Antiestrogenic Properties of Raloxifene

Mw, Draper; De, Flowers; Ja, Neild; Huster, WJ; Rl, Zerbe

doi:10.1159/000139284

Cited by 40 publications

(16 citation statements)

References 17 publications

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“…Data about the action of raloxifene on human pituitary secretion are, at present, few. In male volunteers the drug blunts estrogeninduced changes in serum gonadotropin levels (8). In premenopausal women, Baker et al (9) showed that raloxifene increases serum FSH and E2 levels, and reduces PRL concentrations by 10 -35% of basal values.…”

Section: Discussionmentioning

confidence: 99%

“…In fact, although some studies, performed in vitro or in rats, show that raloxifene acts as a pure estrogen antagonist at the pituitary level (5,6), others show that it exerts an estrogenic action on the hypothalamic -pituitary structures (7). In male volunteers, raloxifene blunts estrogen-induced changes in serum anterior pituitary hormone levels (8), whereas in premenopausal women, it does not alter the length of the menstrual cycle or the day of luteinizing hormone (LH) surge, but stimulates follicle-stimulating hormone (FSH) secretion, increases serum 17b-estradiol (E2) levels and decreases serum prolactin (PRL) values (9). In postmenopausal women, the effect of raloxifene on pituitary function has been little investigated, even though this drug is currently approved for the prevention of postmenopausal osteoporosis.…”

Section: Introductionmentioning

confidence: 99%

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Effects of long-lasting raloxifene treatment on serum prolactin and gonadotropin levels in postmenopausal women

Lasco

Cannavò²,

Gaudio³

et al. 2002

European Journal of Endocrinology

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Objective: To evaluate the effects of a 6 month administration of raloxifene hydrochloride, a selective estrogen receptor modulator which was recently approved for the prevention of osteoporosis, on serum gonadotropin and prolactin (PRL) levels and on TRH-stimulated PRL responsiveness in postmenopausal women who have not undergone estrogen replacement therapy. Design and methods: Sixteen healthy postmenopausal women were divided into two groups on the basis of their bone status, evaluated by dual energy X-ray absorptiometry at the lumbar level. Eight women (chronological age 52:4^4:1 (S.D.) years, menopausal age 42:4^3:9 years), in whom T-score L2 -L4 was less than 2 2.5 S.D., were treated with raloxifene (60 mg p.o.) administered daily for 6 months (group 1), while the other eight women (chronological age 52:6^2:5 years, menopausal age 42:13 :6 years), in whom the T-score L2 -L4 ranged between 21 and 22.5 S.D., were used as a control group (group 2). Serum PRL, FSH, LH and 17b-estradiol (E2) levels were evaluated at baseline and after 3 and 6 months of treatment. In all subjects, PRL responsiveness to TRH (200 mg i.v.) administration was evaluated at baseline and at the end of the study. Results: At baseline, mean PRL, LH and FSH levels were not significantly different in the two groups (PRL 133:6^21:7 vs 136:7^28:1 mIU=l (NS), LH 25:1^6:8 vs 24:4^6:7 mIU=ml (NS), FSH 74:42 5:0 vs 71:1^24:1 mIU=ml (NS), in group 1 and group 2 respectively). No significant variations in serum FSH and LH values, in either group, or in serum PRL levels in group 2, were observed at the 3 and 6 month examinations. On the contrary, serum PRL values decreased significantly in group 1 after 3 months ð100:1^47:7 mIU=l; P , 0:05Þ and 6 months ð81:5^30:2 mIU=l; P , 0:001Þ: At baseline, no significant differences were observed in the TRH-stimulated serum PRL peak between the groups (1015:4^30:5 vs 1030:2^25:7 mIU=l in group 1 and in group 2 respectively), while it decreased significantly at the 6 month examination in group 1 ð770:5^47:4 mIU=l; P , 0:001Þ and it was significantly lower than in group 2 ð1068:1^301:8 mIU=l; P ¼ 0:02Þ: Serum E2 was not detected at baseline and at each examination, in all patients. Conclusions: The decrease of PRL values induced by long-term raloxifene administration in postmenopausal women could be explained by a direct antiestrogenic effect of raloxifene on lactotrope cells or by the recently suggested increase of opiatergic tone on the hypothalamic -pituitary region.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Effects of long-lasting raloxifene treatment on serum prolactin and gonadotropin levels in postmenopausal women

Lasco

Cannavò²,

Gaudio³

et al. 2002

European Journal of Endocrinology

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“…Estrogens 22,407,408 Ovulation suppressants and anticancer Heroin and methadone 409 Opiates (in addicts) Clofibrate 410 Hypolipidemic 5-Fluorouracil 411 Anticancer Perphenazine 412 Tranquilizer Tamoxifen 413,414 Chemotherapy Raloxifene [414][415][416] Osteoporosis…”

Section: Increase Tbg Concentrationmentioning

confidence: 99%

Thyroid Function Testing

Weiss¹,

Refetoff

2016

Endocrinology: Adult and Pediatric

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“…HCl, [176] was developed to maintain the beneficial estrogenic activity on bone and lipids, while mimicking antiestrogenic activity on endometrial and breast tissues [179]. The initial use of raloxifene as a breast cancer drug [180] was aborted due to its poor performance in comparison to tamoxifen in laboratory model. However, it is being widely considered as a prophylactic therapy in the prevention of breast cancer in high-risk women [77].…”

Section: Raloxifenementioning

confidence: 99%

Medicinal Chemistry and Emerging Strategies Applied to the Development of Selective Estrogen Receptor Modulators (SERMs)

Musa¹,

Khan²,

Cooperwood³

2007

CMC

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Selective estrogen receptor modulators (SERMs), known previously as "antiestrogens", are a new category of therapeutic agents used for the prevention and treatment of diseases such as osteoporosis and breast cancer. SERMs act as ER-agonist in some tissues while acting as ER-antagonist in others based on conformational change of the receptors, particularly at the helix 12. Currently, there are two classes of clinically approved SERMs; triphenylethylene derivatives (e.g., tamoxifen) and benzothiophene derivatives (e.g., raloxifene). Tamoxifen, raloxifene and toremifene are the most widely used SERMs. Tamoxifen, an antagonist of the breast tissue, is the first clinically identified compound with noticeable SERM activity. Although tamoxifen has been very successful in breast cancer treatment, its agonistic effect on the uterus is said to be associated with increase risk of developing endometrial cancer. Ideally, it is presumed that SERMs should selectively act as an agonist in the bone and brain while simultaneously acting as an antagonist in the breast and uterus. Therefore, the therapeutic goal of SERMs is the prevention of estrogen deficiency diseases without promoting estrogen-associated tumor growth. Therefore, the objective of this review is to summarize various effects that have been applied in improving the tissue-selectivity of SERMs, highlighting the emerging understanding of their mechanism of actions in selected target tissues and the development of the SERMs. The significance in recent discovery of selective estrogen receptor alpha modulators, SERAMs will also be reviewed.

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Antiestrogenic Properties of Raloxifene

Cited by 40 publications

References 17 publications

Effects of long-lasting raloxifene treatment on serum prolactin and gonadotropin levels in postmenopausal women

Effects of long-lasting raloxifene treatment on serum prolactin and gonadotropin levels in postmenopausal women

Thyroid Function Testing

Medicinal Chemistry and Emerging Strategies Applied to the Development of Selective Estrogen Receptor Modulators (SERMs)

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