The evolution of synthetic oral drug properties.
An analysis of the properties of 1791 synthetic, oral drugs approved and/or marketed since 1937 demonstrates that the median molecular weight of oral drugs has increased substantially over the past 60 years. Fewer than 5% of approved/marketed oral drugs have more than 4-H bond donors and just 2% have MW>500 and >3 H-bond donors.
Proudfoot
John R
JR
Boehringer Ingelheim Pharmaceuticals Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877, USA. jproudfo@rdg.boehringer-ingelheim.com
D000284:Administration, Oral; D001682:Biological Availability; D003625:Data Collection; D049673:History, 20th Century; D049674:History, 21st Century; D006801:Humans; D006860:Hydrogen Bonding; D008970:Molecular Weight; D004364:Pharmaceutical Preparations / Q000737:chemistry* / Q000266:history*; D010599:Pharmacokinetics; D016008:Statistical Distributions; D013329:Structure-Activity Relationship
D004364:Pharmaceutical Preparations