Conjugated Estrogens and Bazedoxifene

Abstract

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Duavee: a tissue-selective estrogen complex for menopausal symptoms and prevention of osteoporosis

“…Of the three combinations, BZA-estradiol pair was more effective in antagonizing the stimulatory effects of estradiol than RLX or lasofoxifene (p<0.05). 3,6 Similar finding was observed in ovariectomized cynomolgus monkeys where daily doses of BZA 20 mg/CE 0.45 mg and 0.625 mg reduced endometrial proliferation. 9 In another study with ovariectomized sexually immature mice, BZA, RLX and lasofoxifene in doses of 2 mg/kg, 10 mg/kg, and 2 mg/kg, respectively, were combined with 3 mg/kg of CE.…”

“…It has agonistic action on bone tissue thus preventing osteoporosis and antagonistic action at endometrium and breast tissue, where it inhibits the proliferative effects of estrogen leading to decreased incidence of endometrial hyperplasia, uterine bleeding, and breast stimulation, respectively. 6,8 The pairing of BZA with CE is based on these favorable aspects which is lacking in other SERMS like raloxifene (RLX), tamoxifene, and lasofoxifene. 9…”

“…BZA undergoes enterohepatic circulation, so there is a possibility of some drug interactions because of this phenomenon. [5][6][7]…”

“…The common adverse reactions reported with the use of BZA/CE tablets in placebo-controlled trials included muscle spasms, nausea, diarrhea, dyspepsia, abdominal pain upper, oropharyngeal pain, dizziness, and neck pain. 6,10…”

“…5 This is the only TSEC to be approved by the regulatory authorities which retains the efficacy of estrogen in management of vasomotor symptoms, VVA and osteoporotic changes along with the additive protective effects of the SERM, BZA on breast and endometrial tissues. 6…”