Is artesunate (repurposed drug) effective as a treatment for prostate cancer?

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Artesunate as a Repurposed Drug for Prostate Cancer

Artesunate is not recommended for prostate cancer treatment, as it lacks guideline support, has no proven survival benefit in clinical trials, and established therapies with demonstrated mortality and quality of life benefits are available.

Guideline Position on Repurposed Drugs

Major oncology societies explicitly recommend against using repurposed medications without proven survival benefit for prostate cancer treatment 1, 2. The European Society for Medical Oncology, American Society of Clinical Oncology, and National Comprehensive Cancer Network do not include artesunate in any treatment algorithms for prostate cancer 1.

Established First-Line Treatments with Proven Survival Benefits

For patients requiring systemic therapy, guideline-recommended options with demonstrated mortality benefits include:

Metastatic Hormone-Sensitive Disease

  • ADT plus docetaxel for fit patients with high-volume disease (HR 0.61 for overall survival) 3
  • ADT plus abiraterone for high-risk disease per LATITUDE trial 3
  • ADT plus enzalutamide (160 mg daily) with strong survival benefits 3
  • ADT plus apalutamide (240 mg daily) with improved radiographic progression-free and overall survival 3

Castration-Resistant Disease

  • Docetaxel-based chemotherapy remains standard with proven overall survival benefit (HR 0.76) 3
  • Abiraterone or enzalutamide for asymptomatic/mildly symptomatic chemotherapy-naïve patients 3, 2
  • Radium-223 for bone-predominant symptomatic disease (HR 0.70 for overall survival) 3
  • Cabazitaxel after docetaxel failure with survival benefit 3

Why Artesunate Cannot Be Recommended

Lack of Clinical Trial Evidence

While preclinical studies show artesunate inhibits growth of docetaxel-resistant prostate cancer cells through multiple mechanisms including G0/G1 arrest, apoptosis induction, and ferroptosis 4, these are laboratory findings only. No phase III randomized controlled trials have evaluated artesunate's impact on overall survival, prostate cancer-specific mortality, or quality of life in prostate cancer patients 4, 5.

Mechanistic Studies Are Insufficient

Research demonstrates artesunate can restore sensitivity to antiandrogens in castrate-resistant cells by targeting NF-κB signaling and inducing AR degradation 5. Animal studies show tumor regression in xenograft models 5. However, these preclinical findings have not translated into human clinical trials demonstrating survival benefit, which is the mandatory standard for prostate cancer treatment recommendations 1, 2.

Safety Concerns in Cancer Context

While artesunate has established safety as an antimalarial drug 6, 7, its safety profile specifically in cancer patients receiving concurrent standard therapies (docetaxel, novel hormone agents) remains undefined. The cardiovascular toxicity concerns noted with other repurposed agents underscore the need for rigorous clinical trial data 1.

Clinical Decision Algorithm

For any prostate cancer patient, prioritize treatments in this order:

  1. Determine disease stage and risk category using PSA, Gleason score, imaging, and castration status 3

  2. For metastatic hormone-sensitive disease:

    • Offer ADT plus novel hormone agent (abiraterone, enzalutamide, or apalutamide) 3, 2
    • Consider ADT plus docetaxel for fit patients with high-volume disease 3
    • Consider triplet therapy (ADT + docetaxel + novel hormone agent) for fit patients with de novo metastatic disease 2
  3. For castration-resistant disease:

    • First-line: Abiraterone or enzalutamide if chemotherapy-naïve 3, 2
    • Docetaxel for symptomatic patients or rapidly progressing disease 3
    • Radium-223 for bone-predominant symptomatic disease without visceral metastases 3
  4. After progression on first-line therapy:

    • Cabazitaxel, alternative novel hormone agent, or olaparib (if BRCA1/2 mutations) 3, 2
    • 177Lu-PSMA-617 for PSMA-expressing tumors after taxane and AR axis inhibitor 2

Critical Pitfalls to Avoid

Do not delay proven therapies to trial unproven repurposed drugs, as this directly compromises survival outcomes 1. The window for effective intervention in metastatic prostate cancer is time-sensitive, particularly in high-volume or rapidly progressing disease 3.

Do not confuse preclinical activity with clinical efficacy. Artesunate's demonstrated activity against cancer cell lines 4, 7 and its ability to sensitize cells to chemotherapy 8 are hypothesis-generating only and do not substitute for phase III trial evidence of survival benefit.

Recognize that "low toxicity" in malaria treatment does not guarantee safety when combined with cytotoxic chemotherapy or novel hormone agents in cancer patients with different comorbidity profiles 1.

References

Guideline

Fosfestrol in Prostate Cancer Treatment

Praxis Medical Insights: Practical Summaries of Clinical Guidelines, 2025

Guideline

Prostate Cancer Treatment Guidelines

Praxis Medical Insights: Practical Summaries of Clinical Guidelines, 2025

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

Anti-tumor mechanism of artesunate.

Frontiers in pharmacology, 2024

Research

The anti-malarial artesunate is also active against cancer.

International journal of oncology, 2001

Research

[Current research analysis and prospects on sensitization effect of artesunate on anti-cancer radiotherapy and chemotherapy].

Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica, 2019

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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