Lead Optimization

Using our integrated drug discovery platform that includes a panel of ADME assays, our expert medicinal chemists can quickly optimize a lead series based on potency, selectivity, and desired properties. Lead compounds can quickly advance into pharmacokinetic studies to generate candidate compounds for in vivo efficacy studies.

Lead optimization services include:

• Design and synthesis of new analogs to optimize early lead compounds into clinical candidates. Typically, 500-1200 compounds are prepared.
• Formulate patent strategies and design of analogs for best intellectual property protection
• Optimization based on specified target profile and screening cascade (e.g., potency, selectivity, metabolism, bioavailability, efficacy, safety)

Click to read about our case studies:

• Arginase inhibitors
• Ironistat-B

FAQ

• How do you help optimize lead compounds?

  Our team of medicinal chemists uses an integrated approach to optimize lead compounds, considering potency, selectivity, solubility, metabolic stability, and other properties. We also include novelty and patentability into our design and consideration.

• How is lead optimization different from Hit-to-Lead?

  Lead optimization is the expansion of Hit-to-Lead with the goal of identify a novel compound which is more potent, more selective, with suitable pharmacokinetic profile to be tested in animal models, and eventually to identify a preclinical candidate.

• What are the typical timelines for lead optimization?

  It can vary depending on the complexity of the project, including synthesis, selectivity and property requirement, but typically range from 1-2 years.

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