Prodrug Applications for Targeted Cancer Therapy
A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".
Deadline for manuscript submissions: 31 January 2026 | Viewed by 47

Special Issue Editors
Interests: drug design and synthesis; organic chemistry; prodrugs; medicinal chemistry; anticancer drugs; molecular pharmacology
Special Issue Information
Dear Colleagues,
Targeted cancer therapies have become a cornerstone of modern oncology treatment strategies, offering the potential for enhanced efficacy and reduced systemic toxicity. Among these strategies, prodrugs represent a highly promising approach to improving the selectivity and therapeutic index of anticancer agents. Recent developments in prodrug design have enabled precise control over activation mechanisms, opening new avenues for overcoming biological barriers such as poor solubility, low membrane permeability, and multidrug resistance. This Special Issue will focus on the latest advances in prodrug-based approaches for targeted cancer therapy, highlighting the rational design, synthesis, in vitro, and in vivo evaluation of prodrugs. We aim to explore the role of prodrugs in next-generation cancer treatments and to discuss their translational potential.
We invite original research articles, reviews, and short communications addressing (but not limited to) the following topics:
- Novel prodrug designs for tumor-selective activation,
- Stimuli-responsive prodrugs (e.g., enzymatic, redox, or pH-triggered),
- Prodrug–nanocarrier conjugates and delivery systems,
- Mechanisms to overcome resistance in cancer therapy using prodrugs,
- Pharmacokinetic, pharmacodynamic, and stability studies of prodrug systems,
- Clinical perspectives and regulatory aspects of prodrug development.
This Special Issue aims to provide a comprehensive overview of the current state and future directions of prodrug applications in oncology, fostering collaboration between researchers in drug design, formulation science, and preclinical and clinical pharmacology.
We look forward to your valuable contributions.
Prof. Dr. René C.-Gaudreault
Dr. Atziri Corin Chavez Alvarez
Guest Editors
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Keywords
- anticancer agents
- prodrugs
- targeted cancer therapy
- precision medicine
- translational oncology
- structure–activity relationship
- clinical oncology
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