Kisspeptin-10
Kisspeptin-10 (Metastin 45-54)
Investigational decapeptide hypothalamic-pituitary-gonadal axis activator. Acts ABOVE GnRH: kisspeptin neurons in the arcuate nucleus and AVPV are the master regulators of GnRH pulsatility. Bolus IV administration produces a rapid LH spike in healthy men and in subsets of hypogonadal patients. NOT approved for any indication anywhere in the world; available only via research-only / research peptide gray-market channels and used off-label in biohacker/PED communities for HPTA stimulation. Edinburgh group (Anderson, Skorupskaide, George) and Imperial College (Dhillo) have published most of the human translational data.
At a glance
- Half-life
- ~4 min Extremely short: ~4 minutes plasma t½ in human IV bolus studies; in vitro serum t½ ~55 seconds. Kisspeptin-54 (longer isoform) has t½ ~27.6 min and is preferred for sustained-effect protocols. KP-10's pharmacology is pulsatile-bolus by design: daily/weekly continuous schedules do not match its mechanism. Peak LH response at ~10 min post IV bolus.
- Routes
- SubQ · IV
- Vial sizes
- 1 mg · 5 mg
- Evidence base
- 3 studies 3 human
Mechanism
Endogenous KISS1 gene product cleaved to active 10-residue C-terminus. Binds GPR54 (KISS1R) on hypothalamic GnRH neurons, triggering GnRH release into the hypophyseal portal system. Downstream: ↑LH and ↑FSH from pituitary gonadotrophs → ↑testosterone (men) or ovarian stimulation (women). Plasma t½ ~4 minutes; sexually dimorphic response demonstrated: robust LH response in men, blunted in women. KP-10 acts upstream of GnRH and produces equivalent LH peak with much shorter duration than KP-54. KP-10 stimulated T and LH in T2DM hypogonadal men: proof-of-concept that hypothalamic kisspeptin tone is rescuable in metabolic hypogonadism. Action is permissive on the HPG axis: does NOT bypass it.
Dosing
Any amounts shown here are reported from published studies only. 3 of 3 catalogued studies involved human subjects. COMPOUND does not publish its own dosing guidance.
Published evidence
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Human RCT 2015
Kisspeptin-10 stimulation of gonadotrophin secretion in men
Direct IV comparison of KP-10/KP-54/GnRH gonadotrophin response in healthy men. KP-10 acts upstream of GnRH and produces equivalent LH peak with much shorter duration.
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Human RCT 2011
The effects of kisspeptin-10 on reproductive hormone release show sexual dimorphism in humans
Direct PK/PD of IV kisspeptin-10 vs kisspeptin-54 vs GnRH; established 4-min plasma t½ for KP-10 and demonstrated robust LH response in men, blunted in women.
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Human pilot 2013
Exploring the pathophysiology of hypogonadism in men with type 2 diabetes: kisspeptin-10 stimulates serum testosterone and LH secretion
KP-10 stimulated T and LH in T2DM hypogonadal men: proof-of-concept that hypothalamic kisspeptin tone is rescuable in metabolic hypogonadism.
Reported side effects
- Injection site reaction (SubQ)
- Common Mild · Mild local erythema; resolves within hours.
- Transient flush (high-dose IV)
- Occasional Mild · Reported in higher IV bolus protocols; transient.
- Headache
- Occasional Mild · Reported in research cohorts; usually mild and transient.
- Nausea
- Rare Mild · Uncommon.
- Paradoxical mood changes
- Rare Mild · Anecdotal: kisspeptin neurons project to limbic regions; mood/arousal effects reported in Dhillo group fMRI work.
- Tachyphylaxis with continuous infusion
- Very common Moderate · GPR54 desensitizes within hours of continuous exposure: the receptor was evolved for pulsatile signaling. Bolus dosing only; never infuse.
Interactions
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Triptorelin Redundant
Both drive downstream LH/FSH release via the GnRH→pituitary axis. Stacking provides no additional benefit and risks pituitary overstimulation.
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Cetrorelix Contraindicated
GnRH antagonists block the downstream effect of KP-10 at the pituitary: KP-10 releases GnRH, the antagonist blocks it.
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Opioids Caution
Chronic opioids suppress kisspeptin neurons (opioid-induced hypogonadism). KP-10 can rescue LH/T in this context: a published research finding, not clinical practice.
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Test Cypionate Caution
Exogenous testosterone provides negative feedback at the hypothalamus and pituitary, partially overriding KP-10 stimulation. LH spike is blunted on TRT.
Reconstitution and storage
Lyophilised peptide; reconstitute with bacteriostatic water. Typical research practice: 2mL BAC water per 5mg vial → 2.5mg/mL stock. Dose conversion: 100mcg = 0.04mL of 2.5mg/mL stock. NOT for human injection per supplier labeling.
Lyophilised: store at -20°C, stable >2 years. Reconstituted: refrigerate 2-8°C, use within 30 days; protect from freeze-thaw cycles.