Bazedoxifene (Conbriza®, Viviant®) is the first third-generation
selective estrogen receptor modulator (
SERM) and it is approved for the treatment of
postmenopausal osteoporosis in the EU and Japan.
Bazedoxifene contains an
indole-based core binding domain that binds with high affinity to
estrogen receptors and exhibits favourable effects on bone and
lipid profiles, with no clinically relevant endometrial or breast stimulation. Oral
bazedoxifene once daily reduced the incidence of new vertebral fractures in patients with
postmenopausal osteoporosis in a large, well designed trial of 3 years' duration; both
bazedoxifene and
raloxifene were significantly more effective than placebo. Neither
bazedoxifene nor
raloxifene reduced the incidence of nonvertebral fractures in the overall study population; however,
bazedoxifene, but not
raloxifene, reduced the rate of nonvertebral fractures in high-risk patients. Moreover, data from patients who continued to receive the
drug during a 2-year extension phase of this trial indicate that
bazedoxifene continues to provide protection against new vertebral fractures for up to 5 years.
Bazedoxifene also increases bone mineral density and reduces the levels of bone turnover markers.
Bazedoxifene was generally well tolerated and did not detrimentally affect the reproductive tract or breast tissue in clinical trials, thereby demonstrating a favourable risk-benefit profile. A pharmacoeconomic analysis conducted from an EU perspective predicted
bazedoxifene to be cost effective in some EU countries. Therefore,
bazedoxifene presents another useful option for the treatment of
postmenopausal osteoporosis, especially in those at high risk for
osteoporotic fracture.