•Triterpenoids work as reversal agents for anticancer drug resistance treatment.•The chemical and anticancer properties of triterpenoids are introduced here.•The findings and mechanisms of triterpenoids reversing multidrug resistance (MDR) are summarized.•Triterpenoids might be the potential chemosensitizers for anticancer treatment. Overexpression of ATP-binding cassette (ABC) transporters in cancer cells results in multidrug resistance (MDR), which is one of the major obstacles in the treatment of cancer patients. None of the strategies to overcome MDR has been successfully applied in the clinic until now. Plenty of evidence shows that some triterpenoids function as reversal agents of MDR for anticancer drug resistance treatment. Here, we review the latest findings of reversing cancer MDR with triterpenoids. Findings are summarized showing that triterpenoids are MDR modulators and potential chemosensitizers. Finally, we contemplate future prospects of modulating MDR in the clinic.