecules into preclinical candidates and, eventually, therapeutics.