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The landscape of small-molecule prodrugs.

Zachary FralishAshley ChenShaharyar KhanPei ZhouDaniel Reker
Published in: Nature reviews. Drug discovery (2024)
Prodrugs are derivatives with superior properties compared with the parent active pharmaceutical ingredient (API), which undergo biotransformation after administration to generate the API in situ. Although sharing this general characteristic, prodrugs encompass a wide range of different chemical structures, therapeutic indications and properties. Here we provide the first holistic analysis of the current landscape of approved prodrugs using cheminformatics and data science approaches to reveal trends in prodrug development. We highlight rationales that underlie prodrug design, their indications, mechanisms of API release, the chemistry of promoieties added to APIs to form prodrugs and the market impact of prodrugs. On the basis of this analysis, we discuss strengths and limitations of current prodrug approaches and suggest areas for future development.
Keyphrases
  • small molecule
  • cancer therapy
  • single cell
  • drug release
  • public health
  • healthcare
  • social media
  • big data
  • machine learning
  • health insurance
  • drug delivery
  • health information
  • dna methylation
  • drug discovery