What is the Origin of GnRH Analogue Therapy?

The therapy is based on the discovery and subsequent synthesis of the native GnRH decapeptide. Scientists developed "analogues" to improve the peptide's pharmacological properties, such as its half-life and potency, for clinical use. The observation that continuous, non-pulsatile administration of GnRH agonists paradoxically suppresses the pituitary led to the development of this therapy for downregulating sex hormone production.

What is the Mechanism of GnRH Analogue Therapy?

GnRH analogues function through two main mechanisms depending on the molecule: Agonists, when administered continuously, initially cause a surge but then desensitize the pituitary GnRH receptors, leading to a profound suppression of gonadotropin and sex steroid production, a process called chemical castration. Antagonists, conversely, immediately and competitively block the GnRH receptor, resulting in rapid suppression of the reproductive hormones. Both mechanisms are employed to achieve therapeutic hypoestrogenism or hypoandrogenism.

GnRH Analogue Therapy

Meaning

GnRH analogue therapy involves the clinical use of synthetic compounds that structurally resemble Gonadotropin-releasing hormone, the hypothalamic peptide that controls the release of luteinizing hormone and follicle-stimulating hormone from the pituitary gland. These agents are designed to either suppress or stimulate the reproductive axis, finding application in managing conditions such as endometriosis, prostate cancer, and precocious puberty. The choice between agonist and antagonist analogues dictates the specific therapeutic outcome.