Kisspeptin-54
Also known as Metastin · KP-54 · Kisspeptin (54 amino acid form)
Kisspeptin-54 (metastin) is the 54-amino-acid form of the hypothalamic peptide kisspeptin, which acts on the KISS1R (GPR54) receptor to drive GnRH and downstream LH and FSH release. Academic human studies have given it intravenously, subcutaneously and intranasally to healthy volunteers, women with hypothalamic amenorrhoea and women undergoing IVF, where it was used to trigger oocyte maturation. It is not approved for any use and is prohibited in sport; this entry summarizes the published studies for research reference only.
- US status
- Not approved — research use only
- Evidence
- Grade B
- Half-life
- Plasma half-life of 27.6 plus or minus 1.1 minutes after intravenous infusion in healthy men 1
- Class
- Endogenous 54-amino-acid peptide agonist of the kisspeptin receptor KISS1R (GPR54); hypothalamic regulator of GnRH secretion
More
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Key takeaways
- Kisspeptin-54 is the 54-amino-acid form of kisspeptin; it activates KISS1R and stimulates LH, FSH and testosterone release in men 1.
- In women, its LH-stimulating effect was greatest in the preovulatory phase and least in the follicular phase of the menstrual cycle 2.
- In women with hypothalamic amenorrhoea, repeated administration over 2 weeks led to marked desensitization of the gonadotropin response 3.
- In phase 2 IVF studies, kisspeptin-54 used as an oocyte-maturation trigger was followed by egg maturation in most women, and no moderate, severe or critical OHSS occurred among 60 high-risk women 5,6.
- It is not approved anywhere and is prohibited at all times by WADA as a testosterone-stimulating peptide in males 9,12.
Development stage
Where Kisspeptin-54 sits between laboratory work and regulatory approval.
- PreclinicalAnimal and cell work
- Phase 1First human safety studies
- Phase 2Early efficacy signal
- Phase 3 (current)Confirmatory trials
- ApprovedCleared by a regulator
Stage comes from the regulatory record and ClinicalTrials.gov studies naming the compound (for compounds approved nowhere, only completed trials or trials with posted results count) (checked 2026-10-24). A registered trial is not a result.
Mechanism of action
Kisspeptin is the endogenous ligand of the G protein-coupled receptor KISS1R (GPR54); inactivating mutations of this pathway are associated with failure of reproductive function and infertility 1,5.
Neuroendocrine action
Kisspeptin acts at the hypothalamus to release an endogenous pool of GnRH, which in turn drives pituitary LH and FSH secretion 7. In humans, raising circulating kisspeptin-54 increased LH, FSH and testosterone in men 1, and produced an LH surge of roughly 12 to 14 hours in women undergoing IVF 7.
Desensitization
Continuous or repeated exposure produced tachyphylaxis of the gonadotropin response in women with hypothalamic amenorrhoea, while responsiveness to GnRH was preserved 3.
Molecular structure
PubChem CID 71306396 ↗
2D depiction generated from the PubChem record. Depictions are schematic and do not show salt form, counter-ions or conformation.
- Formula
- C258H401N79O78
- Molecular weight
- 5857 g/mol
- CAS
- 388138-21-4
- InChIKey
- KAHDONZOCXSKII-NJVVDGNHSA-N
Kisspeptin-54 draw calculator
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| Water | mg/mL | Draw |
|---|---|---|
| 0.5 mL | 20 | — |
| 1 mL | 10 | — |
| 1.5 mL | 6.667 | — |
| 2 mL | 5 | — |
| 2.5 mL | 4 | — |
| 3 mL | 3.333 | — |
| 5 mL | 2 | — |
Published adverse-event data
Reported in the cited trials or product labels. Frequencies apply to the stated population and do not transfer to other settings.
- Moderate ovarian hyperstimulation syndrome1 of 31 (3.2%) single trigger vs 0 of 31 with additional administration
- Moderate, severe or critical OHSS0 of 60
- Any side effect or adverse event (intranasal)None encountered
Emerging safety signals
- Repeated administration in women with hypothalamic amenorrhoea caused desensitization (tachyphylaxis) of LH and FSH responses within 2 weeks (small randomized evidence) 3. 3 (2009)
- In healthy women given repeated follicular-phase kisspeptin-54, cycles persisted but were shorter, with earlier LH peaks and earlier luteal phase onset (small crossover evidence) 4. 4 (2013)
- FDA placed the related fragment kisspeptin-10 in 503A category 2 (bulk drug substances that raise significant safety risks); kisspeptin-54 is not named 10. 10 (2026)
What is not known: Kisspeptin-54 has no regulatory label, and human studies have been small, short and mostly from a single academic centre 5,6,7. Long-term safety, effects of chronic exposure beyond a few weeks, and direct comparison with established IVF triggers were not established in the sources reviewed 7. Adverse-event reporting in the abstracts is limited.
