Monograph in Regulatory peptides
Kisspeptin-10
The shortest fully active form of kisspeptin, a hypothalamic hormone that switches on the reproductive axis. Human studies are small physiology experiments measuring hormone responses.
Also called KP-10 · Metastin (45-54)
Best evidence: Randomized human trials
Small human physiology studies, including a 2026 randomized, single-blind, placebo-controlled study in 15 men; endpoints are hormone levels, not clinical outcomes.
Not FDA-approved · FDA compounding Category 2 (503A)
Residue Editorial Team · updated
What is Kisspeptin-10?
Kisspeptin-10 is the minimal kisspeptin sequence with full intrinsic bioactivity; kisspeptins stimulate GnRH and thus LH and FSH secretion1PubMedKisspeptin-10 is a potent stimulator of LH and increases pulse frequency in men. George JT et al. J Clin Endocrinol Metab. 2011.. In healthy men, intravenous boluses raised LH within 30 minutes, and infusions raised testosterone and LH pulse frequency1. Women respond differently depending on cycle phase and sex steroids2PubMedThe effects of kisspeptin-10 on reproductive hormone release show sexual dimorphism in humans. Jayasena CN et al. J Clin Endocrinol Metab. 2011.,3PubMedKisspeptin-10 stimulation of gonadotrophin secretion in women is modulated by sex steroid feedback. George JT et al. Hum Reprod. 2012.. FDA placed Kisspeptin-10 in compounding Category 2 in September 20234FDACertain Bulk Drug Substances for Use in Compounding that May Present Significant Safety Risks. U.S. FDA, content current as of 04/22/2026..
Key findings
- IV bolus in healthy men raised LH from 4.1 to 12.4 IU/L at 30 minutes at the maximal 1 µg/kg; 3 µg/kg gave a smaller response1.
- A 22.5-hour infusion at 4 µg/kg/h raised testosterone from 16.6 to 24.0 nmol/L1.
- Healthy women in the follicular phase showed no gonadotropin response even at high doses, but women in the preovulatory phase did2.
- In 2026, daily 8-hour subcutaneous infusions sustained LH increases over 12 days in healthy men, while continuous infusion for 5 days did not5PubMedChronic subcutaneous kisspeptin-10 stimulates gonadotropin secretion for 12 days in healthy men. Yeung AC et al. Eur J Endocrinol. 2026..
- FDA added Kisspeptin-10 to Category 2 for 503A compounding on September 29, 2023, citing immunogenicity risk and limited safety information4.
What is Kisspeptin-10, chemically?
| PubChem CID | 25240297 “Kisspeptin-10” |
|---|---|
| Formula | C63H83N17O14 |
| Molecular weight | 1,302.4 g/mol |
| CAS (as listed) | 374675-21-5 |
| FDA UNII | FS1N52VS3S |
| InChIKey | RITKWYDZSSQNJI-INXYWQKQSA-N |
| Length | 10 residues |
| Route in trials | Intravenous or subcutaneous (research infusions and boluses) |
| Mechanism | Kisspeptin receptor (KISS1R) agonist; stimulates hypothalamic GnRH release |
- Hydrophobic
- Polar
- Basic (+)
- Gly / Pro / Cys
What is kisspeptin-10?
Kisspeptins are hypothalamic peptides critical to human reproductive physiology2. Kisspeptin-10 is the minimal sequence with full intrinsic bioactivity1. PubChem lists the sequence YNWNSFGLRF and the synonym metastin 45-546PubChemPubChem compound record: Kisspeptin-10. C63H83N17O14 · MW 1302.4 g/mol..
How does kisspeptin-10 work?
Kisspeptins stimulate gonadotropin-releasing hormone (GnRH) and thus the pituitary's release of LH and FSH1. Animal work suggests kisspeptin integrates metabolic signals with the reproductive axis7PubMedExploring the pathophysiology of hypogonadism in men with type 2 diabetes: kisspeptin-10 stimulates serum testosterone and LH secretion in men with type 2 diabetes and mild biochemical hypogonadism. George JT et al. Clin Endocrinol (Oxf). 2013., and in women its effect depends on sex-steroid feedback, with the pituitary an important site of estrogen feedback3.
What have studies found?
Men. In the first human dose-response study, intravenous boluses produced a rapid, dose-dependent LH rise, maximal at 1 µg/kg. Infusion raised LH pulse frequency, pulse size and testosterone1. A 2026 randomized, single-blind, placebo-controlled study found daily 8-hour subcutaneous infusions sustained higher LH for 12 days, whereas gonadotropins returned to vehicle levels during 5 days of continuous infusion5.
Women. Healthy women in the follicular phase did not respond at doses that worked in men, but preovulatory women did2. Postmenopausal women had larger LH and FSH responses, and women on the combined pill had none3.
Disorders. In men with type 2 diabetes and low testosterone, an 11-hour infusion raised LH pulse frequency and testosterone7. In two women with hyperprolactinemic amenorrhea, a 12-hour infusion reactivated gonadotropin secretion8PubMedHypothalamic-Pituitary-Ovarian Axis Reactivation by Kisspeptin-10 in Hyperprolactinemic Women With Chronic Amenorrhea. Millar RP et al. J Endocr Soc. 2017..
