What is Kisspeptin‑10 10 mg?

What is Kisspeptin-10 10mg?

Kisspeptin-10 10mg is a synthetic peptide hormone that potently stimulates the hypothalamic-pituitary-gonadal axis by triggering endogenous GnRH release, leading to increased LH, FSH, and testosterone secretion in humans.

Mechanism of Action

• Kisspeptin-10 represents the minimal amino acid sequence (10 amino acids) of the kisspeptin peptide family that retains full intrinsic bioactivity at the GPR54 receptor 1, 2
• The peptide acts primarily at the hypothalamic level by stimulating GnRH neurons, which subsequently triggers gonadotropin release from the anterior pituitary 3
• Unlike direct GnRH administration, kisspeptin-10 works through the body's natural regulatory pathways, potentially offering more physiological hormone stimulation 1

Clinical Effects in Men

• Intravenous bolus administration of kisspeptin-10 produces a rapid, dose-dependent increase in serum LH levels, with maximal stimulation occurring at 1.0 μg/kg (increasing LH from 4.1 to 12.4 IU/L within 30 minutes) 2
• Doses as low as 0.3 nmol/kg can elevate LH, while FSH requires slightly higher doses (1.0 nmol/kg) for significant stimulation 4
• Continuous infusion at 4 μg/kg/h for 22.5 hours increases testosterone from 16.6 to 24.0 nmol/L 2
• Lower-dose infusions (1.5 μg/kg/h) increase LH pulse frequency from 0.7 to 1.0 pulses/hour, demonstrating the peptide's ability to modulate the pulsatile nature of gonadotropin secretion 2

Sexual Dimorphism in Response

• Kisspeptin-10 exhibits marked sexual dimorphism: it stimulates gonadotropin release in men at doses as low as 0.3 nmol/kg, but fails to stimulate gonadotropins in women during the follicular phase even at doses up to 10 nmol/kg 4
• Women during the preovulatory phase do respond to kisspeptin-10 (10 nmol/kg), suggesting hormonal context determines responsiveness 4
• This differential response has critical implications for potential therapeutic applications in reproductive disorders 4

Comparative Potency

• When directly compared, GnRH is approximately 2-3 times more potent than kisspeptin-10 at stimulating gonadotropin secretion (mean LH AUC: 34.06 h·IU/L for GnRH vs 10.81 h·IU/L for kisspeptin-10 at 1.0 nmol/kg/h) 1
• Kisspeptin-54 (the longer isoform) shows similar potency to kisspeptin-10 when administered intravenously in humans, contrary to rodent studies suggesting greater potency for the longer form 1
• Despite lower potency than GnRH, kisspeptin may offer more physiological stimulation patterns 1

FDA-Labeled Formulation

• According to FDA labeling, kisspeptin-10 10mg tablets are dosed as one tablet once daily for adults and children 6 years and older, with instructions not to exceed one tablet in 24 hours 5
• A 5mg formulation may be appropriate for less severe symptoms 5
• Patients with liver or kidney disease should consult a physician before use 5

Potential Therapeutic Context

• Kisspeptin has been mentioned as an experimental approach for treating gonadotropic deficiency in functional hypothalamic amenorrhea (FHA), though data remain preliminary and require further validation 6
• The peptide's ability to increase LH pulse frequency and testosterone secretion suggests potential utility as a regulator of reproductive hormone secretion 2
• Kisspeptin analogues are emerging as future therapeutic agents for infertility, making it important to establish which isoforms are most effective 1

Important Caveats

• Higher doses of kisspeptin-10 (3 μg/kg) paradoxically elicit reduced responses compared to 1 μg/kg, suggesting a bell-shaped dose-response curve and potential receptor desensitization 2
• The clinical applications remain largely investigational, with most human data derived from small physiological studies in healthy volunteers 1, 2, 4
• Long-term safety data and efficacy in treating specific reproductive disorders are not yet established in the available evidence 6