Background viewing
We haven't found a clinician video focused on Kisspeptin-54 yet. Meanwhile, this widely watched talk covers the science of aging in general. It does not discuss Kisspeptin-54.
These creators are not affiliated with Amiravo and do not endorse Amiravo or any product linked on this site. Nothing here is medical advice. Video views counted on YouTube as of Oct 24, 2026.
Regulatory status
- Status
- Not approved by the FDA or, in the sources reviewed, any other regulator. A Drugs@FDA / openFDA query for kisspeptin returned no application record 9. Kisspeptin-54 is not named in FDA's May 14, 2026 503A bulk substances list, where kisspeptin-10 is in category 2 (significant safety risks) 10. Human studies have been academic, investigator-led trials 5,7.
- United States (FDA)
- Not approved. A Drugs@FDA / openFDA query for kisspeptin returns no matching applications 9. Kisspeptin-54 is not named in FDA's May 14, 2026 503A bulk substances list; kisspeptin-10 is listed in category 2 10.
- Sport (WADA)
- Prohibited at all times. Section S2.2.1, testosterone-stimulating peptides in males, names kisspeptin and its agonist analogues 12.
Status varies by country and changes over time. How we describe regulatory status.
Quality and testing notes
Kisspeptin-54 is a 54-residue C-terminally amidated peptide with the PubChem sequence GTSLSPPPESSGSRQQPGLSAPHSRQIPAPQGAVLVQREKDLPNYNWNSFGLRF-NH2 and formula C258H401N79O78 [11]. A certificate of analysis would typically show HPLC purity with chromatogram, intact mass by high-resolution mass spectrometry against that sequence (confirming C-terminal amidation), net peptide content, counter-ion and residual solvent content, and endotoxin testing. Because kisspeptin-10 shares the C-terminal decapeptide, identity testing should distinguish the full-length 54-mer from shorter fragments.
How purity testing works · Reading a certificate of analysis
Check a Kisspeptin-54 certificate of analysis against its expected mass (5,857 Da)Storage and handling
No approved-product storage instructions exist. In one study a nasal-spray formulation was stable for up to 60 days at 4 degrees C [8]; otherwise handling should follow the supplier's documentation.
Frequently asked questions
How does kisspeptin-54 differ from kisspeptin-10?
Is kisspeptin-54 FDA-approved?
What happens to hormones after kisspeptin-54?
Has it been used in IVF research?
Does the response wear off with repeated use?
What is its half-life?
Is it banned in sport?
Latest indexed research
No new studies were filed in the last sweep.
Search all studies on Kisspeptin-54 (PubMed, Europe PMC, ClinicalTrials.gov)Listed by publication type from the index record. Inclusion is not an endorsement; open the source to read the findings.
Revision history
Meaningful changes to this entry, with dates and sources. Last reviewed Oct 23, 2026. Typo and layout fixes are not listed.
No recorded changes since the change log began on Oct 23, 2026.
Last reviewed October 23, 2026 by the Amiravo editorial team.
Need the math?
Laboratory arithmetic with every formula shown.
For research use only. Not for human or veterinary use. Not a drug, food, or dietary supplement. This page is educational and is not medical advice.
Unbranded reference image. Amiravo does not produce, supply or sell this compound.
Specifications
- Molecular formula
- C258H401N79O78
- Molecular weight
- 5,857 g/mol
- CAS number
- 388138-21-4
- PubChem CID
- 71306396
- FDA UNII
- 2VG74ZW2K5
- Sequence
- GTSLSPPPESSGSRQQPGLSAPHSRQIPAPQGAVLVQREKDLPNYNWNSFGLRF-
NH2 - Format
- Lyophilized vial
- Type
- Single compound
Identifiers from PubChem. Verify against the supplier’s documentation for your lot.
Research stats
How much has been published, not how good it is.
- PubMed records
- 109
- Indexed as human research
- 69
- Animal-only research
- 33
- Randomized controlled trials
- 12
- Registered trials
- 19
- Trials with posted results
- 6
- NIH-funded projects naming it
- 12
Counts from title/abstract searches of PubMed, ClinicalTrials.gov, openFDA and NIH RePORTER, checked 2026-10-24. Names shared with other substances can inflate counts. FAERS reports are spontaneous and do not establish cause. Funding shows interest, not evidence. Method
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