What is the Origin of Clomiphene Citrate Use?

Clomiphene citrate was developed in the 1960s and quickly became a foundational drug in reproductive endocrinology, initially for treating female infertility. Its use in male hormonal health emerged from a deeper understanding of the HPG axis feedback loops, demonstrating its utility as an alternative to exogenous testosterone replacement therapy.

What is the Mechanism of Clomiphene Citrate Use?

Clomiphene acts as an estrogen receptor antagonist in the hypothalamus and pituitary gland, tricking these centers into sensing low estrogen levels. In response, the hypothalamus increases the pulsatile release of Gonadotropin-Releasing Hormone (GnRH), which subsequently stimulates the pituitary to release Follicle-Stimulating Hormone (FSH) and Luteinizing Hormone (LH). LH then signals the testes to increase testosterone biosynthesis, effectively raising serum testosterone levels while maintaining testicular function.

Clomiphene Citrate Use ∞ Area

Clomiphene Citrate Use

Meaning

The clinical administration of the non-steroidal selective estrogen receptor modulator (SERM) clomiphene citrate, primarily to stimulate the hypothalamic-pituitary-gonadal (HPG) axis. In men, it is often utilized off-label to increase endogenous testosterone production by preventing estrogenic negative feedback on the hypothalamus and pituitary gland. In women, its traditional role is to induce ovulation in cases of anovulatory infertility.