MK-0752 + tamoxifen

MK-0752 + tamoxifen is an investigational combination therapy consisting of MK-0752, a potent oral small molecule inhibitor of gamma-secretase (Notch signaling pathway inhibitor), and tamoxifen, a selective estrogen receptor modulator (SERM). MK-0752 inhibits the Notch signaling pathway by blocking gamma-secretase activity, which is implicated in the pathogenesis of various cancers through its role in cell differentiation and proliferation[1][4][5][7]. Tamoxifen acts as an antagonist to the estrogen receptor in breast tissue and is widely used as hormonal therapy for hormone receptor-positive breast cancer. The combination has been explored preclinically and clinically for synergistic antitumor effects, particularly in cancers where both Notch signaling and estrogen receptor pathways are relevant.