Estradiol valerate, sold for use by mouth under the brand name Progynova and for use by injection under the brand names Delestrogen and Progynon Depot among others, is an estrogen medication. Chemically it is the 17beta-valerate ester of 17beta-estradiol (C23H32O3, molar mass approximately 356.5 g/mol, CAS 979-32-8) and functions as a lipophilic prodrug that is enzymatically hydrolyzed to active estradiol and valeric acid after administration. The compound is a white to off-white crystalline powder with low water solubility and is formulated for oral tablets and intramuscular depot injections; depot injection produces sustained plasma estradiol levels through slow release from the oil vehicle while oral tablets undergo first-pass metabolism with more rapid systemic appearance of estradiol. Analytical control typically uses HPLC or LC-MS for assay and related substances, and the substance is characterized by its specific rotation, infrared profile, and chromatographic retention compared to reference standards.
Parent: Estradiol Valerate
Parent: Estradiol Valerate
Parent: Estradiol Valerate
Parent: Estradiol Valerate
Parent: Estradiol Valerate
Parent: Estradiol / Estradiol Valerate
Impurity and related-compound profiles for estradiol valerate batches commonly include free estradiol (from hydrolysis or incomplete esterification), estrone and 17alpha-estradiol (oxidation or isomerization products), residual valeric acid or valve-rate-related esters, trace amounts of higher or lower chain esters, oxidative degradation products and process-related residual solvents or catalysts. Typical pharmaceutical quality-control specifications aim for high assay purity, for example assay >= 98.0% by validated HPLC, with individual related substances frequently limited to no more than 0.5% each and total related substances commonly limited to no more than 2.0% subject to the product specification and regulatory monograph. Identification and quantitation are performed by validated chromatographic methods, with GC or headspace GC for volatile residues and ICP or related techniques for heavy metal limits.
Estradiol valerate is used to provide systemic estrogen activity in clinical settings such as menopausal hormone therapy, management of estrogen deficiency states, certain contraceptive combinations in some regions, transgender feminine hormone therapy, and controlled ovarian stimulation or endometrial preparation in assisted reproduction protocols. Its role is to supply estradiol after in vivo conversion of the ester to active estradiol.
Estradiol is the biologically active hormone (17beta-estradiol) while estradiol valerate is an esterified prodrug of estradiol. The valerate ester increases lipophilicity, alters absorption and release characteristics, and must be hydrolyzed by esterases to release active estradiol and valeric acid. Differences therefore lie in formulation, pharmacokinetics and routes of administration rather than the pharmacodynamic receptor activity of the liberated estradiol.
In IVF protocols estradiol valerate is used to prepare or support the endometrium and to provide controlled estrogen exposure during ovarian stimulation, luteal support or frozen embryo transfer cycles. After administration it is converted to estradiol which acts on the endometrium to promote proliferation and receptivity according to the timing and dosing schedule determined by the clinical protocol.
Progynova, an oral estradiol valerate formulation, delivers estradiol systemically after intestinal absorption and hepatic processing; it raises circulating estradiol concentrations to achieve estrogen replacement or modulation as indicated by the treatment regimen, restoring estrogen-dependent physiological effects once converted to active estradiol.
