Recent trends in targeted anticancer prodrug and conjugate design

Yashveer Singh1, Matthew Palombo, Patrick J Sinko

  • 1Department of Pharmaceutics, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854-8020, USA.

Insights

Targeted prodrug and conjugate design aims to improve cancer therapy by selectively delivering anticancer agents to tumors. This approach minimizes toxicity to healthy cells and overcomes drug resistance, enhancing patient outcomes.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Drug Delivery

Background:

  • Anticancer drugs often cause significant toxicity to healthy cells due to their nonselective antiproliferative nature.
  • Drug resistance in solid tumors and off-target toxicities are major limitations in current cancer chemotherapy, leading to poor patient prognosis.
  • Prodrug and conjugate strategies aim to enhance the efficacy and safety of anticancer agents.

Purpose of the Study:

  • To review recent advancements in prodrug and conjugate design for cancer treatment.
  • To critically analyze various targeting strategies for selective drug delivery to tumors.
  • To present a comparative account of the advantages and disadvantages of different approaches.

Main Methods:

  • Review of recent literature on prodrug and conjugate design in cancer therapy.
  • Analysis of targeting strategies exploiting tumor-specific characteristics (e.g., pH, enzymes, hypoxia, antigens).
  • Comparative evaluation of different prodrug and conjugate approaches.

Main Results:

  • Targeted prodrug and conjugate design focuses on selective delivery of anticancer agents to tumor tissues.
  • Strategies leverage tumor microenvironment features like low pH, elevated enzymes, hypoxia, and tumor-specific antigens.
  • Classical prodrug design addressed physicochemical and biopharmaceutical challenges, while newer designs focus on tumor targeting.

Conclusions:

  • Targeted prodrug and conjugate design offers a promising strategy to improve cancer treatment by enhancing drug selectivity and reducing systemic toxicity.
  • Exploiting tumor-specific characteristics enables more effective and safer delivery of anticancer agents.
  • Continued research in this area is crucial for developing next-generation cancer therapies.

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