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Machine-assisted translation — the German original version is authoritative.
Pure research compound
Kisspeptin
Kisspeptin-54 · Kisspeptin-10 · KP-54 · KP-10 · Metastin · KISS1-Genprodukt · KiSS-1
Kisspeptin is an endogenous neuropeptide encoded by the KISS1 gene that occurs in several lengths (including kisspeptin-54 and the active C-terminal fragment kisspeptin-10). It is regarded as a central pacemaker of the reproductive axis: via its receptor it stimulates the release of GnRH in the hypothalamus and, downstream, the pituitary hormones LH and FSH. In clinical reproductive research, exogenous kisspeptin is investigated under study conditions — for example to trigger egg maturation in in vitro fertilization or in cases of menstrual cycle disorders. The human evidence comes mostly from smaller, controlled studies; specifically for PCOS it remains preliminary (proof-of-concept) and incomplete in its efficacy so far. A conclusive picture of long-term safety and benefit outside narrowly defined questions is not available. Kisspeptin is not approved as a medicinal product anywhere.
Regulatory status
In clinical trials only · not approved
Investigational compound of reproductive research — studied in clinical trials but not approved as a medicinal product.
Drug class
Neuropeptide / reproductive neurohormone (KISS1R/GPR54 agonist); investigational compound
Half-life (informative)
Short and length-dependent: for kisspeptin-10 a plasma half-life of about 4 minutes has been reported in humans, and for the longer kisspeptin-54 about 28 minutes (Jayasena et al., Human Reproduction 2015).
Studied in the literature
In human studies investigated mostly systemically — as an intravenous bolus or infusion, partly subcutaneously; purely descriptive, not an application guide.
Mechanism of action
Kisspeptin binds to the receptor KISS1R (formerly GPR54) on GnRH-producing neurons in the hypothalamus. Activation of this receptor triggers the release of GnRH (gonadotropin-releasing hormone), which in turn stimulates the pituitary to secrete the gonadotropins LH (luteinizing hormone) and FSH (follicle-stimulating hormone). Kisspeptin thus acts as an upstream amplifier or switch of the hypothalamic-pituitary-gonadal axis and is involved in controlling the onset of puberty, the menstrual cycle, and the preovulatory LH surge. The C-terminal decapeptide (kisspeptin-10) carries the receptor-active core sequence.
Because of its rapid inactivation, kisspeptin was used in studies as a bolus or continuous infusion depending on the research question. Longer analogues (e.g. the developmental compound TAK-448/MVT-602 class) have been investigated in order to extend the duration of action. All pharmacokinetic data come from the controlled study context.
Research history
The KISS1 gene was discovered in 1996 in Hershey (Pennsylvania), initially as a metastasis suppressor in melanoma cells; its 54-amino-acid product was therefore first named “metastin”. In 2001 the orphan receptor GPR54 (today KISS1R) was identified as the binding site for KISS1 peptides. The breakthrough for reproductive research came in 2003 from two independent research groups (including those around Seminara and de Roux), who showed that loss-of-function mutations in the GPR54 gene in humans are associated with absent puberty and hypogonadotropic hypogonadism. Since then, exogenous kisspeptin has been investigated in clinical studies as a tool and a possible therapeutic target in reproductive medicine.
Regulatory status by region
Not an approved medicinal product. Use in humans is envisaged only within the framework of authorized clinical trials.
Not an FDA-approved medicinal product. Kisspeptin and analogues have been and are being investigated in FDA-regulated studies; there is no marketing authorization.
No country has approved kisspeptin as a regular medicinal product. Availability in humans is limited to the study setting.
Research areas
- Triggering egg maturation (ovulation trigger) in assisted reproduction / IVF
- Diagnosis and treatment of menstrual cycle disorders (e.g. hypothalamic amenorrhea); in PCOS so far only an early proof-of-concept with incomplete efficacy, not an established treatment
- Evaluation of pubertal disorders and hypogonadotropic hypogonadism
- Investigation of sexual function and sexual brain processing (e.g. in reduced sexual desire)
- Basic research on the control of the hypothalamic-pituitary-gonadal axis
Documented effects (from the literature)
- Rise in the pituitary hormones LH and FSH after administration — the central effect, reproduced in several human studies.
- Documented triggering of final egg maturation (ovulation trigger) in a controlled IVF study.
- In a randomized study in men with reduced sexual desire, altered activity in sexual-processing brain areas and increased penile tumescence compared with placebo.
- In the previous, mostly short studies kisspeptin was largely well tolerated; the reported measures concerned above all the hormonal response.
Safety concerns & caution
- The human evidence comes from smaller, controlled short-term studies; data on long-term safety and on repeated use are largely lacking.
- Kisspeptin intervenes directly in the reproductive and hormonal axis — effects on the menstrual cycle, hormone balance, and fertility cannot be assessed outside narrowly defined study questions.
- Effect and tolerability depend strongly on peptide length (kisspeptin-10 vs. -54), dose, and route of administration; uncontrolled use cannot be derived from study data.
- Use in pregnancy or in people with existing endocrine disorders is not established and belongs, if at all, within the study setting.
Risks of gray-market purchase
- Kisspeptin vials sold as a “research peptide” are not subject to any pharmaceutical control — identity, purity, actual peptide content, and sterility are unverified.
- Risk of confusion and mislabeling: different lengths (KP-10, KP-54) and analogues are traded under similar names, with very different properties.
- Intervening in the hormonal axis without medical diagnosis and monitoring can mask or aggravate existing disorders.
- Gray-market products may be contaminated or contain endotoxins; their origin and manufacturing conditions are usually not traceable.
Frequently asked questions
What does kisspeptin do in the body?
It is an endogenous neuropeptide and acts as an upstream switch of the reproductive axis: via its receptor it stimulates the release of GnRH in the hypothalamus, which prompts the pituitary to secrete LH and FSH. These control the ovaries and testes — kisspeptin is involved, among other things, in puberty, the menstrual cycle, and ovulation.
Is kisspeptin approved as a medication?
No. Kisspeptin is not approved as a medicinal product anywhere. It is being investigated in clinical studies — for example as an ovulation trigger in in vitro fertilization or in menstrual cycle disorders — and is therefore regarded as an investigational compound, not an approved consumer or therapeutic product.
How solid is the body of evidence?
There are robust but mostly small and short controlled human studies, above all on the hormonal response (LH/FSH rise) and on individual applications such as egg maturation. Statements on long-term safety, repeated use, or benefit outside these narrowly defined questions cannot be derived from them — there are clear knowledge gaps here.
Sources
Primary and reference sources for your own reading.
- PubMedYang L, Dhillo WS — Kisspeptin as a therapeutic target in reproduction (Expert Opin Ther Targets, 2016)
- PubMedJayasena CN et al. — Direct comparison of intravenous kisspeptin-10, kisspeptin-54 and GnRH on gonadotrophin secretion in healthy men (Human Reproduction, 2015)
- PubMedRomero-Ruiz A et al. — Kisspeptin treatment induces gonadotropic responses and rescues ovulation in models and women with PCOS (Human Reproduction, 2019)
- PubMedMills EG et al. — Effects of Kisspeptin on Sexual Brain Processing and Penile Tumescence in Men With HSDD: A Randomized Clinical Trial (JAMA Network Open, 2023)
Related substances
Mentioned in these guide articles
Unfamiliar terms? Look them up in the glossary or read the fundamentals.
This profile is for information and education only. It is not medical advice and deliberately contains no dosing or usage details. Decisions about use belong in a doctor’s hands.