Kisspeptin-54
A 54-amino-acid product of the KISS1 gene that stimulates hypothalamic GnRH neurons, making it a master regulator of reproductive hormone release. Investigational only: studied for triggering egg maturation in IVF and probing hypothalamic reproductive disorders, with no marketed product.
01 Overview
Kisspeptin-54 acts upstream of GnRH, binding the KISS1R (GPR54) receptor on GnRH neurons to drive pulsatile LH and FSH secretion. Loss-of-function mutations in this system cause congenital hypogonadotropic hypogonadism, which established kisspeptin's central role in puberty and fertility.
Clinical research has tested kisspeptin-54 as a more physiological trigger for oocyte maturation in IVF — potentially lowering ovarian hyperstimulation risk compared with hCG — and as a diagnostic probe of hypothalamic function. The human data are early-phase and limited, so it remains an investigational peptide rather than an approved therapy.
02 Mechanism
Agonist at the kisspeptin receptor (KISS1R/GPR54) on hypothalamic GnRH neurons, stimulating GnRH release and downstream LH/FSH secretion.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| IVF oocyte-maturation trigger (research) | 6.4–12.8 mcg | SubQ | Single research bolus (µg/kg-based); investigational only. |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| LH/FSH surgeTriggers an endogenous LH surge, tested to mature oocytes in IVF cycles. | Physiological gonadotropin rise | Clinical | |
| Probe of hypothalamic functionUsed experimentally to assess GnRH-neuron responsiveness in reproductive disorders. | Diagnostic response | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Mild transient reactionsGenerally well tolerated in short studies; occasional mild injection-related effects. | Mild | Unknown | Observational | |
| Limited long-term safety dataHuman exposure is confined to short research studies; chronic effects are uncharacterised. | Moderate | Unknown | Unconfirmed |