Drug intelligence / Profile preview

estradiol valerate + dydrogesterone

Development stage
Phase 4
Lead developer
Abbott
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Estradiol valerate + dydrogesterone is an oral combination drug consisting of estradiol valerate (an estrogen) and dydrogesterone (a progestin). It is primarily used in menopausal hormone therapy for postmenopausal women to treat and prevent hot flashes and osteoporosis. Estradiol valerate acts as a prodrug that is converted into 17β-estradiol, the main endogenous estrogen in women. Dydrogesterone is a synthetic progestogen structurally similar to natural progesterone and provides endometrial protection against hyperplasia induced by estrogens. The combination relieves climacteric symptoms, preserves bone mineral density, improves cardiovascular risk profile by increasing HDL and decreasing LDL cholesterol levels, reduces insulin resistance, and offers predictable cycle control with low rates of noncyclical bleeding. It has also been studied as add-back therapy during GnRH agonist treatment for endometriosis to reduce pain symptoms and bone mass loss while minimizing adverse effects[1][2][4][5].

Brand names
FemostonClimaston
Other names
E2/DYDestradiol/dydrogesterone
02

Targets

PR (Progesterone receptor)GPER1 (G protein-coupled estrogen receptor 1)ESR2 (ERβ)ESR1 (ERα)

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