Recent advances in endocrinology open a door for clinical application of 
selective estrogen receptor modulator (SERM) and selective progesterone receptor 
modulator (SPRM) in the treatment of uterine leiomyoma. With regard to SERM, 
treatment with raloxifene is shown to reduce leiomyoma size in postmenopausal 
women. Although raloxifene causes shrinkage of leiomyomas in combination with 
gonadotropin-releasing hormone agonist in premenopausal women, the effects of 
monotherapy with raloxifene on leiomyoma growth in premenopausal women remain 
controversial. By contrast, tamoxifen may not be suitable for long-term 
treatment of leiomyomas due to an agonistic action on the endometrium. Treatment 
with progesterone antagonist (RU486) or SPRM (J867) has been demonstrated to 
inhibit leiomyoma growth and improve clinical symptoms in premenopausal women. 
No serious adverse effects associated with SERM or SPRM have been reported. In 
light of therapeutic efficacy and few adverse effects, SERM and SPRM may hold 
promise as novel treatment modalities for leiomyoma. Further studies are 
warranted to determine the optimal strategy for the treatment of leiomyoma with 
SERM and SPRM.