Current and Evolving Approaches to Individualizing Estrogen Receptor-Based Therapy for Menopausal Women

Santen RJ1,Kagan R, Altomare CJ,Komm B, Mirkin S,Taylor HS. J Clin Endocrinol Metab. 2014 Jan 1:jc20133680 PMID:24423357
Adding progestogens to estrogens changes the risk profile of hormonal therapy for menopausal women, and recent data support the need for progestogen-free options. Several current
and evolving approaches to managing estrogen deficiency allow for progestogen
omission. We review the mechanisms of estrogen activity and provide an overview
of emerging and available estrogen receptor (ER)-based therapies. Advances in
our understanding of ER pharmacology have led to therapies designed to optimize
ER activity, including selective-estrogen receptor modulators (SERMs) and
tissue-selective estrogen complexes (TSECs). Each estrogen, SERM, and TSEC
exhibits a unique profile of tissue-specific activity, spanning the spectrum
from ER agonism to antagonism. Systemic estrogens unopposed by progestogens
effectively manage menopausal symptoms in hysterectomized postmenopausal women
but require progestogen use in postmenopausal women with a uterus. SERMs are
effective for managing certain aspects of estrogen deficiency in postmenopausal
women, but data suggest pairing a SERM with estrogens to form a TSEC provides a
more optimal therapeutic profile for women with a uterus. Treating signs and
symptoms of estrogen deficiency requires an individualized approach based on a
woman's goals and the purported risks of different therapies. New and emerging
agents have demonstrated efficacy in postmenopausal women with a uterus, while
allowing these women to avoid progestogens and their possible adverse effects.
Comment- This review offers an extensive contemporary analysis of approaches to
treating menopausal symptoms, and is valuable read for anyone managing such