Hexarelin common uses, half-life, side effects and more

Also known as Examorelin

About

Hexarelin is a synthetic growth hormone releasing peptide. It makes the pituitary release its own growth hormone. It is GHRP-6 with one extra methyl group added to help it survive digestion. It releases more growth hormone than GHRP-6 does. No source establishes by how much. It reached phase 2 trials for growth hormone deficiency and was discontinued there. No regulator anywhere has ever reviewed it. It also binds a second receptor found on heart and immune cells. That is unusual for this family and is why it turns up in cardiovascular research.

Common uses

  • Raising growth hormone without injecting growth hormone itself
  • Recovery and body composition (community use)
  • Short cycles chosen because the response fades
  • Appetite stimulation
  • Historical testing for growth hormone deficiency

Frequency

Once or twice daily in community practice

Dosing

Community practice is 100 to 200 mcg under the skin once or twice a day. That figure comes from forum protocols catalogued in a review. The longest published trial happens to land in the same place, at 1.5 mcg per kg under the skin twice a day for 16 weeks. Other published work used single doses into a vein at 0.5 to 2 mcg per kg. Children in the growth studies were given 60 mcg per kg by nose three times a day. The commonly quoted cycle of a few weeks on and several weeks off matches no source. The one catalogued community cycle runs 8 to 12 weeks on and 4 weeks off. The growth hormone response is down about a third after one week of twice-daily dosing and down about 45 percent by 16 weeks. It returns to baseline four weeks after stopping.

Half-life

No human study has measured how long hexarelin itself lasts in the blood. The widely quoted 55 minutes is not the peptide's half-life. It is how fast the growth hormone response fades. That same sentence also gives the 30 minute peak and the 240 minute return to baseline. Measured half-lives exist only in animals at about two hours in dogs and about 76 minutes in rats. A review that reports a bare half-life for hexarelin is quoting the rat figure without saying so.

Side effects

  • A rise in cortisol, ACTH, and prolactin after a single dose
  • The cortisol and ACTH response fades with repeated dosing before the growth hormone response does
  • Less deep sleep when dosed in the evening
  • Increased appetite in rodent studies
  • No side effects were reported in the published human courses given by nose or by mouth

How it works

Hexarelin activates the ghrelin receptor on the pituitary and releases the body's own growth hormone. That raises IGF-1 from the liver. It also binds a scavenger receptor called CD36 on heart cells, blood vessel lining, and immune cells. The two receptors do different jobs. The short-lived boost in heart contraction runs through the ghrelin receptor rather than through CD36. What CD36 does in the heart is narrow the coronary arteries. The researchers who found that proposed it as a possible mechanism for coronary spasm rather than as a benefit. CD36 also drives cholesterol handling in immune cells. That work was done in cell culture and mice rather than in hearts.

Research quality

Hexarelin reached phase 2 for growth hormone deficiency and was discontinued. It was never tested in phase 3 and no regulator has reviewed it. The human record is a set of small short studies of hormone release. The longest ran 16 weeks in 12 elderly adults. The most-cited finding from that work is the fading growth hormone response. A small program gave it by nose to short children for several months and growth speeded up. Those studies had no control group and never reported adult height. A blood marker of heart risk doubled in those same children and insulin rose more than threefold. No human study has ever measured a heart outcome.

Warnings

  • It is banned in sport at all times and is named individually on the prohibited list
  • Its effect on coronary arteries in laboratory hearts was narrowing rather than widening and was proposed as a mechanism for coronary spasm
  • Children given it by nose for several months had a doubling of a blood marker of heart risk and a large rise in insulin
  • Mouse studies covering pregnancy found fewer successful pregnancies and impaired memory in the offspring
  • Growth hormone and IGF-1 drive cell growth so it is not for anyone with a current or past cancer

Sources (11)

  • Growth hormone releasing activity of hexarelin in humans, a dose-response study and the origin of the misread 55 minute figure (Imbimbo et al.)

    European Journal of Clinical Pharmacology 1994 (PMID 7957536)

  • Growth hormone releasing activity of hexarelin after intravenous, subcutaneous, intranasal and oral administration in man (Ghigo et al.)

    Journal of Clinical Endocrinology and Metabolism 1994 (PMID 8126144)

  • Radioimmunoassay for hexarelin and its pharmacokinetic studies in dogs (Roumi et al.)

    Peptides 1995 (PMID 8545255)

  • Kinetics and disposition of hexarelin in rats, reporting a 76 minute intravenous half-life (Roumi et al.)

    Drug Metabolism and Disposition 2000 (PMID 10611139)

  • Sixteen weeks of twice-daily hexarelin in adults, showing a falling and reversible growth hormone response (Rahim, O'Neill and Shalet)

    Journal of Clinical Endocrinology and Metabolism 1998 (PMID 9589671)

  • Repeated subcutaneous hexarelin abolishes the ACTH and cortisol response before blunting growth hormone (Maccario et al.)

    European Journal of Endocrinology 2002 (PMID 11888836)

  • Acute hexarelin and cardiac performance in coronary artery disease patients during bypass surgery (Broglio et al.)

    European Journal of Pharmacology 2002 (PMID 12144941)

  • CD36 mediates the cardiovascular action of growth hormone releasing peptides, reporting coronary vasoconstriction (Bodart et al.)

    Circulation Research 2002 (PMID 11988484)

  • Intranasal hexarelin in short children, reporting raised lipoprotein(a) and insulin (Laron et al.)

    European Journal of Endocrinology 1997 (PMID 9150696)

  • Hexarelin given across the evening reduces deep sleep and delta power (Frieboes et al.)

    Psychoneuroendocrinology 2004 (PMID 15177700)

  • Prohibited list section S2.2.4, naming examorelin among the growth hormone releasing peptides

    World Anti-Doping Agency 2026 Prohibited List

PubMed search terms (4)

Related

Quick facts
Category
Growth Hormone Muscle
Routes
Subcutaneous Intravenous Intranasal
Legal status
Research use only Gray market Banned in sport
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