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Kisspeptin

Grade B: Human evidence, not approved for this use

TL;DR: Kisspeptin is not FDA-approved for any indication in the United States and is classified as investigational. Human clinical evidence comes primarily from academic research centers in the UK and US, with the strongest data in reproductive endocrinology. Phase 1 and Phase 2 trials have demonstrated that kisspeptin-54 can trigger LH surges and oocyte maturation in women undergoing IVF. A phase 2 randomized trial at Imperial College London reported a live-birth rate of about 45 percent per embryo transfer when kisspeptin-54 was used to trigger egg maturation. This approach has been studied particularly in women at high risk of ovarian hyperstimulation syndrome (OHSS). Small trials have also examined kisspeptin's role in stimulating endogenous LH secretion in men with hypogonadotropic hypogonadism and in assessing HPG axis function diagnostically. Outside reproductive endocrinology, evidence is limited to mechanistic and early-phase studies. The total human trial exposure across all kisspeptin research is small, no Phase 3 trials have been completed, and no regulatory submission has been filed in the US.

Key Takeaways

  • Grade B: Human evidence, not approved for this use
  • Not FDA approved: Investigational only; not FDA-approved for any indication and not authorized for compounding in the United States.
  • Compounding: Not FDA-approved for any indication. The FDA placed kisspeptin-10 in Category 2 of its interim 503A bulk-substances policy (substances it has identified as presenting potential significant safety risks), so it is not eligible for routine pharmacy compounding. Clinical use occurs only within approved research protocols at academic institutions.
Kisspeptin chemical structure
Structure via PubChem CID 71306396

Mechanism

Kisspeptin is a hypothalamic neuropeptide that binds the KISS1R (GPR54) receptor on GnRH neurons, stimulating pulsatile GnRH release and downstream LH and FSH secretion from the pituitary.

Evidence

Kisspeptin is not FDA-approved for any indication in the United States and is classified as investigational. Human clinical evidence comes primarily from academic research centers in the UK and US, with the strongest data in reproductive endocrinology. Phase 1 and Phase 2 trials have demonstrated that kisspeptin-54 can trigger LH surges and oocyte maturation in women undergoing IVF. A phase 2 randomized trial at Imperial College London reported a live-birth rate of about 45 percent per embryo transfer when kisspeptin-54 was used to trigger egg maturation. This approach has been studied particularly in women at high risk of ovarian hyperstimulation syndrome (OHSS). Small trials have also examined kisspeptin's role in stimulating endogenous LH secretion in men with hypogonadotropic hypogonadism and in assessing HPG axis function diagnostically. Outside reproductive endocrinology, evidence is limited to mechanistic and early-phase studies. The total human trial exposure across all kisspeptin research is small, no Phase 3 trials have been completed, and no regulatory submission has been filed in the US.

Safety and risks

Human clinical trial data are limited in sample size and duration, so the full safety profile of kisspeptin is not established. Reported adverse effects in controlled research settings have been mild, primarily mild nausea or flushing. Because kisspeptin powerfully stimulates the hypothalamic-pituitary-gonadal axis, chronic or unmonitored administration carries theoretical risk of dysregulating reproductive hormone balance, including potential effects on testosterone, estrogen, ovarian function, and menstrual regularity. The impact on hormonally sensitive conditions (hormone-receptor positive cancers, endometriosis, polycystic ovary syndrome) has not been characterized in controlled trials. Kisspeptin is not included on the FDA's 503A or 503B bulk drug substance lists and is not legal to compound for clinical use in the US; compounded preparations carry uncharacterized risks of purity, potency, and sterility.

Interactions

Concurrent use with GnRH agonists or antagonists, sex steroid hormones, or other HPG axis-active agents could produce unpredictable additive or antagonistic hormonal effects; combination use has not been characterized in human safety studies.

Federal compounding status

503A/503B Category 2: significant safety risk as of 2023.

The FDA placed this substance (503A) in Category 2 of its interim bulk-substances policy, the list it has identified as presenting potential significant safety risks, so it is not eligible for routine pharmacy compounding. FDA source

Federal status only, from public FDA records. State pharmacy-board rules vary and are not covered here. This is regulatory reporting, not legal advice. All compounds.

Compounding legality

Not FDA-approved for any indication. The FDA placed kisspeptin-10 in Category 2 of its interim 503A bulk-substances policy (substances it has identified as presenting potential significant safety risks), so it is not eligible for routine pharmacy compounding. Clinical use occurs only within approved research protocols at academic institutions.

Sources

  1. Clinical Potential of Kisspeptin in Reproductive Health. (2021) review
  2. [Potential clinical application of Kisspeptin in reproductive endocrinology]. (2017) review
  3. Kisspeptin and neurokinin B: roles in reproductive health. (2025) review
  4. The Role of Kisspeptin in the Control of the Hypothalamic-Pituitary-Gonadal Axis and Reproduction. (2022) review
  5. Kisspeptin system-physiology and clinical perspectives. (2025) review
  6. Kisspeptin and clinical disorders. (2013) review
  7. Clinical Translational Studies of Kisspeptin and Neurokinin B. (2019) review
  8. Potential Clinical Use of Kisspeptin. (2015) review
  9. Interactions between kisspeptin and bone: Cellular mechanisms, clinical evidence, and future potential. (2024) review
  10. Reproductive functions of Kisspeptin/KISS1R Systems in the Periphery. (2019) review
  11. Kisspeptin Administration Stimulates Reproductive Hormones but Does Not Affect Anxiety in Humans. (2025) rct
  12. Advances in clinical applications of kisspeptin-GnRH pathway in female reproduction. (2022) review
  13. The Neuroendocrine Regulation of Reproductive Behavior and Emotional Control by Kisspeptin. (2025) review
  14. Understanding the functions of kisspeptin and kisspeptin receptor (Kiss1R) from clinical case studies. (2019) review
  15. The human hypothalamic kisspeptin system: Functional neuroanatomy and clinical perspectives. (2021) review
  16. The kisspeptin-GnRH pathway in human reproductive health and disease. (2014) review
  17. Invited review: Translating kisspeptin and neurokinin B biology into new therapies for reproductive health. (2022) review
  18. Kisspeptin receptor agonist has therapeutic potential for female reproductive disorders. (2020) other
  19. Intranasal kisspeptin administration rapidly stimulates gonadotropin release in humans. (2025) rct
  20. Associations of serum kisspeptin levels with metabolic and reproductive parameters in men. (2021) other
  21. Kisspeptin signaling in the amygdala modulates reproductive hormone secretion. (2016) other
  22. Kisspeptin a potential therapeutic target in treatment of both metabolic and reproductive dysfunction. (2024) review
  23. The Emerging Therapeutic Potential of Kisspeptin and Neurokinin B. (2024) review
  24. The kisspeptin receptor: A key G-protein-coupled receptor in the control of the reproductive axis. (2018) review
  25. Kisspeptin in functional hypothalamic amenorrhea: Pathophysiology and therapeutic potential. (2024) review

Kisspeptin is Not FDA approved. PeptideGrids presents evidence and regulatory status for informational purposes only. We do not sell, supply, source, or help anyone obtain this compound, and we provide no dosing or administration guidance. This is not medical advice; consult a licensed clinician. Full disclaimer.

Last reviewed June 1, 2026 by PeptideGrids editorial team (independently audited).