Investigational / not FDA-approved

Hexarelin

Examorelin GHS-R agonist hexapeptide — investigational; not FDA-approved.

Editorial review:

What evidence says

Evidence snapshot

This drawer marks papers. It is not a plan, a dose, or a source. A paper is a bounded report. It is not a protocol. Grades name the object. They are not a safety rating.

Identity lock. Hexarelin (INN examorelin) is a synthetic hexapeptide GH secretagogue: His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH₂. PubChem CID 6918297; formula C47H58N12O6; MW ~887.0; CAS 140703-51-1 (also 208251-52-9 on PubChem xref — note dual RN). It is a ghrelin / GHS-receptor agonist class object. It is not GHRP-2 (pralmorelin), not GHRP-6, and not ipamorelin — different sequences and pharmacology grades. No approved indication in this framing. Off-label does not apply. There is no label to be off of. Mark GH-axis stimulation, pituitary-reserve testing, or exploratory cardiac papers as named endpoints — not bodybuilding.

Bottom line

Human evidence is mainly acute endocrine provocation: hexarelin releases GH (and can affect ACTH/cortisol/prolactin) in children, adults, and elderly volunteers; it has been explored as a pituitary-reserve / GHD-diagnostic stimulus. Small acute cardiac-performance work exists. Most cardioprotection, cardiomyocyte, and disease-model papers are preclinical. Do not average hexarelin into GHRP-2, GHRP-6, or ipamorelin drawers, and do not inflate physique claims from GH spikes.

Papers

Early human — GH / endocrine responses

PMID 8762732 — Massoud 1996

Tested: repeated administration of hexarelin and GHRH on GH responsivity (desensitization / responsivity object).

Does not show: chronic outpatient therapy benefit, or equivalence to GHRP-2/GHRP-6.

PMID 9437229 — Arvat 1997

Tested: age-related variations in GH, prolactin, ACTH, and cortisol responses to hexarelin.

Does not show: a treatment indication for aging or body composition.

PMID 9801989 — Bellone 1998

Tested: hexarelin as a GH stimulus across pubertal children and adults (power of stimulus; weaker in prepubertal comparison context in that line of work).

Does not show: approved pediatric growth therapy, or ipamorelin results.

PMID 10990150 — Rahim 1998

Tested: whether desensitization to hexarelin occurs with repeated use (GH-axis responsivity).

Does not show: a physique or recovery protocol grade.

PMID 10197083 — Rahim 1998

Tested: effect of body composition on hexarelin-induced GH release in normal elderly subjects.

Does not show: hexarelin as a fat-loss or muscle-building treatment.

PMID 10469018 — Korbonits 1999

Tested: hexarelin as a test of pituitary reserve in patients with pituitary disease.

Does not show: chronic replacement therapy equivalence to rhGH, or recreational use safety/efficacy.

PMID 11238504 — Arvat 2001

Tested: endocrine activities of ghrelin in humans compared and interacted with hexarelin.

Does not show: that hexarelin equals endogenous ghrelin for all endpoints, or a approved drug use.

Human — exploratory cardiac

PMID 12144941 — Broglio 2002

Tested: acute hexarelin on cardiac performance in patients with coronary artery disease during bypass surgery.

Does not show: an approved cardiology indication, or chronic outpatient cardiac benefit.

Preclinical / mechanism context (not human efficacy)

PMID 25278975 — Mao 2014

Tested: narrative/review of cardiovascular actions of hexarelin (secondary synthesis of mostly non-human and limited human signals).

Does not show: a new pivotal human cardiac RCT.

PMID 11322493 — Filigheddu 2001

Tested: hexarelin protection of H9c2 cardiomyocytes from doxorubicin-induced cell death (cell model).

Does not show: human cardioprotection efficacy.

PMID 12379504 — Pettersson 2002

Tested: ghrelin and hexarelin stimulation of H9c2 cardiomyocyte proliferation.

Does not show: human clinical cardiac remodeling benefit.

What is not established

Approved therapeutic use. Body composition, anti-aging, sleep, or “recovery” as human treatment claims. Equivalence to GHRP-2, GHRP-6, or ipamorelin. Chronic safe outpatient GH-secretagogue therapy. Identity between laboratory hexarelin and unlabeled vials. Acute GH release is not a physique indication.

Selected sources

8762732 9437229 9801989 10990150 10197083 10469018 11238504 12144941 25278975 11322493 12379504

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