Kisspeptin

Snapshot

Kisspeptin (also called metastin) is an endogenous hypothalamic peptide hormone that activates gonadotropin-releasing hormone (GnRH) neurons and so drives luteinizing hormone release. The US Food and Drug Administration (FDA) places kisspeptin-10 in a compounding category for substances that may present significant safety risks⁴, and the World Anti-Doping Agency (WADA) prohibits kisspeptin and its agonist analogues at all times⁴.

In hypothalamic amenorrhea, kisspeptin-54 injection acutely stimulated gonadotropin release, but two weeks of repeated injections produced desensitization¹. A phase 2 trial found a single kisspeptin-54 injection triggered oocyte maturation in nearly all women at high risk of ovarian hyperstimulation syndrome, with no moderate or severe cases². In 2025, a randomized crossover trial found intranasal kisspeptin-54 raised luteinizing hormone in healthy adults and in women with hypothalamic amenorrhea, the first non-invasive route reported⁵. Studied preparations are kisspeptin-54 given by injection or nasal spray⁵ and synthetic receptor agonists such as MVT-602⁶; see Form comparison.

The FDA states that compounded kisspeptin-10 may pose risk for immunogenicity for certain routes, and that it lacks sufficient information to know whether harm occurs in humans⁴. In a randomized crossover trial, intravenous kisspeptin-54 did not alter anxiety, cortisol, or blood pressure⁷.

Last updated October 17, 2026. Read how we make monographs.