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Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
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Related Experiment Video

Updated: Jan 14, 2026

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Published on: February 17, 2023

Dexamethasone-Appended Activatable Prodrug Overcoming Multidrug Resistance.

Jungryun Kim¹, Chong Hu², Paramesh Jangili¹

¹Department of Chemistry, Korea University, Seoul 02841, Korea.

Journal of Medicinal Chemistry

|October 23, 2025

Summary

This summary is machine-generated.

This study developed Dex-Dox, a novel prodrug that overcomes chemotherapy resistance. Dex-Dox effectively reduced tumor volumes in drug-resistant models, offering a promising strategy for cancer therapy.

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The Clinical Application of Tumor Treating Fields Therapy in Glioblastoma

The Clinical Application of Tumor Treating Fields Therapy in Glioblastoma

Published on: April 16, 2019

Area of Science:

Oncology
Drug Development
Biochemistry

Background:

Residual tumor cells post-chemotherapy often display multidrug resistance (MDR) and increased invasiveness, leading to metastasis and recurrence.
Overcoming MDR is crucial for improving cancer treatment efficacy and patient outcomes.

Purpose of the Study:

To develop and evaluate a novel reactive oxygen species (ROS)-responsive prodrug, Dex-Dox, for overcoming MDR in tumor cells.
To assess the in vitro and in vivo efficacy of Dex-Dox in drug-resistant cancer models.

Main Methods:

Conjugation of dexamethasone (Dex) with doxorubicin (Dox) via an oxidative stress-responsive linker to create the Dex-Dox prodrug.
In vitro assessment of Dex-Dox's effect on drug-resistant cells, including apoptosis induction and anti-angiogenesis activity.
In vivo therapeutic evaluation and histological analysis in a Dox-resistant tumor mouse model.

Main Results:

Dex-Dox demonstrated significant enhancement of drug sensitivity, promoted apoptosis, and inhibited angiogenesis in drug-resistant cells in vitro.
In vivo studies showed that Dex-Dox substantially reduced tumor volumes, particularly in a Dox-resistant mouse model.
Dexamethasone alone did not exhibit antitumor activity, highlighting the prodrug's specific mechanism.

Conclusions:

Dex-Dox is a potent ROS-responsive prodrug effective against multidrug-resistant cancer cells.
The findings underscore Dex-Dox's potential as an innovative therapeutic strategy to combat MDR in cancer treatment.
Further investigation into Dex-Dox could lead to improved clinical outcomes for patients with resistant tumors.