Overview and Examples of Drug Screening in Cell-and Tissue-Based Assay Systems: Screening Funnels for In Vitro and In Vivo Studies

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Chronically elevated intraocular pressure (IOP) is a hallmark of open-angle glaucoma, the most prevalent form of this neurodegenerative eye disease around the world. Although a number of drugs have been approved for lowering and controlling IOP, there continues to be an unmet medical need for superior therapeutics that exhibit better pharmacodynamics and can overcome the significant compliance issues associated with current medicines. As such, it is necessary to continue drug discovery research using both in vitro and in vivo screening methods. In terms of the former, several cell- and tissue-based assay systems have been developed and implemented in compound screening paradigms that rely on a variety of readouts to assess receptor binding affinity, functional potency, and relative selectivity. In the current chapter, an overview of many functional assay systems using cultured cells or intact tissues derived from ocular tissues involved in ocular hypertension will be presented.