Kisspeptin-10
Also known as: KISS1 decapeptide, Kisspeptin 112-121, Kisspeptin‑10, KP-10, KP‑10, Metastin (10-19), Metastin(10)
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Summary
Kisspeptin‑10 (KP‑10) is a ten‑amino‑acid fragment of the KiSS‑1 gene product that acts as a high‑affinity ligand for the G protein‑coupled receptor GPR54 (KISS1R). It is studied as a neuropeptide that drives gonadotropin‑releasing hormone (GnRH) secretion, influences hippocampal synaptic transmission, and modulates cancer‑related pathways and vascular biology. KP‑10 is not an approved drug; it is used experimentally via intranasal, intravenous or subcutaneous delivery to probe reproductive and other physiological mechanisms.
Mechanism of Action
KP‑10 binds GPR54, a Gq/11‑coupled receptor, activating phospholipase C, intracellular calcium release and downstream kinases such as ERK1/2, p38, CaMKII and tyrosine kinases. In hypothalamic neurons this cascade triggers GnRH release, increasing luteinising hormone (LH) pulses. In hippocampal dentate granule cells the same receptor‑mediated signaling enhances postsynaptic AMPA‑receptor‑mediated excitatory currents. In vascular cells KP‑10 induces endothelial inflammation, smooth‑muscle apoptosis and matrix‑metalloproteinase activation via MAPK pathways, contributing to atherogenesis.
What the Research Shows
Animal studies in non‑human primates show that KP‑10 stimulates GnRH release at pre‑pubertal and pubertal stages, with females displaying greater sensitivity. Human infusion studies report that continuous, receptor‑saturating KP‑10 raises LH pulse frequency without desensitisation over 22 hours, in both healthy and hypogonadal subjects. In rodent hippocampal slices, KP‑10 rapidly potentiates excitatory postsynaptic currents through GPR54‑dependent, calcium‑ and MAPK‑mediated mechanisms, suggesting a role in cognition and epilepsy. Cancer reviews describe KISS1‑derived peptides as metastasis suppressors, though their influence on autophagy and angiogenesis is complex. Vascular research indicates that KP‑10 acts as a vasoconstrictor and pro‑atherogenic factor, accelerating plaque development in Apoe‑/‑ mice, effects reversible by a GPR54 antagonist.
Reported Benefits
KP‑10 is a potent experimental tool for activating the gonadotropic axis, useful in studies of puberty, fertility and LH dynamics. Its ability to modulate hippocampal synaptic strength offers a model for investigating memory and seizure mechanisms. The peptide’s expression patterns and functional effects are being explored as potential biomarkers for cancer progression and as a target for anti‑metastatic strategies.
Limitations of the Evidence
KP‑10 is investigational and lacks regulatory approval for any therapeutic use. Human data are limited to short‑term infusion studies, providing no information on chronic dosing or disease treatment. Its pro‑atherogenic actions in animal models raise safety concerns, and its role in cancer appears dual‑faceted, with both suppressive and potentially promotive effects on tumor biology. Sex‑specific sensitivity and the need for continuous receptor saturation further complicate translation to clinical practice.
Safety Considerations
The abstracts report no acute adverse events in short‑term human infusions, but animal experiments demonstrate that chronic KP‑10 exposure can accelerate atherosclerotic plaque formation, increase vascular inflammation and promote endothelial dysfunction. These findings suggest potential cardiovascular risks, especially with prolonged administration. The peptide’s effects on neuronal excitability also warrant caution in contexts such as epilepsy. Comprehensive safety profiling in humans remains lacking.
How It Is Administered
KP‑10 has been administered experimentally by intranasal spray, intravenous injection or subcutaneous infusion. Formulations are typically aqueous peptide solutions delivered as bolus or continuous infusion in research settings. No commercial dosage forms or approved routes exist.
