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- W1968711897 abstract "Macrocycles are ideal in efforts to tackle “difficult” targets, but our understanding of what makes them cell permeable and orally bioavailable is limited. Analysis of approximately 100 macrocyclic drugs and clinical candidates revealed that macrocycles are predominantly used for infectious disease and in oncology and that most belong to the macrolide or cyclic peptide class. A significant number (N = 34) of these macrocycles are administered orally, revealing that oral bioavailability can be obtained at molecular weights up to and above 1 kDa and polar surface areas ranging toward 250 Å2. Moreover, insight from a group of “de novo designed” oral macrocycles in clinical studies and understanding of how cyclosporin A and model cyclic hexapeptides cross cell membranes may unlock wider opportunities in drug discovery. However, the number of oral macrocycles is still low and it remains to be seen if they are outliers or if macrocycles will open up novel oral druggable space." @default.
- W1968711897 created "2016-06-24" @default.
- W1968711897 creator A5056426064 @default.
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- W1968711897 date "2013-09-17" @default.
- W1968711897 modified "2023-10-10" @default.
- W1968711897 title "Macrocyclic Drugs and Clinical Candidates: What Can Medicinal Chemists Learn from Their Properties?" @default.
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- W1968711897 doi "https://doi.org/10.1021/jm400887j" @default.
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