Kisspeptin-10

HRT MEMBERS ONLY

INDICATIONS FOR USE

Kisspeptin-10 is used off-label to treat secondary hypogonadism and as a potential adjunct to testosterone replacement therapy. It enhances endogenous testosterone production by stimulating the hypothalamic-pituitary-gonadal axis. It is also being investigated for its roles in fertility and sexual function.

ROUTE OF ADMINISTRATION

  • Subcutaneous injection

FORMULATIONS AND PRICING

FormulationPrice
5mg multi-dose vial (1mg/mL x 5mL)$135

COMMON INITIAL DOSING REGIMENS

  • A typical dose is 0.1–0.3 mg subcutaneously, administered 2–3 times weekly. Dosing may be adjusted based on clinical response and serum testosterone levels.

MECHANISM OF ACTION

  • Kisspeptin-10 is a potent stimulator of the hypothalamic-pituitary-gonadal axis. It binds to GPR54 (kisspeptin receptor), triggering the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus. This leads to increased secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary, ultimately boosting testosterone production in the testes.

COMMON SIDE EFFECTS

  • Endocrine: Transient elevation in estradiol levels, which can cause mild gynecomastia or water retention.

  • General: Headache, dizziness, and fatigue, particularly during the initial treatment period.

  • Injection Site: Mild erythema, swelling, or discomfort at the injection site.

  • Rare: Overstimulation of the gonadal axis may lead to mood swings or irritability.

CONTRAINDICATIONS

  • Absolute: Known hypersensitivity to kisspeptin-10 or its components.

  • Relative: Use with caution in patients with pre-existing conditions such as gynecomastia, significant baseline estradiol elevation, or pituitary dysfunction. It is not effective in cases of primary testicular failure.

MORE INFORMATION

  • FDA Safety Data Sheet not available (experimental peptide therapy)

  • Sharma A. Kisspeptin and Testicular Function-Is it Necessary?. Int J Mol Sci. 2020 [PubMed Link]

  • Feng T. Kisspeptin and its Effect on Mammalian Spermatogensis. Curr Drug Metab. 2019 [PubMed Link]

  • Tsoutsouki J. Novel therapeutic avenues for kisspeptin. Curr Opin Pharmacol. 2022 [PubMed Link]

  • Rønnekleiv OK. Hypothalamic Kisspeptin Neurons and the Control of Homeostasis. Endocrinology. 2022 [PubMed Link]

  • Mills EGA. Kisspeptin as a Behavioral Hormone. Semin Reprod Med. 2019 [PubMed Link]

  • Lee EB. Sexual Dimorphism in Kisspeptin Signaling. Cells. 2022 [PubMed Link]

  • Tsukamura H. Kisspeptin and mammalian reproduction. Peptides. 2024 [PubMed Link]

  • Trevisan CM. Kisspeptin/GPR54 System: What Do We Know About Its Role in Human Reproduction?. Cell Physiol Biochem. 2018 [PubMed Link]

  • Mills EGA. Kisspeptin and the control of emotions, mood and reproductive behaviour. J Endocrinol. 2018 [PubMed Link]

  • Abbara A. Clinical Potential of Kisspeptin in Reproductive Health. Trends Mol Med. 2021 [PubMed Link]

  • Sliwowska JH. Kisspeptin a potential therapeutic target in treatment of both metabolic and reproductive dysfunction. J Diabetes. 2024 [PubMed Link] 

  • Ghaderpour S. The relation between obesity, kisspeptin, leptin, and male fertility. Horm Mol Biol Clin Investig. 2021 [PubMed Link] 

  • Comninos AN. Emerging Roles of Kisspeptin in Sexual and Emotional Brain Processing. Neuroendocrinology. 2018 [PubMed Link]

  • Koysombat K. Kisspeptin and Neurokinin B: roles in reproductive health. Physiol Rev. Published online January 15, 2025 [PubMed Link]