Related Experiment Video
Updated: Jan 16, 2026
Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Exploring Potential for Repurposing Antiretroviral Drugs Etravirine and Efavirenz in Prostate and Bladder Cancer
Mariana Pereira1,2,3, Nuno Vale1,3,4
1PerMed Research Group, RISE-Health, Faculty of Medicine, University of Porto, Alameda Professor Hernâni Monteiro, 4200-319 Porto, Portugal.
Abstract:
Background/Objectives: Prostate and bladder cancers are significant global health challenges with increasing incidence and limited treatment options in advanced stages. Drug repurposing offers a cost-effective strategy to accelerate the development of new anticancer therapies. This study investigated the antitumor activity of the non-nucleoside reverse transcriptase inhibitors efavirenz (EFV) and etravirine (ETV) in prostate and bladder cancer models. Methods: PC-3 prostate cancer and UM-UC-5 bladder cancer cell lines were treated with EFV, ETV, or their combination. Cell viability was assessed at 24, 48, and 72 h to evaluate time and concentration-dependent effects. Wound-healing assays were used to measure cell migration, and clonogenic assays assessed long-term proliferative capacity. Results: Both EFV and ETV decreased cell viability in a time and dose-dependent manner. ETV showed greater potency in PC-3 cells, while EFV demonstrated more consistent effects in UM-UC-5 cells. Combination treatment enhanced cytotoxicity, particularly at 48 and 72 h, suggesting potential synergy. Wound-healing assays indicated impaired migration in UM-UC-5 cells treated with ETV or the EFV + ETV combination. Clonogenic assays confirmed reduced long-term proliferation in both cell lines following treatment. Conclusions: EFV and ETV exhibit selective anticancer activity in prostate and bladder cancer cells, with enhanced effects when combined. These findings support their potential as repurposed therapeutic agents and warrant further preclinical evaluation for prostate and bladder cancer therapy.
Insights
Efavirenz (EFV) and etravirine (ETV), repurposed drugs, show anticancer effects against prostate and bladder cancer cells. Combination therapy enhances their effectiveness, suggesting potential for new cancer treatments.
Area of Science:
- Oncology
- Pharmacology
- Drug Repurposing
Background:
- Prostate and bladder cancers present growing global health challenges.
- Advanced stages of these cancers have limited treatment options.
- Drug repurposing offers a cost-effective strategy for novel anticancer therapies.
Purpose of the Study:
- To investigate the antitumor activity of efavirenz (EFV) and etravirine (ETV) in prostate and bladder cancer models.
- To evaluate the efficacy of EFV and ETV as repurposed anticancer agents.
Main Methods:
- Utilized PC-3 prostate and UM-UC-5 bladder cancer cell lines.
- Assessed cell viability, migration (wound-healing assay), and long-term proliferation (clonogenic assay).
- Treated cells with EFV, ETV, or their combination, evaluating time and dose-dependent effects.
Main Results:
- EFV and ETV reduced cancer cell viability in a time- and dose-dependent manner.
- Combination treatment demonstrated enhanced cytotoxicity and potential synergy.
- Impaired cell migration and reduced long-term proliferation were observed.
Conclusions:
- EFV and ETV exhibit selective anticancer activity in prostate and bladder cancer cells.
- Combined EFV and ETV treatment shows enhanced efficacy.
- These findings support further preclinical evaluation of EFV and ETV for prostate and bladder cancer therapy.
