Early Screening for Lead Optimization

The choice of the right drug candidate is a challenging process and requires a multidisciplinary approach. Despite the fact that a compound or dozens of analogs could prove to be active against the targeted enzyme or pathway during the drug discovery process, many times none of them will be the ideal drug candidate capable of reaching the status of an investigational new drug.  Harlan Laboratories can support you in the process of lead optimization, providing you with the pivotal information you may need to make the right decision.

Harlan Laboratories offers a screening package to support your lead optimization process. This package consists of:

• Early PK or TK profiling, including biodistribution screening including blood-brain barrier penetration (if applicable) and preliminary safety assessment
• In vitro metabolic stability (straightforward tests with liver microsomes and blood or plasma)
• Protein binding
• Fast bioanalytical method development using the fast chromatography approach by UPLC^® MS/MS and including method qualification/characterization
• Early formulation (“pre”-preclinical formulation)
• Fast Ames test

The screening is generally performed in rodents at this stage and can be adapted to meet your needs.