The Phosphodiesterase-5 Inhibitor Vardenafil Is a Potent Inhibitor of ABCB1/P-Glycoprotein Transporter Reversal of MDR by Vardenafil
2011

Vardenafil Reverses Drug Resistance in Cancer Cells

publication Evidence: moderate

Author Information

Author(s): Ding Pei-Rong, Tiwari Amit K., Ohnuma Shinobu, Lee Jeferson W. K. K., An Xin, Dai Chun-Ling, Lu Qi-Si, Singh Satyakam, Yang Dong-Hua, Talele Tanaji T., Ambudkar Suresh V., Chen Zhe-Sheng

Primary Institution: Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, St. John's University, Jamaica, New York, United States of America

Hypothesis

Can vardenafil reverse multidrug resistance (MDR) in cancer cells mediated by the ABCB1 transporter?

Conclusion

Vardenafil effectively reverses ABCB1-mediated drug resistance in cancer cells by blocking the drug efflux function of the transporter.

Supporting Evidence

  • Vardenafil significantly increased the intracellular accumulation of paclitaxel in ABCB1 overexpressing cells.
  • Vardenafil did not alter the expression of the ABCB1 protein in the tested cancer cells.
  • Vardenafil enhanced the cytotoxicity of anticancer drugs in ABCB1 overexpressing cells.

Takeaway

Vardenafil, a drug usually for erectile dysfunction, can help cancer treatments work better by stopping cancer cells from pushing out the medicine.

Methodology

The study used MTT assays to assess cytotoxicity and measured drug accumulation and efflux in various cancer cell lines.

Limitations

The study primarily focused on in vitro experiments, and further in vivo studies are needed to confirm the findings.

Statistical Information

P-Value

p<0.01

Statistical Significance

p<0.05

Digital Object Identifier (DOI)

10.1371/journal.pone.0019329

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