Loperamide, an FDA-Approved antidiarrhea drug, effectively reverses the resistance of multidrug resistant MCF-7/MDR1 human breast cancer cells to doxorubicin-induced cytotoxicity

Yanfei Zhou, Rajagopalan Sridhar, Liang Shan, Wei Sha, Xinbin Gu, Saraswati Sukumar

Research output: Contribution to journalArticle


Loperamide is an FDA-approved antidiarrhea drug which acts on the μ-opioid receptors in the mesenteric plexus of large intestine and exhibits limited side effects. We hypothesized that loperamide might reverse the multidrug resistance (MDR) of human cancer cells to chemotherapeutic agents. MCF-7/MDR1 cells express high level of MDR1 and are resistant to doxorubicin. We found that loperamide significantly enhanced the cytotoxicity of doxorubicin to MCF-7/MDR1 cells in a dose-dependent manner. In conclusion, loperamide reversed the resistance of MCF-7/MDR1 cells to doxorubicin, suggesting that chemotherapy in combination with loperamide may benefit patients with MDR tumors once applied in clinic.

Original languageEnglish (US)
Pages (from-to)119-125
Number of pages7
JournalCancer Investigation
Issue number2
StatePublished - Feb 1 2012



  • Breast cancer
  • Doxorubicin
  • Loperamide
  • Multidrug resistance

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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