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PeptideHormone

Kisspeptin

The upstream gatekeeper that gates GnRH pulse generation.

EndogenousEstablishedInvestigational

The gate above the gate. Finding it rewrote where the reproductive axis was thought to begin.

Identity

Class
RF-amide peptide (KISS1 products, e.g. kisspeptin-54/10)
Source
Hypothalamus (KNDy and AVPV neurons)
Receptor
KISS1R (formerly GPR54)

Key properties

Evidence floorClinicalREF1CLIN1
Molecular weight
≈ 1,302.5 Da
REF
Half-life (native)
~4–30 min (by fragment)
CLIN
Model dosing

Approximate values for the native hormone; engineered analogs are often deliberately larger and far longer-acting. Each figure carries its own provenance tier, and the floor is the weakest of them - the Standard.

Mechanism

Kisspeptin neurons act upstream of GnRH, providing the excitatory drive that gates GnRH pulse generation. Their discovery reframed how the reproductive axis is switched on at puberty and tuned across the cycle.

Reference notes

  • Loss-of-function in KISS1R causes failure to enter puberty — the finding that revealed the pathway.
  • Kisspeptin is now seen as a key gatekeeper sitting above GnRH.
  • It integrates metabolic and steroid-feedback signals into the reproductive axis.

Regulatory status

United States · reviewed September 2026
InvestigationalKisspeptin is in registered human trials but not approved for any indication.
Basis
Kisspeptin-54 and -10 are in human trials for reproductive and metabolic indications; kisspeptin-10 also sits on the FDA 503A Category 2 list.

Status describes the molecule as a drug substance under US law and is an editorial reading of the public record — approvals, trial registrations, and the FDA 503A bulk-substances list. It is not legal advice and it changes; the review date above is the last time the table was checked. Other jurisdictions are noted only where they differ materially.

Common questions

What is Kisspeptin?
The upstream gatekeeper that gates GnRH pulse generation. Structurally it is RF-amide peptide (KISS1 products, e.g. kisspeptin-54/10).
How does Kisspeptin work?
Kisspeptin neurons act upstream of GnRH, providing the excitatory drive that gates GnRH pulse generation. Their discovery reframed how the reproductive axis is switched on at puberty and tuned across the cycle.
How strong is the evidence for Kisspeptin?
PeptideHormone grades Kisspeptin at the "Established" evidence tier — its mechanism and core effects are settled across the peer-reviewed literature. It is catalogued as an endogenous signal the body produces itself, and the tier is an editorial judgment about the public literature that can change as the science does.
What is the half-life of Kisspeptin?
The reported circulating half-life of Kisspeptin is ~4–30 min (by fragment).
Is Kisspeptin FDA-approved?
No — as of September 2026, Kisspeptin is in registered human trials but not approved for any indication. Kisspeptin-54 and -10 are in human trials for reproductive and metabolic indications; kisspeptin-10 also sits on the FDA 503A Category 2 list. Status is US-centric and can change; check the FDA record for the current position.

In the literature

Live registry counts · retrieved

Searched as Kisspeptin. Counts are search hits from the primary registries, not a curated set and not a grade – a measure of how much work exists on Kisspeptin, not how it turned out.

Selected literature

Curated peer-reviewed reviews, sourced from PubMed. Selected for relevance, not exhaustive — open any entry on PubMed for the full record and its primary citations.

  1. 1.The Role of Kisspeptin in the Control of the Hypothalamic-Pituitary-Gonadal Axis and Reproduction · Frontiers in endocrinology, 2022 · PMID 35837314
  2. 2.Pubertal development and regulation · The lancet. Diabetes & endocrinology, 2016 · PMID 26852256

External references

Kisspeptin in the public knowledge graph — the same entity resolved across the authoritative chemistry and protein databases.