tamoxifen + melatonin

Tamoxifen + melatonin refers to both the combination of the selective estrogen receptor modulator (SERM) tamoxifen with the neurohormone melatonin, and a series of novel, chemically synthesized drug conjugates (e.g., C4, C5). These conjugates covalently link tamoxifen and melatonin via carbon chain spacers of varying lengths to create hybrid molecules. Developed by researchers at Tulane University and Duquesne University, these compounds are designed to treat estrogen receptor-positive (ER+), tamoxifen-resistant, and triple-negative breast cancers (TNBC). The conjugates aim to maintain the anti-tumor efficacy of tamoxifen while potentially offsetting its adverse effects, such as increased uterine cancer risk and the development of drug resistance, by incorporating the oncostatic properties of melatonin. Mechanistically, they target both the estrogen receptor alpha (ESR1) and melatonin MT1 receptors, showing the ability to inhibit tumor growth in models of estrogen-resistant breast cancer without the uterotropic effects typically associated with tamoxifen.

Other names

Melatonin-tamoxifen drug conjugatesTamoxifen-melatonin hybrids