Related Experiment Video
Updated: Jun 12, 2025

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
Artesunate enhances the efficacy of enzalutamide in advanced prostate cancer
Xinyi Wang1, Jinghui Liu1, Fengyi Mao1
1Department of Toxicology and Cancer Biology, University of Kentucky, Lexington, Kentucky, USA.
Abstract:
Prostate cancer (PCa) is one of the leading causes of death among men worldwide. Treatments targeting the androgen receptor pathway remain the standard therapy for PCa patients. Enzalutamide (ENZ), a second-generation androgen receptor inhibitor, was developed to treat castration-resistant prostate cancer. However, while patients initially respond to ENZ, drug resistance typically develops within a few months. Artesunate (ART), a semisynthetic derivative of the Artemisinin plant, is approved for antimalaria treatment. In this study, we conducted an FDA-approved drug screening and identified ART as a potential candidate for overcoming ENZ resistance in PCa. Mechanistically, ART induces the degradation of c-Myc, enhancing the efficacy of ENZ. Additionally, patient dataset analysis revealed that c-Myc plays a significant role in developing ENZ resistance. To summarize, these findings suggest a novel therapeutic strategy for ENZ-resistant prostate cancer.
Insights
Artesunate (ART) can overcome enzalutamide (ENZ) resistance in prostate cancer by degrading c-Myc. This finding suggests a new therapeutic strategy for patients with advanced prostate cancer.
Area of Science:
- Oncology
- Pharmacology
Background:
- Prostate cancer (PCa) is a leading cause of cancer death in men.
- Androgen receptor pathway inhibitors like enzalutamide (ENZ) are standard PCa treatments.
- Enzalutamide resistance is a major clinical challenge in castration-resistant prostate cancer.
Purpose of the Study:
- To identify FDA-approved drugs that can overcome enzalutamide resistance in prostate cancer.
- To investigate the potential of artesunate (ART) as a therapeutic agent for enzalutamide-resistant PCa.
Main Methods:
- FDA-approved drug screening was performed to identify novel therapeutic candidates.
- The mechanism of action of artesunate in overcoming enzalutamide resistance was investigated.
- Patient datasets were analyzed to assess the role of c-Myc in enzalutamide resistance.
Main Results:
- Artesunate (ART) was identified as a promising drug for overcoming enzalutamide (ENZ) resistance in prostate cancer.
- ART enhances ENZ efficacy by inducing the degradation of c-Myc.
- Patient data analysis confirmed c-Myc's significant role in the development of ENZ resistance.
Conclusions:
- Artesunate represents a potential therapeutic strategy to combat enzalutamide resistance in prostate cancer.
- Targeting c-Myc degradation may be a viable approach to restore sensitivity to enzalutamide therapy.
More Related Videos
Related Concept Videos
Combined Effects of Drugs: Synergism
Such synergistic combinations...
Targeted Cancer Therapies
There are several types of targeted therapies against...
Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
Dose-Response Relationship: Potency and Efficacy
Antiepileptic Drugs: Potassium Channel Activators
Ezogabine has gained approval as an adjunctive treatment...
Tissue-Drug Binding: Localization of Drugs and its Significance
Drugs can bind to different tissue components, enhancing their distribution and localization. The factors influencing drug localization in tissues include the drug's lipophilicity, structural characteristics, tissue perfusion rate, and pH differences. These factors determine...

