Kisspeptin

Safety Profile

How It Works

Kisspeptin is the brain's master switch for reproductive hormones. It activates KISS1R on specialized GnRH neurons, which tells the pituitary gland to release LH and FSH -- the hormones that drive testosterone production in men and estrogen/progesterone/ovulation in women. Two groups of Kisspeptin brain cells work together: one generates the steady background pulse of reproductive hormones (arcuate nucleus), and the other triggers the big hormone surge needed for ovulation (AVPV, in women). Think of Kisspeptin as the ignition key for the entire reproductive hormone chain (PMID 21470997, PMID 21632807, PMID 24615662).

Studied Dosages

7 dosing entries documented.

Studies

Tier 3: Multiple controlled human studies demonstrate kisspeptin's potent stimulation of LH/FSH in healthy volunteers and patients with reproductive disorders (PMID 21470997, PMID 21632807, PMID 21976724, PMID 19820030, PMID 30046307). Phase 3 mechanistic studies completed (NCT03286517, NCT03771326, NCT03315325), but these are investigator-led physiological studies, not pivotal therapeutic approval trials. Kisspeptin-54 has been used as an IVF oocyte maturation trigger in clinical trials (PMID 24615662, PMID 26194072). However, Kisspeptin is not FDA-approved, is listed in FDA 503A Category 2 with safety concerns, no pivotal Phase 3 efficacy/approval trials have been completed for a specific disease indication, and individual human studies have small sample sizes. Both evaluators agreed on Tier 3.

Legal Status

Not FDA-approved for any indication. No Drugs@FDA or FDA label matches found. Kisspeptin-10 is listed in FDA 503A Category 2 (added September 29, 2023) due to potential significant safety risks: immunogenicity for certain routes of administration, complexities with peptide-related impurities and API characterization, and limited or no human safety data for proposed routes. ClinicalTrials.gov shows completed and withdrawn investigator studies but no active therapeutic development program. NOTE: HHS Secretary Kennedy announced Feb 27, 2026 that this peptide is expected to be reclassified to Category 1 (pending formal FDA publication) (compoundable). Official FDA publication pending as of March 2026.