Table I.
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.