droloxifene

Droloxifene is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group and an analogue of tamoxifen. It was developed for the treatment of breast cancer, osteoporosis in men and postmenopausal women, and cardiovascular disorders but was never marketed. Droloxifene has a high affinity for estrogen receptors—10 to 60 times higher than tamoxifen—and exhibits both antiestrogenic effects in breast tissue and partial estrogen agonist effects in bone and liver. In clinical studies it showed less partial estrogen agonistic activity compared to tamoxifen. Droloxifene decreases luteinizing hormone (LH) and follicle-stimulating hormone (FSH), increases sex hormone-binding globulin levels (indicating hepatic estrogenic activity), induces apoptosis in breast cancer cells, inhibits bone resorption/turnover in animal models of postmenopausal osteoporosis without causing uterine hypertrophy or liver tumors seen with some other SERMs. Despite promising pharmacological properties—including rapid pharmacokinetics—it was found to be less effective than tamoxifen for advanced breast cancer treatment in phase III trials; development was discontinued around 2000[2][4][5][8].

Other names

3-hydroxytamoxifen3-OH-TAM