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May 17, 2026Journal of the American Chemical Society0 citationsOpen Access

Challenges and Opportunities for Cleavable Linkers Used in Polymer–Drug Conjugates

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FKFatemeh KarimiKLKatherine E. S. LocockJCJohn Chiefari

Key Points

  • This work aims to explore the challenges and potential of cleavable linkers in polymer-drug conjugates for improved drug delivery.
  • Outlines advantages and pitfalls of various linker types
  • Discusses challenges in clinical adoption and efficacy
  • Highlights recent developments in polymer science and prodrug chemistry
  • Identified issues with specificity and complexity of current cleavage strategies
  • Proposed new opportunities to enhance clinical adoption of polymer-drug conjugates
  • Critical analysis of efficacy and biocompatibility challenges faced in the field

Abstract

Polymer-drug conjugates with cleavable linkers show excellent promise as controlled-release drug delivery systems for a range of diseases; however, several cleavage strategies fall short in their specificity or require additional complexities that pose significant challenges for clinical adoption. This Perspective outlines the advantages and pitfalls of various linker types in terms of their responsiveness to their target cleavage stimuli. Aside from overcoming efficacy and biocompatibility challenges, we critically discuss other key challenges in the translation of these materials and highlight the latest clinical developments. Taking inspiration from other areas of prodrug chemistry and polymer science, new opportunities for this field are proposed, which aim to overcome the current barriers and may be the key to the clinical adoption of this exciting class of therapeutics.

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Cite This Study

Karimi et al. (2026) studied this question.

synapsesocial.com/papers/6a095ac47880e6d24efe0a55https://doi.org/10.1021/jacs.6c03661
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