Kisspeptin-10

Also known as: Metastin 45-54, Kisspeptin (112-121), KP-10

Evidence: Preclinical

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Overview

Ten-residue C-terminal kisspeptin fragment that activates KISS1R (GPR54); IV doses raised LH and LH pulse frequency in small human studies. Not approved anywhere; on FDA's 503A safety list.

Kisspeptins are cleavage products of the KISS1 gene product and are the natural ligands of the receptor GPR54, now KISS1R (Kotani 2001). Kisspeptin-10 is the shortest fully active C-terminal fragment. Human work with it consists of short IV dosing studies in healthy volunteers measuring LH, FSH and testosterone (George 2011; Jayasena 2011; Chan 2011). The IVF egg-maturation and sexual-brain-processing studies often cited for kisspeptin used kisspeptin-54, a different peptide. Listed on FDA's 503A category 2 (safety concerns) page, live table, added 2023-09-29, as of 2026-04-22: https://www.fda.gov/drugs/human-drug-compounding/certain-bulk-drug-substances-use-compounding-may-present-significant-safety-risks

Benefits

LH and FSH release (human IV physiology studies, men and women), increased LH pulse frequency (healthy men, small studies), IVF egg-maturation trigger (kisspeptin-54 only, not this peptide)

Dosing reference

Research dose: Community range 100 to 400 mcg subcutaneous; human studies of kisspeptin-10 dosed it intravenously.
Range: 100 to 400 mcg, 1x daily or as directed
Reconstitution: 2 mL bacteriostatic water
Common vial sizes: 1 mg, 5 mg

Human studies of kisspeptin-10 gave it intravenously; subcutaneous community use is not dose-tested. It stimulates endogenous GnRH release. FDA lists kisspeptin-10 on the live 503A category 2 table (see side effects).

Mechanism

Kisspeptin-10 binds KISS1R (GPR54), a Gq-coupled receptor identified as the kisspeptin receptor in 2001 (Kotani 2001). In humans its effects are consistent with action above the pituitary on GnRH neurons: an IV bolus raised LH within minutes in healthy men, and a continuous infusion increased LH pulse frequency (George 2011). A single bolus also reset the timing of the next GnRH-driven LH pulse (Chan 2011). Responses differ by sex and cycle phase; women in the follicular phase responded much less than men (Jayasena 2011).

Evidence

Preclinical: animal or in vitro data only

IV kisspeptin-10 raised LH in healthy men in a dose-dependent way, and infusion increased LH pulse frequency (George et al., 2011)
LH response to kisspeptin-10 was strong in men and weak in women in the follicular phase (Jayasena et al., 2011)
A single IV bolus of kisspeptin-10 reset the timing of GnRH-driven LH pulses in men (Chan et al., 2011)
Kisspeptin-10 was identified as an active cleavage product binding GPR54 in cell assays (Kotani et al., 2001)
Human-trial status: no kisspeptin-10 trial has tested a clinical outcome; IV kisspeptin-54, a different isoform, stimulated the reproductive axis in men (Dhillo et al., 2005) and triggered egg maturation in IVF (Jayasena et al., 2014); listed on FDA's 503A category 2 page since 2023-09-29

References

Side effects

Published human studies are short IV sessions in small groups of healthy volunteers and report hormone changes rather than a systematic safety profile (George 2011; Jayasena 2011). It acutely raises LH, FSH and sex steroids. Repeated-dose effects on the reproductive axis have not been studied in humans. FDA placed kisspeptin-10 on its 503A category 2 list, citing safety concerns for compounding.

Storage

Storage: Refrigerated (2-8°C)
Lyophilized: 24+ months at room temperature
Reconstituted: 28-30 days refrigerated

Pharmacology

Half-life: No human plasma half-life for kisspeptin-10 confirmed in this pass; ~28 min is the kisspeptin-54 figure from Dhillo 2005, a different isoform, and was removed
Bioavailability: Human studies gave kisspeptin-10 by IV bolus or infusion (George 2011; Chan 2011). No subcutaneous or other non-IV bioavailability figure has been published for this fragment.
Molecular weight: 1302.47 Da
Sequence: Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2

Stacks with

Gonadorelin (GnRH)