Drug intelligence / Profile preview

Quinestrol

Development stage
Unknown
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Quinestrol is a synthetic estrogen medication primarily used in hormone replacement therapy for menopausal symptom relief such as hot flashes. It has also been used to treat breast cancer and prostate cancer and has applications in gender-affirming hormone therapy for transgender women. Quinestrol is the 3-cyclopentyl ether of ethinyl estradiol; after oral administration it is stored in adipose tissue and slowly released as it is metabolized to its active form (ethinyl estradiol). Its mechanism of action involves binding to the estrogen receptor (ESR1), leading to regulation of gene transcription that mediates typical estrogenic effects on target tissues including the female reproductive tract and mammary gland. Quinestrol increases hepatic synthesis of sex hormone-binding globulin (SHBG) and suppresses follicle-stimulating hormone (FSH) from the anterior pituitary. In some countries it has been marketed alone or in combination with progestins as a long-term oral contraceptive; veterinary uses include fertility control in rodents[1][2][4][5].

Brand names
Agalacto-QuileaBasaquinesEstonEstrovisEstrovisterPlestrovisQui-LeaSolunaYueketing
Other names
Ethinyl estradiol 3-cyclopentyl etherEthinylestradiol cyclopentyl ether
02

Targets

ESR1 (ERα)ESR2 (ERβ)

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