Routes of Administration
Goals & Uses
- Stimulation of LH and FSH secretionReproductive EndocrinologyHigh
- ContraceptionReproductiveLow
- Infertility treatmentReproductiveModerate
- Treatment of hypogonadotropic hypogonadismEndocrinologyModerate
- Treatment of hypothalamic amenorrheaReproductive EndocrinologyModerate
- Oocyte maturation trigger in ARTFertility / Assisted ReproductionModerate
- Tumor suppression / anti-metastatic effectsOncologyLow
- Assessment of HPG axis integrity (diagnostic)DiagnosticsModerate
- Metastasis suppressionOncologyModerate
Contraindications
- Hormone-sensitive malignanciesOncologyHigh
- Known hypersensitivity to kisspeptin or excipientsAllergy/ImmunologyHigh
- Ovarian hyperstimulation syndrome (OHSS) risk — caution in ARTReproductive EndocrinologyModerate
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Pregnancy (outside of intended ART trigger use)ReproductiveModerate
- Hormone‑sensitive cancersOncologyModerate
Adverse Effects
- Injection site reactionsLocalCommon
- HeadacheNeurologicCommonPain in the head or upper neck
- Ovarian hyperstimulation syndromeReproductive / EndocrineRare
- FlushingVascularUncommonWarmth and redness of the skin
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- Transient flushingVasomotorUncommon
Drug Interactions
- Sex steroid hormones (estrogen, testosterone, progesterone)Low
- Estrogen therapyLow
- Gonadotropins (FSH, LH, hCG)Moderate
- GnRH analogues (agonists/antagonists)Moderate
- GnRH analoguesModerate
Population Constraints
- PregnancyReproductive SafetyRelative
- Pediatric patientsAgeRelative
- Patients with history of hormone-sensitive cancerOncologyRelative
- Pediatric patients (prepubertal)AgeRelative
- Pregnant womenReproductiveAbsolute
- Renal or hepatic impairmentOrgan DysfunctionRelative
Regulatory Status
- European UnionInvestigationalEarly clinical studies ongoing.
- United StatesInvestigationalPhase I/II trials for infertility.
- United KingdomInvestigationalResearch use only.
Not approved for any therapeutic indication; used only in clinical research and early‑phase trials.
Evidence & Sources
- Journal ArticleModerateGarcia JP, et al.2019-01-01T00:00:00.000000Z
- Journal ArticleModerateArai AC2009-01-01T00:00:00.000000Z
- Journal ArticleModerateUlasov IV, et al.2019-01-01T00:00:00.000000Z
- Journal ArticleModerateTena-Sempere M2006-01-01T00:00:00.000000Z
- Journal ArticleModerateWatanabe T, Sato K2020-01-01T00:00:00.000000Z
- Journal ArticleModerateAnderson RA, Millar RP2022-01-01T00:00:00.000000Z
Frequently Asked Questions
Can kisspeptin‑10 be used to treat infertility?
Current evidence is limited to short‑term infusion studies showing increased LH pulse frequency; there are no clinical trials demonstrating efficacy or safety for infertility treatment, and the peptide is not approved for this indication.
Does KP‑10 have any approved medical uses?
No. KP‑10 is classified as an investigational compound used only in research; regulatory agencies have not granted approval for any therapeutic application.
What are the main safety concerns with KP‑10?
Animal data indicate that prolonged exposure can promote atherosclerotic plaque growth and vascular inflammation. Human data are insufficient to define cardiovascular or neurological risks, so caution is advised in any prolonged use.
How does KP‑10 affect the brain beyond reproduction?
In rodent hippocampal slices, KP‑10 enhances excitatory synaptic transmission via GPR54‑mediated activation of MAPK and calcium pathways, suggesting a role in synaptic plasticity and possibly in seizure susceptibility.
Is there evidence that KP‑10 can suppress cancer spread?
KISS1, the precursor of KP‑10, is recognized as a metastasis‑suppressor protein, but the specific contribution of the KP‑10 fragment to tumor suppression versus promotion remains unclear, with studies reporting both inhibitory and pro‑angiogenic effects.
What is Kisspeptin-10?
Kisspeptin‑10 (KP‑10) is a ten‑amino‑acid fragment of the KiSS‑1 gene product that acts as a high‑affinity ligand for the G protein‑coupled receptor GPR54 (KISS1R). It is studied as a neuropeptide that drives gonadotropin‑releasing hormone (GnRH) secretion, influences hippocampal synaptic transmission, and modulates cancer‑related pathways and vascular biology. KP‑10 is not an approved drug; it is used experimentally via intranasal, intravenous or subcutaneous delivery to probe reproductive and other physiological mechanisms.
What is Kisspeptin-10 used for?
Kisspeptin-10 is educationally associated with: Stimulation of LH and FSH secretion, Contraception, Infertility treatment, Treatment of hypogonadotropic hypogonadism, Treatment of hypothalamic amenorrhea, Oocyte maturation trigger in ART, Tumor suppression / anti-metastatic effects, Assessment of HPG axis integrity (diagnostic), Metastasis suppression. Educational only — not medical advice.
How is Kisspeptin-10 administered?
Recorded routes of administration: Intranasal, Intravenous, Subcutaneous.
What are the potential side effects of Kisspeptin-10?
Reported adverse effects include: Injection site reactions, Headache, Ovarian hyperstimulation syndrome, Flushing, Nausea, Transient flushing. This list is not exhaustive — consult a qualified clinician.
Who should avoid Kisspeptin-10?
Recorded contraindications: Hormone-sensitive malignancies, Known hypersensitivity to kisspeptin or excipients, Ovarian hyperstimulation syndrome (OHSS) risk — caution in ART, Pregnancy, Pregnancy (outside of intended ART trigger use), Hormone‑sensitive cancers. Consult a qualified clinician before use.