Tofupill/Femarelle (DT56a): a new phyto-selective estrogen receptor modulator-like substance for the treatment of postmenopausal bone loss

Abstract

Tofupill treatment in postmenopausal women increases BMD without unwanted estrogenic effect. Tofupill appears to be a promising phyto-SERM for the prevention of postmenopausal osteoporosis.

DT56a stimulates gender-specific human cultured bone cells in vitro

“…DT56a was shown in previous clinical studies to be an effective agent in preventing postmenopausal osteoporosis [18], with no effect on the uterus. Bone loss induced by ovariectomy in female rats, has been widely used as a model for studying postmenopausal osteoporosis [26][27][28][29][30][31][32].…”

“…Femarelle has been shown to increase bone mineral density in postmenopausal women [18] and to relieve vasomotor symptoms with no effect on sex hormone levels or endometrial thickness [19]. Its properties as a SERM were shown in previous studies: Rats were fed for 4 days with estradiol-17␤ (E 2 ) or DT56a.…”

DT56a (Femarelle), contrary to estradiol-17β, is effective in human derived female osteoblasts in hyperglycemic condition

“…Femarelle increased bone mineral density in postmenopausal women [21] and relieved vasomotor symptoms with no effect on sex hormone levels or endometrial thickness [21]. Its SERM properties were shown in previous studies in rat model [22,23] and in MCF-7 human breast cancer cell-line [24].…”

Les SERM(s)

“…En particulier, le DT 56a, un nouveau phyto-SERM, pourrait agir dans la prise en charge de l'ostéoporose en stimulant la formation osseuse [43].…”