Prodrug design and development has proven to be a valuable complementary tool in modern drug design. In an integrated approach to drug design including optimization of compound structures in terms of efficacy, safety, and drugability, the prodrug principle offers opportunities for a temporarily change and improvement of physicochemical, pharmaceutical, biopharmaceutical, and ADME properties of a pharmacologically active molecule. The prodrug principle constitutes a tool for building additional properties into interesting pharmacologic active molecules, which are of vital importance for the development of clinically useful drugs. Thus, integration of prodrug considerations into the drug design paradigm may increase the opportunity for discovery and development of novel innovative drugs and treatment concepts to the benefit of patients.
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