zuclomiphene

Zuclomiphene is a non-steroidal triphenylethylene derivative that exhibits antiestrogenic properties. It is the cis-isomer of clomiphene. Zuclomiphene functions as a selective estrogen receptor modulator (SERM). It binds to estrogen receptors, and its effect depends on the specific tissue and the presence of endogenous estrogen. In some tissues, it acts as an antagonist, blocking the effects of estrogen, while in others, it can act as an agonist, mimicking estrogen's effects.

Historically, zuclomiphene, often in combination with its trans-isomer (transclomiphene), was developed as a medication for infertility. The combined formulation, known as clomiphene citrate, has been widely used to induce ovulation in women with ovulatory dysfunction. Zuclomiphene's antiestrogenic action at the hypothalamus and pituitary gland is thought to lead to increased secretion of gonadotropins, specifically follicle-stimulating hormone (FSH) and luteinizing hormone (LH), which in turn stimulates follicular development and ovulation.

While clomiphene citrate remains a common treatment, the specific role and therapeutic applications of zuclomiphene as a single agent are less prominent. Research has investigated its potential in other areas, but its primary historical and current relevance is as a component of clomiphene citrate in reproductive medicine. Side effects associated with clomiphene citrate, which can be attributed to the actions of both isomers, may include hot flashes, abdominal discomfort, and visual disturbances.