The expanding role of prodrugs in contemporary drug design and development

This study describes the discovery of selexipag and demonstrates that a sulfonamide group can be a promoiety for carboxylic acid

Jarkko Rautio; Nicholas A. Meanwell; Li Di; Michael J. Hageman


Scholarcy highlights

  • This study provides an illustration of some of the key points of polymer therapeutics from the laboratory to the clinic
  • This is an outstanding review on carboxylesterases and their functions in the metabolic activation of prodrugs
  • This study investigates species and in vitro system differences in the hepatic and extrahepatic hydrolysis of 11 prodrugs in an effort to improve our understanding of animal species differences when developing hydrolysable prodrugs
  • In the past 10 years, the US Food and Drug Administration has approved at least 30 prodrugs, which accounts for more than 12% of all approved small-molecule new chemical entities
  • This study describes the discovery of fostemsavir, a prodrug designed to address dissolution-limited and solubility-limited absorption issues
  • This is a comprehensive review of the development and application of ProTide technology to deliver nucleoside phosphate and phosphonate derivatives that are used in the commercially important antiviral drugs tenofovir alafenamide and sofosbuvir

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