Abstract: The management of resistance to endocrine therapy in breast cancer is more of a challenge, and the reversal of endocrine resistance has currently being extensively explored. Although the resistance mechanisms are complicated, researchers have designed massive trials, both in vivo and in vitro from tumor growth inhibition, signal transduction, apoptosis induction and cell cycle arrest, to reverse the drug resistance and maintain or even enhance the antiestrogen efficacy. To date, endocrine combined with targeted therapy has become the central focus of the research. This article will summarize the preclinical and clinical trials which aim to reverse the endocrine resistance and discuss the possible directions of future research.