Studies have shown that EPZ6438, the FDA-approved EZH2 inhibitor, has marginal effect on the growth of TNBC cells.58 Recently, proteolytic targeting chimeras (PROTACs) and hydrophobic tagging technology demonstrated the possibility of degrading EZH2 with promising results in preclinical studies of breast cancer.33,34 Thus, an irreversible inhibitor with enzymatic inhibition combined with depletion or degradation of EZH2 has potential therapeutic benefit for EZH2-highly expressed TNBC or other related malignancies. Here, EZH2 is linked to breast cancer.