Drug intelligence / Profile preview

17β-estradiol + micronized progesterone

Development stage
Phase 4
Lead developer
TherapeuticsMD
Modality
Small Molecules
Administration
Transdermal, Oral
01

Overview

This hormone replacement therapy regimen consists of a 100-μg 17β-estradiol transdermal patch administered continuously, paired with 200 mg of cyclic oral micronized progesterone for 12 days each month. Developed and studied by researchers at Massachusetts General Hospital, this physiologic replacement strategy is designed to treat bone loss in adolescent and young adult female athletes with hypothalamic amenorrhea or oligoamenorrhea. Unlike oral contraceptives, which can suppress IGF-1 levels and potentially hinder bone accrual, this transdermal delivery bypasses first-pass hepatic metabolism, maintaining IGF-1 levels and more effectively improving bone mineral density at the spine and hip. The regimen aims to optimize peak bone mass during the critical window of adolescent development.

Other names
Physiologic estrogen replacementTransdermal estradiol and cyclic progesterone
02

Targets

ER (Estrogen receptor)PR (Progesterone receptor)PGRMC1PGRMC2 (Progesterone receptor membrane component 2)mPRα (Membrane progesterone receptor alpha)mPRβ (Membrane progesterone receptor beta)

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