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the tissue selective estrogen complex a promising new menopausal therapy组织选择性雌激素复杂的有前途的新治疗更年期.pdf

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the tissue selective estrogen complex a promising new menopausal therapy组织选择性雌激素复杂的有前途的新治疗更年期

Pharmaceuticals 2012, 5, 899-924; doi:10.3390/ph5090899 OPEN ACCESS pharmaceuticals ISSN 1424-8247 /journal/pharmaceuticals Review The Tissue Selective Estrogen Complex: A Promising New Menopausal Therapy Barry S. Komm * and Sebastian Mirkin Women’s Health, Pfizer Inc., 500 Arcola Rd., Collegeville, PA 19426, USA; E-Mail: sebastian.mirkin@ * Author to whom correspondence should be addressed; E-Mail: Barry.Komm@; Tel.: +1-484-865-2776; Fax: +1-484-865-4321. Received: 2 July 2012; in revised form: 18 August 2012 / Accepted: 24 August 2012 / Published: 4 September 2012 Abstract: Menopause is associated with health concerns including vasomotor symptoms, vulvar/vaginal atrophy (VVA), and osteoporosis. Estrogen therapy or combined estrogen-progestin therapy (EPT) are primary treatment options for menopausal symptom relief and osteoporosis prevention. Because EPT has been associated with some safety/tolerability concerns relating to undesirable effects of estrogen and progestin, alternative options are needed. The tissue selective estrogen complex (TSEC) is a novel class of agents pairing a selective estrogen receptor modulator (SERM) with 1 or more estrogens. The TSEC combines the established efficacy of estrogens on menopausal symptoms and bone with the protective effects of a SERM on the reproductive tract. The pairing of bazedoxifene (BZA) with conjugated estrogens (CE) has been evaluated in