[Next generation selective estrogen receptor modulators].
Selective estrogen receptor modulators (SERMs) have the potential to provide the skeletal benefits of estrogen without the increased risk of uterine and breast cancer. Raloxifene, second generation SERM has been approved for the prevention and treatment of osteoporosis. Lasofoxifene (LAS) and bazedoxifene (BZA, TSE-424), novel SERMs, act as a tissue selective estrogen antagonist or agonist. These novel SERMs inhibited bone turnover and prevented bone loss caused estrogen deficiency. Furthermore, these SERMs did not affect the uterine endometrial thickness and reduced serum cholesterol. These date suggest that LAS and TSE-424 are novel potential therapy for the prevention of osteoporosis in postmenopausal women.
Chaki
Osamu
O
Section of Gynecology, Yokohama City University Medical Center.
D000818:Animals; D015519:Bone Density / Q000187:drug effects; D050071:Bone Density Conservation Agents / Q000494:pharmacology*; D002784:Cholesterol / Q000097:blood; D005260:Female; D006801:Humans; D007211:Indoles / Q000494:pharmacology; D010024:Osteoporosis / Q000188:drug therapy; D011759:Pyrrolidines / Q000494:pharmacology; D020845:Selective Estrogen Receptor Modulators / Q000494:pharmacology*; D013764:Tetrahydronaphthalenes / Q000494:pharmacology; D014599:Uterus / Q000187:drug effects
D050071:Bone Density Conservation Agents; D007211:Indoles; D011759:Pyrrolidines; D020845:Selective Estrogen Receptor Modulators; D013764:Tetrahydronaphthalenes; C111332:Lasofoxifene; D002784:Cholesterol; C447119:bazedoxifene