Bazedoxifene/conjugated estrogens for menopausal symptom treatment and osteoporosis prevention

ABSTRACT

Postmenopausal women with vasomotor and vaginal symptoms are commonly treated with estrogens or combined estrogen/progestin therapy (hormone therapy). However, hormone therapy is associated with some safety and tolerability concerns and its benefit/risk profile may vary for women based on their time since menopause. The tissue selective estrogen complex (TSEC) pairs a selective estrogen receptor modulator with one or more estrogens, with the goal of relieving menopausal symptoms and preserving bone mineral density without stimulating the breast or endometrium. Bazedoxifene/conjugated estrogens (BZA/CE) is the first TSEC in clinical development. BZA 20 mg/CE 0.45 and 0.625 mg have been shown in phase-3 clinical trials to significantly improve hot flushes and vulvar/vaginal atrophy measures in symptomatic postmenopausal women and to prevent bone loss in postmenopausal women at risk for osteoporosis while ensuring endometrial safety. These doses of BZA/CE have also demonstrated significant improvements in quality-of-life scores, sleep parameters, and treatment satisfaction compared with placebo. BZA 20 mg/CE 0.45 and 0.625 mg showed high cumulative rates of amenorrhea and low rates of breast pain, similar to those with placebo. The favorable treatment effects seen with BZA/CE were generally consistent in women < 5 or ≥ 5 years since menopause. Based on its demonstrated efficacy and safety in women both closer to or further from menopause, BZA/CE may be an appropriate alternative to hormone therapy for the treatment of menopausal symptoms and the prevention of osteoporosis.

Key words::

• TISSUE SELECTIVE ESTROGEN COMPLEX
• TSEC
• BAZEDOXIFENE
• CONJUGATED ESTROGENS
• MENOPAUSE
• OSTEOPOROSIS
• VASOMOTOR SYMPTOMS

ACKNOWLEDGEMENTS

Medical writing support for this manuscript was provided by Katie Gersh, PhD, of MedErgy and was funded by Pfizer Inc. The authors retained full editorial control over the content of the article.

Conflict of interest J. Pinkerton has served as a consultant (fees to the University of Virginia) for Pfizer Inc, Teva, Depomed, Noven, and NovoNordisk, received grants/research support (fees to the University of Virginia) from Pfizer Inc, Depomed, Bionova, and Endoceutics, and has served on a Data Safety Monitoring Board for Boehringer Ingelheim. J. Pickar and J. Racketa are former employees of Wyeth Research/Pfizer Inc. J. Pickar has served as a consultant for Wyeth, Depomed, BHR Pharma, Bionovo, and ASCEND Therapeutics. S. Mirkin is a current employee of Pfizer Inc.

Source of funding Medical writing support for this manuscript was provided by Katie Gersh, PhD, of MedErgy and was funded by Pfizer Inc.