Compounds / Kisspeptin

Kisspeptin

Also known as: Kisspeptin-10 (KP-10); Kisspeptin-54 (KP-54, metastin); KISS1-derived peptide; KP-13

INVESTIGATIONAL Tier 2 – Clinical Hormonal and Reproductive

Primary research focus: Reproductive endocrinology research (upstream stimulation of the HPG axis; fertility and IVF)

Last updated July 2026 · Reviewed against FDA labeling and published research.

What is Kisspeptin?

Kisspeptin is a family of peptides encoded by the KISS1 gene that act as the furthest-upstream trigger of the reproductive (hypothalamic-pituitary-gonadal) axis. The full-length circulating form is kisspeptin-54 (KP-54, also called metastin); the minimal active fragment is kisspeptin-10 (KP-10), the C-terminal decapeptide. Kisspeptin is investigational, with a substantial human clinical-trial record in fertility (especially KP-54), but it is not FDA-approved for any indication.

How it works

Kisspeptin binds the KISS1R receptor (also called GPR54) on gonadotropin-releasing-hormone (GnRH) neurons in the hypothalamus, triggering Gq-coupled signaling (calcium mobilization, ERK1/2 and p38 MAPK). This drives GnRH release into the pituitary portal system, stimulating luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion, which in turn drive gonadal steroid production and gametogenesis. Because it acts above GnRH, it recruits the body's own pulse generator; it can produce an LH surge suitable for triggering egg maturation with a lower ovarian-hyperstimulation risk than traditional triggers.

How it’s supplied

Not FDA-approved or commercially available as a medicine. In clinical trials it is given by subcutaneous injection or intravenous infusion. Research-grade kisspeptin-10 is sold as a lyophilized peptide for reconstitution; such products are not FDA-reviewed for potency or sterility, and legitimate clinical access is essentially limited to research protocols.

Dosage Chart

RouteSubcutaneous
For reference only, compiled from FDA labeling, clinical trials, and established protocols. Not medical advice or a dosing recommendation. Confirm against current prescribing information and consult a qualified healthcare professional.
Vial size
BAC water

Units shown are for a U-100 insulin syringe (100 units = 1 mL), calculated from the vial size and BAC water you select. Always confirm against your prescription and your syringe markings.

PhaseDoseFrequencyNotes
Weeks 1-2 100mcg 1x Daily
Weeks 3-12 200mcg 1x Daily
Special considerations
  • Rotate injection sites to reduce irritation and lipohypertrophy
  • Not for use during pregnancy or breastfeeding
  • Do not exceed the recommended dose to try to speed results

Potential Benefits and Side Effects

Effects reported in published research. Not a promise of results, and not medical advice.

Reported benefits
  • Reported in human clinical trials (especially kisspeptin-54) and research; not an approved therapy.
  • Stimulates the body's own GnRH, LH, and FSH release from the top of the axis.
  • Triggers oocyte maturation in IVF with a reduced risk of ovarian hyperstimulation syndrome.
  • Can restore GnRH pulsatility in hypothalamic amenorrhea and stimulate the axis in hypothalamic-origin hypogonadism.
  • Studied for roles in sexual desire and reproductive-brain function.
Reported side effects
  • In trials kisspeptin has generally been well tolerated for acute and short-term use.
  • Effects relate mainly to reproductive-hormone changes.
  • Longer-term and repeated-dosing safety is not fully characterized.
  • Practical limitation: very short half-life, particularly for kisspeptin-10.

Warnings and contraindications

Important safety information. This is not exhaustive — read the full prescribing information and consult your prescriber or pharmacist.

Warnings
  • No FDA-approved labeling exists; the following reflect the compound's status and trial experience, not an FDA label.
  • Kisspeptin is investigational; while acute and short-term human use has looked well tolerated in trials, long-term safety is not established.
  • Effects on the reproductive axis mean it can alter hormone levels, ovulation, and fertility; it should not be used casually.
  • Kisspeptin-10 has a very short half-life, limiting practical use outside a clinical setting.
  • Research-grade material varies in identity and purity.
  • Use in pregnancy or with hormone-sensitive conditions should be guided by a specialist.
Contraindications
  • Not established as a drug; no FDA labeling. Precautionary considerations include hormone-sensitive tumors, pregnancy, and known hypersensitivity.

Reconstitution Steps

How to prepare the lyophilized vial. Confirm specifics with your pharmacist or prescriber.

