Bazedoxifene: a novel selective estrogen receptor modulator for postmenopausal osteoporosis. 2010

T J de Villiers
Panorama MediClinic and University of Stellenbosch, Cape Town, South Africa.

Several new selective estrogen receptor modulators (SERMs) are currently under clinical development for the prevention and/or treatment of postmenopausal osteoporosis, with the goal of optimizing the estrogen receptor agonist/antagonist activity in target tissues. Bazedoxifene is a novel SERM under clinical investigation for the prevention and treatment of postmenopausal osteoporosis. Emerging clinical data have shown that bazedoxifene is effective in preventing bone loss and osteoporotic fractures in postmenopausal women, with no evidence of breast or endometrial stimulation. Two large, prospective, international phase 3 studies have been completed. In postmenopausal women at risk for osteoporosis, bazedoxifene has been shown to preserve bone mineral density and to reduce bone turnover. In postmenopausal women with osteoporosis, bazedoxifene has demonstrated significant protection against new vertebral fractures and against non-vertebral fractures in women at higher fracture risk. The treatment effects of bazedoxifene were supported by findings from independent re-analyses using the Fracture Risk Assessment Tool (FRAX), which showed that bazedoxifene significantly reduced the risk of all clinical and morphometric vertebral fracture and of non-vertebral fracture in women at or above a FRAX-based threshold. Bazedoxifene was generally safe and well tolerated in the phase 3 studies and showed neutral effects on the breast and an excellent endometrial safety profile; such attributes allow for the partnering of bazedoxifene with conjugated estrogens for menopausal symptom relief. Collectively, these results suggest that bazedoxifene may be a promising new therapy for the prevention and treatment of postmenopausal osteoporosis as a monotherapy or in combination with conjugated estrogens in menopausal hormone therapy.

UI MeSH Term Description Entries
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D008055 Lipids A generic term for fats and lipoids, the alcohol-ether-soluble constituents of protoplasm, which are insoluble in water. They comprise the fats, fatty oils, essential oils, waxes, phospholipids, glycolipids, sulfolipids, aminolipids, chromolipids (lipochromes), and fatty acids. (Grant & Hackh's Chemical Dictionary, 5th ed) Lipid
D008327 Mammography Radiographic examination of the breast. 3D-Mammography,Digital Breast Tomosynthesis,Digital Mammography,X-ray Breast Tomosynthesis,3D Mammography,3D-Mammographies,Breast Tomosyntheses, Digital,Breast Tomosyntheses, X-ray,Breast Tomosynthesis, Digital,Breast Tomosynthesis, X-ray,Digital Breast Tomosyntheses,Digital Mammographies,Mammographies,Mammographies, Digital,Mammography, Digital,X ray Breast Tomosynthesis,X-ray Breast Tomosyntheses
D004717 Endometrium The mucous membrane lining of the uterine cavity that is hormonally responsive during the MENSTRUAL CYCLE and PREGNANCY. The endometrium undergoes cyclic changes that characterize MENSTRUATION. After successful FERTILIZATION, it serves to sustain the developing embryo. Endometria
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D014463 Ultrasonography The visualization of deep structures of the body by recording the reflections or echoes of ultrasonic pulses directed into the tissues. Use of ultrasound for imaging or diagnostic purposes employs frequencies ranging from 1.6 to 10 megahertz. Echography,Echotomography,Echotomography, Computer,Sonography, Medical,Tomography, Ultrasonic,Ultrasonic Diagnosis,Ultrasonic Imaging,Ultrasonographic Imaging,Computer Echotomography,Diagnosis, Ultrasonic,Diagnostic Ultrasound,Ultrasonic Tomography,Ultrasound Imaging,Diagnoses, Ultrasonic,Diagnostic Ultrasounds,Imaging, Ultrasonic,Imaging, Ultrasonographic,Imaging, Ultrasound,Imagings, Ultrasonographic,Imagings, Ultrasound,Medical Sonography,Ultrasonic Diagnoses,Ultrasonographic Imagings,Ultrasound, Diagnostic,Ultrasounds, Diagnostic
D015663 Osteoporosis, Postmenopausal Metabolic disorder associated with fractures of the femoral neck, vertebrae, and distal forearm. It occurs commonly in women within 15-20 years after menopause, and is caused by factors associated with menopause including estrogen deficiency. Bone Loss, Perimenopausal,Bone Loss, Postmenopausal,Perimenopausal Bone Loss,Postmenopausal Bone Loss,Postmenopausal Osteoporosis,Osteoporosis, Post-Menopausal,Bone Losses, Perimenopausal,Bone Losses, Postmenopausal,Osteoporoses, Post-Menopausal,Osteoporoses, Postmenopausal,Osteoporosis, Post Menopausal,Perimenopausal Bone Losses,Post-Menopausal Osteoporoses,Post-Menopausal Osteoporosis,Postmenopausal Bone Losses,Postmenopausal Osteoporoses
D017326 Clinical Trials, Phase III as Topic Works about comparative studies to verify the effectiveness of diagnostic, therapeutic, or prophylactic drugs, devices, or techniques determined in phase II studies. During these trials, patients are monitored closely by physicians to identify any adverse reactions from long-term use. These studies are performed on groups of patients large enough to identify clinically significant responses and usually last about three years. This concept includes phase III studies conducted in both the U.S. and in other countries. Clinical Trials, Phase 3 as Topic,Drug Evaluation, FDA Phase 3 as Topic,Drug Evaluation, FDA Phase III as Topic,Evaluation Studies, FDA Phase 3 as Topic,Evaluation Studies, FDA Phase III as Topic
D050723 Fractures, Bone Breaks in bones. Bone Fractures,Broken Bones,Spiral Fractures,Torsion Fractures,Bone Fracture,Bone, Broken,Bones, Broken,Broken Bone,Fracture, Bone,Fracture, Spiral,Fracture, Torsion,Fractures, Spiral,Fractures, Torsion,Spiral Fracture,Torsion Fracture

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