The advantages of macrocycles as drugs include:

  1. Modulation of challenging targets such as protein-protein interactions
  2. Ability to cross biological membranes and reach intracellular targets
  3. Stability to metabolism
  4. Improved target affinity/specificity
  5. Potential for oral bioavailability
  6. Access to novel patentable chemical space

Macrocycles can inhibit protein-protein interactions, and target a diverse array of diseases, including inflammatory and immunological disorders, infectious diseases, cancer, cardiovascular disease, Alzheimer’s and epilepsy.


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