Human Reproduction Update, Vol.6, No.3 pp.212-224, 2000
© European Society of Human Reproduction and Embryology 2000; all rights reserved
A pharmacological review of selective oestrogen receptor modulators
Steven R. Goldsteincbajhjcb,
Suresh Siddhanticbaihedh,
Angelina V. Ciacciacbaihedh and
Leo Plouffe, Jrcbaihedh,1
cbajhjcb Department of Obstetrics
and Gynecology, NYU Medical Center, 530 First Ave., Suite 10N, New
York, NY 10016, and
cbaihedh Lilly Research
Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis,
Indiana 46285, USA
Received on September 27, 1999; accepted on March 6, 2000
Abstract
Selective oestrogen receptor modulators (SERMs) are
structurally diverse non-steroidal compounds that bind to oestrogen
receptors and produce oestrogen agonist effects in some tissues
and oestrogen antagonist effects in others. SERMs are being evaluated
for a number of oestrogen-related diseases, including post-menopausal
osteoporosis, hormone-dependent cancers, and cardiovascular disease.
Several compounds that exhibit a SERM profile are currently available
for clinical use, including clomiphene, tamoxifen, and toremifene
(which are triphenylethylenes) and raloxifene (a benzothiophene).
Clomiphene is used for the induction of ovulation in sub-fertile
women attempting pregnancy. Tamoxifen and toremifene are both used
to treat breast cancer. Tamoxifen may have beneficial effects on
bone mineral density and serum lipids. The effects of toremifene
on serum lipids are similar to that of tamoxifen. Both compounds
have stimulatory effects on the endometrium. Raloxifene, indicated
for the treatment and prevention of post-menopausal osteoporosis,
has beneficial effects on bone mineral density and serum lipids,
but does not increase the risk of endometrial hyperplasia or endometrial
cancer. Recently, raloxifene was shown to reduce the incidence of
vertebral fractures in otherwise healthy women with osteoporosis;
in the same study, a reduced incidence of breast cancer was also
observed. Similar to oestrogens, SERMs increase the incidence of
venous thromboembolism. Several newer compounds that exhibit a SERM
profile are also in clinical development, including other triphenylethylenes
(droloxifene, idoxifene) and benzothiophenes (LY353381·HCl),
benzopyrans (EM-800), and naphthalenes (CP-336,156).
Key words: clomiphene/ / raloxifene/ / SERMs/ / tamoxifen/ / toremifene
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