Is kisspeptin an approved drug?

No. Kisspeptin (including kisspeptin-10 and kisspeptin-54) is supplied for research use only and is not approved by Health Canada, the FDA or the EMA for any human use. The information here describes published laboratory and clinical-research findings, not directions for use.

What is the difference between kisspeptin-10 and kisspeptin-54?

Kisspeptin-54 is the full 54-amino-acid peptide processed from the KISS1 gene product (originally called metastin). Kisspeptin-10 is its C-terminal decapeptide (YNWNSFGLRF-NH2), the minimal fragment that fully activates the KISS1R/GPR54 receptor, and is the form most commonly used in research. They differ in size, molecular weight and reported plasma half-life.

What did human studies report about kisspeptin?

In controlled clinical research, investigators reported that intravenous kisspeptin raised LH, FSH and testosterone and increased LH pulse frequency in men, and that it modulated limbic brain activity and connectivity related to sexual and emotional processing. These are research observations in small samples, not established medical benefits.

How is the chemical identity verified?

The structure, formula (C63H83N17O14), molar mass (1302.4 g/mol), CAS number (374675-21-5) and InChIKey (RITKWYDZSSQNJI-INXYWQKQSA-N) for kisspeptin-10 were confirmed against PubChem (CID 25240297).

Kisspeptin Dosage, Half-Life & Research

Kisspeptin is a neuropeptide encoded by the KISS1 gene and the endogenous ligand for the receptor KISS1R (formerly GPR54). The native peptide is processed to a 54-residue form (kisspeptin-54, originally named metastin) and shorter C-terminal fragments; the decapeptide kisspeptin-10 (the form most commonly supplied for research) retains full intrinsic activity at the receptor.¹ It is filed here under the neuro category because human imaging studies have reported effects on limbic brain activity and emotional processing,⁴⁵ but its best-characterised role is as the master upstream regulator of gonadotrophin (GnRH/LH/FSH) release.² Kisspeptin is not an approved drug and is sold for laboratory research use only. The human studies below used controlled intravenous or subcutaneous administration in clinical research settings; they are not usage directions.

Structure

Sequence & identity

TyrAsnTrpAsnSerPheGlyLeuArgPhe

YNWNSFGLRF-NH₂ · C₆₃H₈₃N₁₇O₁₄ · 1302.4 g/mol (kisspeptin-10)

Structure corresponds to kisspeptin-10 (metastin 45-54), PubChem CID 25240297, InChIKey RITKWYDZSSQNJI-INXYWQKQSA-N.¹ The full parent peptide kisspeptin-54 is a separate, larger entity (~5857 g/mol).

What the research shows

Mechanisms studied

Researchers report that kisspeptin binds KISS1R (GPR54), a G_q/11-coupled receptor expressed on hypothalamic GnRH neurons, triggering phospholipase-C signalling and GnRH release; this in turn drives pulsatile luteinising hormone (LH) and follicle-stimulating hormone (FSH) secretion from the pituitary.² The C-terminal decapeptide (kisspeptin-10) is described as the minimal sequence required for full receptor activation.¹ Beyond the hypothalamus, KISS1R is also expressed in limbic regions, and functional MRI studies in men reported that kisspeptin administration modulated activity and connectivity in the amygdala, hippocampus and related structures.⁴⁵ The native peptide is rapidly cleaved in plasma; one human pharmacokinetic study calculated the circulating half-life of kisspeptin-10 as roughly 3.8-4.1 minutes, with no significant difference between men and women, whereas the larger kisspeptin-54 has been reported with a substantially longer half-life of around 27.6 minutes.⁶

Reported in studies

Dosing in the research literature

The figures below summarise regimens as reported in published research — they are not recommendations or directions for use.

Source / model	Regimen reported	Notes
Dhillo et al., J Clin Endocrinol Metab 2005²	Kisspeptin-54, 90-min intravenous infusion; 4 pmol/kg/min was the lowest rate that maximally raised LH in healthy men	Research-setting administration in 6 male volunteers; reported dose-dependent rise in LH, FSH and testosterone vs saline. Not a usage direction.
George et al., J Clin Endocrinol Metab 2011³	Kisspeptin-10, intravenous bolus 0.01-3.0 µg/kg (peak LH response near 1 µg/kg) and continuous IV infusion (e.g. 1.5 µg/kg/h)	In healthy men, studies reported increased LH and increased LH pulse frequency. Clinical research dosing under monitoring, reported here for reference only.
Comninos et al., J Clin Invest 2017⁴	Kisspeptin-54 IV infusion at 1 nmol/kg/h for 75 min (steady-state for fMRI window)	Dose chosen to give stable circulating levels without an early testosterone rise; used to study brain effects, not as a dosing recommendation.
General	No approved human dose exists	Kisspeptin is research-use-only and not approved by Health Canada, FDA or EMA. Any figures above are study-reported research protocols, not directions for use.

