Traditional small molecule drugs are not suitable for extended binding sites, such as those that feature in protein-protein interactions or Class B GPCRs.

Biologics, such as therapeutic antibodies, are not suitable for oral administration, cannot act inside the cell, and are more expensive to manufacture.  They also suffer from a highly complex patent landscape.

Macrocycles target extended binding sites but have many of the properties of small molecules.  

 

(click to zoom)