Macrocycle therapies can block protein-protein interactions that are undruggable with small molecules; however, oral availability and cell penetration remain key challenges. Encycle Therapeutics Inc.'s chemistry platform generates drug-like macrocycles against validated targets to treat diseases for which oral therapies are needed.

Marketed inhibitors of protein-protein interactions include biologics and other molecules large enough to target the wide, shallow surfaces involved in those interactions, but can only bind extracellular targets. Macrocycles can have sufficient size to block protein-protein interactions yet remain small enough to penetrate cells and block intracellular interactions that biologics and small molecules cannot.