Bazedoxifene
Hormonal / PCTAlso known as: Duavee, Viviant, Bazedoxifene Acetate, TSE-424
Mechanism
Bazedoxifene is a third-generation SERM FDA-approved in combination with conjugated estrogens (as Duavee) for menopausal vasomotor symptoms and osteoporosis prevention. It uniquely acts as both an ER antagonist and an ER degrader (SERM/SERD hybrid), providing strong anti-estrogenic effects in breast and uterus while allowing bone protection.
Technical detail
Bazedoxifene is an indole-derived third-generation SERM with unique SERM/SERD hybrid properties — it antagonizes ER in breast and uterus while also promoting ER-alpha degradation via the ubiquitin-proteasome pathway, distinguishing it from classical SERMs. It prevents estrogen-stimulated endometrial hyperplasia when combined with conjugated estrogens (tissue-selective estrogen complex/TSEC concept). The SMART trials demonstrated non-inferior bone mineral density preservation with endometrial safety. As Duavee, it provides menopausal symptom relief with reduced breast/uterine stimulation risk.