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Kisspeptin is a neuropeptide involved in regulating the hypothalamic-pituitary-gonadal axis and reproductive hormone signaling. Human research includes Kisspeptin-54 and, to a lesser extent, Kisspeptin-10; evidence for long-term outcomes remains limited. Kisspeptin is investigational and not FDA-approved.
For laboratory research only. Not for human or animal consumption.
VIP Peptides · Research Compound
Kisspeptin, also known as metastin, is a family of neuropeptides encoded
by the KISS1 gene. Kisspeptin-54 is the longer form used in many human
studies; Kisspeptin-10 is a shorter C-terminal fragment commonly sold
as a research peptide.
Product Information
Kisspeptin acts upstream in the hypothalamic-pituitary-gonadal
(HPG) axis. It binds to the KISS1R receptor on hypothalamic GnRH
neurons and can trigger gonadotropin-releasing hormone (GnRH)
release. GnRH then signals the pituitary to release luteinizing
hormone (LH) and follicle-stimulating hormone (FSH), which
influence gonadal sex-hormone production.
Genetic findings support the pathway’s role in puberty and
reproductive function: loss-of-function KISS1/KISS1R mutations
are associated with hypogonadotropic hypogonadism, while certain
activating mutations are associated with precocious puberty.
| Compound | Kisspeptin / metastin |
|---|---|
| Encoded by | KISS1 gene |
| Research forms | Kisspeptin-54 and Kisspeptin-10 |
| Receptor | KISS1R / GPR54 |
| Primary pathway | Hypothalamic-pituitary-gonadal axis |
| Regulatory status | Not FDA-approved for any indication |
Evidence & Research
Human studies, primarily involving Kisspeptin-54 and some
Kisspeptin-10, have reported acute increases in LH, FSH and
downstream sex hormones in healthy men and in some women with
hypothalamic amenorrhea.
Kisspeptin has been studied as a trigger for oocyte maturation
in IVF. Research has explored whether this approach may carry
a lower risk of ovarian hyperstimulation syndrome (OHSS) than
traditional hCG triggers.
Placebo-controlled studies in men and women with hypoactive
sexual desire disorder (HSDD) have examined brain activity in
sexual-processing networks. A study in men also reported
increased penile rigidity in response to sexual stimuli.
These findings do not establish a treatment for HSDD.
Kisspeptin is also being studied for its potential diagnostic
role in assessing hypothalamic-pituitary-gonadal axis function.
This remains a research application.
Evidence Limitations
Continuous or frequent exposure may lead to tachyphylaxis, meaning
the LH/FSH response can diminish over time. Research has therefore
examined intermittent or pulsatile approaches.
Long-term evidence for sustained testosterone restoration, fertility
outcomes or lasting changes in sexual function remains limited.
Results from Kisspeptin-54 studies should not automatically be
treated as evidence for a Kisspeptin-10 research vial.
Safety & Regulatory Status
Short-term human studies generally describe kisspeptin as tolerated,
with possible mild effects such as injection-site reactions, flushing
or transient headache. Serious adverse events have been rare in
published acute studies, but this does not establish long-term safety.
Repeated exposure may reduce the hormonal response through
tachyphylaxis. The long-term safety database for chronic use is limited.
Kisspeptin is not FDA-approved for any indication. In 2024, the FDA’s
Pharmacy Compounding Advisory Committee voted against recommending
Kisspeptin-10 for inclusion on the 503A Bulk Drug Substances List,
citing insufficient safety and efficacy evidence. Kisspeptin and its
agonist analogues are prohibited under the WADA Prohibited List.
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