Kisspeptin-10

The 10-amino-acid active tail of kisspeptin, a natural brain hormone from the KISS1 gene. The gene was found in 1996 as a cancer metastasis suppressor ('metastin'); in 2003, receptor mutations were shown to block puberty.

Kisspeptin acts on the KISS1R receptor on GnRH neurons in the hypothalamus, triggering GnRH release, which drives the pituitary to release LH and FSH. Because it works upstream of GnRH, it depends on an intact GnRH neuron and pituitary.

In small studies of healthy men, IV kisspeptin-10 roughly tripled LH within 30 minutes, and a 22.5-hour infusion modestly raised testosterone. Women early in their cycle showed no hormone response by any route; women near ovulation did respond. Most promising fertility and sexual-desire research used kisspeptin-54, including IVF egg-maturation trials and a brain-imaging study of sexual and bonding responses. Repeated-use outcomes, long-term safety and a measured human half-life for kisspeptin-10 are lacking.

No adverse events were reported in the kisspeptin-10 studies, and vital signs and labs stayed stable. FDA cites possible immunogenicity, peptide impurities and little safety data. Sustained exposure may blunt the hormone axis, as shown with kisspeptin-54.

Not approved in the US or elsewhere. FDA's Pharmacy Compounding Advisory Committee voted against adding it to the 503A bulks list in October 2024. FDA has listed it in 503A Category 2 (significant safety risk) since September 2023, and it remained there in 2026, so it is not compoundable. WADA prohibits kisspeptin and its agonists at all times for males under S2.2.1. Status as of October 2026.