Sexual Health & HPG Axis
Peptides affecting sexual function, libido, fertility, and the hypothalamic-pituitary-gonadal axis.
Clinical Overview
Sexual Health & HPG Axis
Peptides affecting sexual function, libido, fertility, and the hypothalamic-pituitary-gonadal axis.
Sexual-health peptides act on central and peripheral pathways governing libido, arousal, and reproductive endocrine function — from FDA-approved melanocortin agonists to HPG-axis preservation agents used alongside testosterone replacement.
Mechanism Classes
Melanocortin receptor agonists
PT-141 (bremelanotide) activates central melanocortin receptors involved in sexual desire and arousal. FDA-approved for HSDD in premenopausal women.
GnRH & kisspeptin analogs
Gonadorelin is a synthetic GnRH decapeptide used for pulsatile pituitary stimulation. Kisspeptin-10 is an upstream regulator of GnRH release, used primarily in research.
HPG-axis preservation agents
Gonadorelin (and historically hCG as an LH analog) preserves testicular size and function during exogenous testosterone replacement by maintaining LH / FSH stimulation.
Regulatory Status
FDA-Approved
- PT-141 / Bremelanotide (HSDD, premenopausal women)
Investigational / Off-Label
- Kisspeptin-10
- Gonadorelin (compounded)
PT-141 is FDA-approved for female HSDD only; off-label use in men and for other indications is common but unapproved. Gonadorelin has historical endocrinology use but the compounded form is unapproved.
Evidence Base
PT-141 has FDA-approval-grade Phase 3 data for female HSDD. Gonadorelin has decades of endocrinology literature for pulsatile GnRH replacement. Kisspeptin-10 remains primarily a research tool with emerging clinical translation.
Primary-Literature References
12
Across 1 linked monograph
Prescribing Considerations
- 1Screen for uncontrolled hypertension and cardiovascular disease before PT-141 (contraindications; transient BP elevation of 3–6 mmHg).
- 2Counsel on common PT-141 side effects: nausea, flushing, headache (typically transient).
- 3TRT monitoring on gonadorelin protocols: testosterone, estradiol, PSA, hematocrit.
- 4Distinguish agents preserving endogenous function (gonadorelin, kisspeptin) from downstream-acting agents (PT-141, testosterone itself).
- 5Kisspeptin-10 use outside research settings is investigational — document informed consent.
- 6Off-label PT-141 use in men for ED is common but not FDA-approved — ensure consent reflects off-label framing.
Peptides in this category(1)
Clinical monographs for each agent — dosing ranges, safety profile, evidence, and prescribing considerations.
2 additional monographs in this category are in clinical review and will be published soon.