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. 2014 Sep 8;21(1):1–12. doi: 10.1093/humupd/dmu048

Table I.

Medications that result in leiomyoma shrinkage and their effects in women.

Class Examples Mechanism of action Side effects Pregnancy category FDA approved for leiomyoma Tumors recur after cessation Comments
GnRH agonists Leuprolide, Triptorelin Abolishes GnRH pulsatility Menopausal symptoms, bone loss X Yes, leuprolide for preoperative anemia only Yes Initial flare effect; Requires add-back therapy after 6 months
GnRH antagonists Ganirelix, Elagolix Competitive inhibition of GnRH Menopausal symptoms, bone loss X No Yes Avoids flare effect of GnRH agonists; Elagolix is the only oral GnRH antagonist
SPRMs Ulipristal, Mifepristone Varied progesterone antagonism Endometrial thickening/hyperplasia X No Yes
Aromatase inhibitors Letrozole, Anastrozole Competitive inhibition of the aromatase enzyme Bone loss D No Yes Can cause follicular stimulation

FDA, Food and Drug Administration.

Pregnancy categories are based on FDA classifications (A–D, X), D = established evidence of fetal risk, but potential benefits may outweigh risks in select patients; X = established evidence of fetal risk, with risks of use in pregnant women clearly outweighing the benefits.