  1. Confirm the amount of peptide in the vial and the volume of diluent you intend to use before starting.
  2. Wash your hands and gather supplies: the lyophilized vial, the diluent (typically bacteriostatic water), an alcohol swab, and a sterile syringe.
  3. Let the vial and diluent reach room temperature if they were refrigerated or frozen.
  4. Wipe the rubber stopper of both the peptide vial and the diluent vial with a fresh alcohol swab and let them air dry.
  5. Draw the intended diluent volume into the syringe.
  6. Insert the needle into the vial and slowly release the diluent down the inside wall rather than directly onto the powder, to avoid foaming.
  7. Do not shake. Gently swirl or roll the vial until fully dissolved.
  8. Inspect the solution: it should be clear and colorless with no visible particles. Do not use if cloudy or containing particles.
  9. Note the resulting concentration (amount divided by diluent volume) so it matches the reconstitution calculator on this page.
  10. Label the vial with the reconstitution date and store as directed under reconstituted storage.

US regulatory status

Classifications are public record but can change. For reference only, not legal advice.

DEA scheduleNot a controlled substance
Development stagePhase 2
503A compoundingNot eligible
503B compoundingNot eligible

Development: Kisspeptins were identified in 2001 as the natural ligands of GPR54 (KISS1R); loss-of-function mutations in this pathway cause absent puberty and hypogonadotropic hypogonadism, genetically validating its central reproductive role. A substantial human clinical program, led largely by Waljit Dhillo's group at Imperial College London, has studied kisspeptin-54 as an egg-maturation trigger in IVF, showing effective oocyte maturation with a reduced risk of ovarian hyperstimulation syndrome (including a Phase 2 randomized controlled trial), as well as studies in hypothalamic amenorrhea, hypogonadotropic hypogonadism, and sexual-desire research. It is not FDA-approved, and no Phase 3 program has been completed. On October 29, 2024, the FDA Pharmacy Compounding Advisory Committee voted to exclude kisspeptin-10 from the 503A bulks list.

Notes: Kisspeptin is investigational and not FDA-approved for any indication. On October 29, 2024, the FDA Pharmacy Compounding Advisory Committee voted (11-0) to exclude kisspeptin-10 from the 503A bulk drug substances list, so it is not eligible for 503A (or 503B) compounding; legitimate clinical access is essentially limited to research trials. It is not explicitly listed on the WADA Prohibited List. It is not a controlled substance. (Status current as of mid-2026.)

International status

UKNot approved (MHRA); used in UK academic clinical research
EUNot approved (EMA)
AustraliaNot approved (TGA)
CanadaNot approved (Health Canada)

Pharmacokinetics

Molecular weightKisspeptin-10 (the C-terminal decapeptide) is approximately 1,302 Da; kisspeptin-54 (metastin) is approximately 5,857 Da. Both share the biologically essential RF-amide C-terminus.
Half-lifeShort and fragment-dependent: kisspeptin-10 is approximately 4 minutes after intravenous dosing, while kisspeptin-54 is approximately 28 minutes after subcutaneous dosing; downstream LH and FSH effects can last many hours.
Time to peakLH and FSH rise within minutes to hours after dosing, depending on the fragment and route.
ClearanceRapid enzymatic degradation; the short half-life is central to its pharmacology, and kisspeptin-54 is longer-acting than kisspeptin-10.
SequenceKisspeptin-10 is Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2 (YNWNSFGLRF-NH2), the minimal fragment that fully activates KISS1R. Kisspeptin-54 is the 54-amino-acid full-length form (metastin). Both derive from the KISS1 gene product and end in an RF-amide motif.

Storage and handling

TemperatureResearch-grade lyophilized powder is typically stored frozen at -20 degrees C long term and refrigerated at 2 to 8 degrees C short term. Not a clinically stored, FDA-approved product.
Light sensitiveProtect from light and moisture; keep the vial sealed.
Shelf lifeLyophilized powder is generally stable for months when frozen; follow the supplier certificate of analysis. There is no FDA-established drug shelf life.
Reconstituted storageAfter reconstitution, solutions are generally refrigerated at 2 to 8 degrees C and used within the supplier-indicated period, with freeze-thaw minimized. No FDA-established in-use dating.

Important Notes

Practical considerations for consistency and safety.

  • Kisspeptin sits at the very top of the reproductive hormone cascade, above GnRH.
  • Kisspeptin-54 is the form with the strongest human trial data (IVF triggering); kisspeptin-10 is shorter-acting and more common in research supply.
  • The FDA advisory committee voted to exclude kisspeptin-10 from the 503A compounding list in October 2024.
  • Its most promising clinical signal is triggering egg maturation with a lower OHSS risk than traditional triggers.
  • Research-grade material varies in identity and purity.

Lifestyle Factors

  • Studied within clinical fertility protocols under specialist supervision.
  • Human lifestyle interactions beyond trial settings are not well characterized.

Related compounds

Important disclaimer

This page is an educational reference, not medical advice, a diagnosis, or a treatment recommendation, and not a substitute for your prescriber or pharmacist. Approval and regulatory status varies by compound and can change. Always confirm against current prescribing information and consult a qualified healthcare professional before making any decision about a medication.