Drug intelligence / Profile preview

cyclofenil

Development stage
Discontinued
Lead developer
ASKA Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Cyclofenil is a synthetic, non-steroidal selective estrogen receptor modulator (SERM) that acts as a mixed agonist and antagonist of estrogen receptors. It was primarily used as a gonadotropin stimulant or ovulation inducer in women with anovulatory infertility and for menopausal hormone therapy. Cyclofenil works by blocking the actions of estrogens in the pituitary gland and hypothalamus, thereby disinhibiting the release of gonadotropins such as luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which can stimulate ovulation. In men, it can increase testosterone levels due to its progonadotropic effects but is not effective for this purpose in women. Cyclofenil binds to estrogen receptor beta (ERβ) and demonstrates tissue-dependent agonism or antagonism. The drug was withdrawn from most markets due to a high risk of hepatotoxicity[1][4][7].

Brand names
Sexovid
Other names
cyclofenilcyclofenil diphenol
02

Targets

ESR1 (ERα)ESR2 (ERβ)

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