Effects of ospemifene and raloxifene on hormonal status, lipids, genital tract, and tolerability in postmenopausal women.
OBJECTIVE
To compare ospemifene and raloxifene regarding their effects on hormones, lipids, genital tract, and tolerability in postmenopausal women.


METHODS
A randomized, double-blind study in which 118 healthy postmenopausal women received 30 (n = 29), 60 (n = 30), or 90 mg (n = 30) of ospemifene or 60 mg (n = 29) of raloxifene for 3 months.


RESULTS
There were no significant differences in the baseline characteristics between study groups. In comparison with raloxifene, follicle-stimulating hormone levels decreased significantly more in the 90-mg ospemifene group and sex hormone-binding globulin levels increased more in all ospemifene groups. Total cholesterol and low-density lipoprotein cholesterol levels decreased more in raloxifene than in ospemifene groups, although the difference in low-density lipoprotein cholesterol between 90-mg ospemifene and raloxifene was not significant. Endometrial thickness did not change in any study group and endometrial biopsies showed atrophy in the majority of subjects at 3 months. All ospemifene groups demonstrated a clear estrogenic effect on the vaginal epithelium, as seen in Pap smears. This was in sharp contrast to the raloxifene group, which had no effect on the vaginal epithelium. Kupperman index decreased in all study groups during treatment. The adverse events were mild, mainly single cases, and no clustering of events was observed. There were no clinically significant abnormal findings in laboratory safety parameters.


CONCLUSIONS
Ospemifene, at the dose of 90 mg/day, was more estrogenic than raloxifene, as shown by changes in serum follicle-stimulating hormone and sex hormone-binding globulin levels. Neither agent stimulated endometrium, but in contrast to raloxifene, ospemifene had a clear estrogenic effect in the vagina. Further studies with ospemifene are needed in subjects with vaginal atrophy.
Komi
Janne
J
Hormos Medical Corporation, Turku, Finland.
Lankinen
Kari S
KS
Härkönen
Pirkko
P
DeGregorio
Michael W
MW
Voipio
Sari
S
Kivinen
Seppo
S
Tuimala
Risto
R
Vihtamäki
Tarja
T
Vihko
Kimmo
K
Ylikorkala
Olavi
O
Erkkola
Risto
R
D004311:Double-Blind Method; D004334:Drug Administration Schedule; D005260:Female; D005640:Follicle Stimulating Hormone / Q000097:blood; D019584:Hot Flashes / Q000188:drug therapy* / Q000473:pathology; D006801:Humans; D008055:Lipids / Q000097:blood; D008875:Middle Aged; D017698:Postmenopause; D020849:Raloxifene Hydrochloride / Q000008:administration & dosage*; D020845:Selective Estrogen Receptor Modulators / Q000008:administration & dosage*; D012738:Sex Hormone-Binding Globulin / Q000187:drug effects; D013629:Tamoxifen / Q000008:administration & dosage* / Q000031:analogs & derivatives*; D016896:Treatment Outcome; D014599:Uterus / Q000166:cytology / Q000187:drug effects; D014621:Vagina / Q000166:cytology / Q000187:drug effects
D008055:Lipids; D020845:Selective Estrogen Receptor Modulators; D012738:Sex Hormone-Binding Globulin; D013629:Tamoxifen; D020849:Raloxifene Hydrochloride; D005640:Follicle Stimulating Hormone; C119141:Ospemifene