Fluoxetine and reversal of multidrug resistance

Dan Peer, Rimona Margalit*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

70 Scopus citations


This review centers on recent findings with respect to modulating cancer multidrug resistance (MDR) with the well-known antidepressant fluoxetine (prozac). The MDR phenomena and mechanisms are discussed, including the roles of ABC transporters as MDR-pumps and the potential involvement of cancer stem cells. The three generations of MDR reversal agents (chemosensitizers) are reviewed, introducing the concept of single-pump and multi-pump agents. The current status of chemosensitization is summarized, pointing-out the need for additional agents and outlining experimental criteria for testing novel candidates. Major in vitro and in vivo findings are summarized showing that fluoxetine is a chemosensitizer of the multi-pump type, and proposing it be considered a fourth-generation chemosensitizer. In concluding, we contemplate future prospects of modulating MDR in the clinic.

Original languageEnglish
Pages (from-to)180-187
Number of pages8
JournalCancer Letters
Issue number2
StatePublished - 18 Jun 2006


  • ABC transporters
  • Chemosensitizers
  • Chemotherapy
  • Fluoxetine
  • Multidrug resistance (MDR)


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