Kisspeptin-10

Summary

Kisspeptin-10 (KP-10) is the shortest biologically active fragment of the KISS1 gene product and acts as a potent endogenous regulator of the hypothalamic-pituitary-gonadal (HPG) axis. It is under investigation for conditions including hypothalamic amenorrhea, hypogonadotropic hypogonadism, infertility, and as a potential trigger for oocyte maturation in assisted reproduction. It is not approved for clinical use in any jurisdiction.

Mechanism of Action

Kisspeptin-10 is a 10-amino acid C-terminal fragment of kisspeptin-54 that binds to the kisspeptin receptor (KISS1R / GPR54) on hypothalamic GnRH neurons, potently stimulating pulsatile GnRH release, which in turn triggers LH and FSH secretion from the pituitary, driving gonadal steroidogenesis and gametogenesis.

Routes of Administration

Goals & Uses

• Stimulation of LH and FSH secretionReproductive EndocrinologyHigh
• 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

Contraindications

• Hormone-sensitive malignanciesOncologyHigh
• Known hypersensitivity to kisspeptin or excipientsAllergy/ImmunologyHigh
• Ovarian hyperstimulation syndrome (OHSS) risk — caution in ARTReproductive EndocrinologyModerate
• Pregnancy (outside of intended ART trigger use)ReproductiveModerate

Adverse Effects

• Injection site reactionsLocalCommon
• HeadacheNeurologicUncommonPain in the head or upper neck
• Ovarian hyperstimulation syndromeReproductive / EndocrineRare
• NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit
• Transient flushingVasomotorUncommon

Drug Interactions

• Sex steroid hormones (estrogen, testosterone, progesterone)Low
• Gonadotropins (FSH, LH, hCG)Moderate
• GnRH analogues (agonists/antagonists)Moderate

Population Constraints

• PregnancyReproductive SafetyRelative
• Patients with history of hormone-sensitive cancerOncologyRelative
• Pediatric patients (prepubertal)AgeRelative
• Renal or hepatic impairmentOrgan DysfunctionRelative

Regulatory Status

• European UnionInvestigationalInvestigated under EMA clinical trial frameworks; no marketing authorization granted.
• United StatesInvestigationalUsed under IND in Phase I/II clinical trials; not FDA-approved for any indication.
• United KingdomInvestigationalStudied at UK academic centers (e.g., Imperial College London) under MHRA-regulated trials; not licensed.

Not approved by the FDA, EMA, or MHRA for any indication. Used in Phase I/II clinical trials for reproductive disorders and ART (assisted reproductive technology). Investigational use only.

Evidence & Sources

No sources recorded yet.