Registered trials. ClinicalTrials.gov lists phase 1 and 2 studies of kisspeptin in reproductive disorders, alongside observational studies of natural levels9TrialClinicalTrials.gov registry search: kisspeptin-10 OR kisspeptin. 36 registered studies at fetch..
Is Kisspeptin-10 FDA-approved?
| Record | Status | Source |
|---|---|---|
| FDA approval | No approved application Drugs@FDA returned no application for “Kisspeptin-10”. | openFDA |
| Compounding: Category 2 Kisspeptin-10 | 503A category 2 since September 29, 2023 “Compounded drugs containing Kisspeptin-10 may pose risk for immunogenicity for certain routes of administration and may have complexities with regard to peptide-related impurities and API characterization. FDA has no, or only limited, safety-related information for the proposed routes of administration. Therefore, the agency lacks sufficient information to know whether the drug would cause harm when administered to humans.” | 4 |
FDA lists Kisspeptin-10 in Category 2 for 503A compounding, added on September 29, 2023. It cites possible immunogenicity, impurity and characterization complexities, and no or only limited safety information for the proposed routes, so FDA lacks sufficient information to know whether it would cause harm in humans4.
What is still unknown?
- Clinical outcomes such as fertility; published endpoints are hormone levels5.
- Long-term dosing. The longest protocol we found ran 12 days5.
What effects has Kisspeptin-10 shown, by body system?
Each row is graded separately using the Residue evidence scale: a compound can carry an A for one use and a D for another.
| System | What was observed | Grade |
|---|---|---|
| LH and testosterone (men) | Dose-dependent LH, FSH and testosterone increases with IV and SC dosing, sustained for 12 days with intermittent infusion1,5. | B |
| Gonadotropins (women) | Response depends on cycle phase and sex-steroid exposure2,3. | C |
| Hypogonadism in type 2 diabetes | Raised LH pulse frequency and testosterone in 4–5 men7. | C |
| Hyperprolactinemic amenorrhea | Reactivated gonadotropin secretion in 2 women8. | C |
How much research is there on Kisspeptin-10?
| Phase | Studies | Breakdown |
|---|---|---|
| Phase 1 | 11 | 7 completed, 1 active or recruiting, 3 stopped, 0 other |
| Phase 2 | 8 | 3 completed, 2 active or recruiting, 3 stopped, 0 other |
| Phase 3 | 3 | 3 completed, 0 active or recruiting, 0 stopped, 0 other |
| Not applicable | 3 | 2 completed, 1 active or recruiting, 0 stopped, 0 other |
| Observational | 11 | 8 completed, 1 active or recruiting, 0 stopped, 2 other |
Compare and continue
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Questions readers ask
Is kisspeptin-10 FDA-approved?
No. Drugs@FDA returned no application, and FDA placed Kisspeptin-10 in Category 2 for 503A compounding on September 29, 20234.
Does kisspeptin-10 raise testosterone?
In small studies of healthy men, infusions raised testosterone along with LH1,5, and an infusion raised testosterone in men with type 2 diabetes and low testosterone7. These are short hormone studies, not treatment trials.
References
Every source below was retrieved from its official API or page and cached on the data-edition date. Numbers match the margin notes.
- 1 PubMed 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. PMID 21632807; doi:10.1210/jc.2011-0089.
- 2 PubMed Jayasena CN, Nijher GM, Comninos AN, et al. The effects of kisspeptin-10 on reproductive hormone release show sexual dimorphism in humans. J Clin Endocrinol Metab 2011. PMID 21976724; doi:10.1210/jc.2011-1408.
- 3 PubMed George JT, Anderson RA, Millar RP. Kisspeptin-10 stimulation of gonadotrophin secretion in women is modulated by sex steroid feedback. Hum Reprod 2012. PMID 22956346; doi:10.1093/humrep/des326.
- 4 FDA Certain Bulk Drug Substances for Use in Compounding that May Present Significant Safety Risks. U.S. FDA, content current as of 04/22/2026.
- 5 PubMed Yeung AC, Phylactou M, Koysombat K, et al. Chronic subcutaneous kisspeptin-10 stimulates gonadotropin secretion for 12 days in healthy men. Eur J Endocrinol 2026. PMID 42549827; doi:10.1093/ejendo/lvag134.
- 6 PubChem PubChem compound record: Kisspeptin-10. C63H83N17O14 · MW 1302.4 g/mol.
- 7 PubMed George JT, Veldhuis JD, Tena-Sempere M, et al. Exploring the pathophysiology of hypogonadism in men with type 2 diabetes: kisspeptin-10 stimulates serum testosterone and LH secretion in men with type 2 diabetes and mild biochemical hypogonadism. Clin Endocrinol (Oxf) 2013. PMID 23153270; doi:10.1111/cen.12103.
- 8 PubMed Millar RP, Sonigo C, Anderson RA, et al. Hypothalamic-Pituitary-Ovarian Axis Reactivation by Kisspeptin-10 in Hyperprolactinemic Women With Chronic Amenorrhea. J Endocr Soc 2017. PMID 29264460; doi:10.1210/js.2017-00328.
- 9 ClinicalTrials.gov ClinicalTrials.gov registry search: kisspeptin-10 OR kisspeptin. 36 registered studies at fetch.