Research use only. Peptigo products are sold to qualified researchers for laboratory use. This information summarises published research for reference and is not medical advice, a dosing recommendation, or directions for human or animal use.

Reported in studies

Effects observed in research

In controlled human research, investigators reported that intravenous kisspeptin (both the -54 and -10 forms) raised circulating LH, FSH and testosterone and increased LH pulse frequency in healthy men.²³ In a randomised, double-blind, placebo-controlled crossover study of 29 healthy heterosexual men, researchers observed that kisspeptin-54 enhanced limbic brain activation (amygdala, hippocampus, putamen, thalamus) in response to sexual and couple-bonding images and that it attenuated negative mood on the PANAS scale; these changes correlated with psychometric measures of reward and sexual aversion.⁴ A follow-up study reported that kisspeptin modulated resting-state brain connectivity (including amygdala-cingulate and hippocampus-cingulate links).⁵ These are mechanistic research findings in small samples; no therapeutic effect, mood benefit or sexual-function indication has been established, and kisspeptin is not approved for any use. Animal data and ongoing trials (e.g. for oocyte maturation) exist but do not constitute approval.

Honest assessment

Strength of evidence

Grade B

Grade B — limited human data. The reproductive-axis effects (LH/FSH/testosterone stimulation) are supported by several controlled human studies, largely from one principal research group at Imperial College London, plus extensive animal work.²³⁶ The neuro/emotional findings rest on a small number of fMRI studies (n=29 and similar), so the “nootropic / neuro” framing reflects early mechanistic signals, not established cognitive or mood outcomes.⁴⁵ There are no large phase 3 efficacy trials, no approved indication, and limited long-term safety data in humans; in a separate animal study, high-dose kisspeptin-54 administration acutely induced testicular degeneration in adult male rats, which is a relevant caution.⁷ Treat all of the above as research observations rather than evidence of benefit.

Handling

Reconstitution & storage

Reconstitute with bacteriostatic water for laboratory handling. Store lyophilised material frozen and reconstituted material refrigerated. Use Peptigo’s reconstitution calculator and storage cheat sheet for working figures.

References

Lee DK, Nguyen T, O’Neill GP, et al. Discovery of a receptor related to the galanin receptors (GPR54) and identification of KiSS-1 / metastin as its ligand. Chemical identity confirmed via PubChem CID 25240297 (kisspeptin-10, CAS 374675-21-5; C63H83N17O14; MW 1302.4; InChIKey RITKWYDZSSQNJI-INXYWQKQSA-N). https://pubchem.ncbi.nlm.nih.gov/compound/25240297
Dhillo WS, Chaudhri OB, Patterson M, et al. Kisspeptin-54 stimulates the hypothalamic-pituitary gonadal axis in human males. J Clin Endocrinol Metab. 2005;90(12):6609-6615. doi:10.1210/jc.2005-1468. PMID:16174713
George JT, Veldhuis JD, Roseweir AK, et al. Kisspeptin-10 is a potent stimulator of LH and increases pulse frequency in men. J Clin Endocrinol Metab. 2011;96(8):E1228-E1236. doi:10.1210/jc.2011-0089. PMID:21632807
Comninos AN, Wall MB, Demetriou L, et al. Kisspeptin modulates sexual and emotional brain processing in humans. J Clin Invest. 2017;127(2):709-719. doi:10.1172/JCI89519. PMID:28112678
Comninos AN, Demetriou L, Wall MB, et al. Modulations of human resting brain connectivity by kisspeptin enhance sexual and emotional functions. JCI Insight. 2018;3(20):e121958. doi:10.1172/jci.insight.121958. PMID:30333302
Jayasena CN, Nijher GMK, Comninos AN, et al. The effects of kisspeptin-10 on reproductive hormone release show sexual dimorphism in humans. J Clin Endocrinol Metab. 2011;96(12):E1963-E1972. doi:10.1210/jc.2011-1408. PMID:21976724 (source of kisspeptin-10 plasma half-life values; kisspeptin-54 half-life ~27.6 min reported in related Imperial College pharmacokinetic work)
Thompson EL, Murphy KG, Patterson M, et al. Kisspeptin-54 at high doses acutely induces testicular degeneration in adult male rats via central mechanisms. Br J Pharmacol. 2009;156(4):609-625. doi:10.1111/j.1476-5381.2008.00061.x. PMID:19226253

Written by the Peptigo Research Team · scientifically reviewed by Peter, Peptigo Research Team · Last reviewed June 2026. We cite primary literature and flag where evidence is limited. Our sourcing & RUO policy →