Drugs approved by the Food and Drug Administration (FDA) or regulatory agencies worldwide fall under two main categories: small molecules; and biologics or large proteins. Both classes have limitations that restrict their functional range. Small molecules target human proteins bearing lipophilic pockets on their surface while large proteins and antibodies target through the exterior of the cell, so neither class interacts with the targets inside the cells. Small molecules and larger proteins together can access only 25% of cell targets; that leaves 75% of human proteins inside the cell that are not targeted by the two drug classes, making these cellular sites ‘undruggable’.
There is a great deal of interest among researchers to target these sites through the development of a novel therapeutic class, such as bicyclic peptides, that lie between the small molecule and monoclonal antibody (mAb) drug classes.
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