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Hexarelin (Examorelin)

Hexapeptide GHRP | Growth Hormone Release & Cardioprotection

Hexarelin (also known as Examorelin) is a synthetic hexapeptide growth hormone releasing peptide (GHRP) and one of the most potent GH secretagogues studied. Derived from GHRP-6 by Mediolanum Farmaceutici, it stimulates growth hormone release through the ghrelin receptor (GHS-R1a) and uniquely binds to cardiac CD36 receptors, providing cardioprotective effects independent of GH release. Hexarelin reached Phase II clinical trials for growth hormone deficiency and congestive heart failure but was discontinued in 2005 for strategic reasons. Research demonstrates its potential in cardioprotection, neuroprotection, and metabolic regulation.

Daily dose

100-300 mcg daily (divided doses)

Frequency

2-3 times daily

Cycle length

8-16 weeks

Storage

2-8°C (refrigerated)

Key benefits

Most potent GHRP for GH release, unique cardioprotective effects via CD36 receptor, supports tissue repair and recovery, neuroprotective properties

How it works

Binds to ghrelin receptor (GHS-R1a) on pituitary somatotrophs to stimulate pulsatile GH release. Also activates cardiac CD36 receptors providing GH-independent cardioprotection through anti-apoptotic and anti-fibrotic mechanisms.

Dosage protocols

Goal

GH Optimization

Dose

100 mcg · 3x daily (morning, midday, evening)

Route

SubQ

Goal

Cardioprotection Research

Dose

100-200 mcg · 2x daily

Route

SubQ

Goal

Recovery/Anti-Aging

Dose

100 mcg · 2x daily (morning and bedtime)

Route

SubQ

Goal

With GHRH (Synergistic)

Dose

100 mcg hexarelin + 100 mcg CJC-1295 · 2-3x daily

Route

SubQ

Research indications

hormonal

Growth Hormone Release — Most potent GHRP studied, stimulating dose-dependent GH release with peak levels at 30 minutes post-injection
IGF-1 Elevation — Increases insulin-like growth factor 1 through enhanced pituitary GH secretion
Pulsatile GH Pattern — Preserves natural GH secretion rhythm when dosed appropriately throughout the day

cardiovascular

Cardioprotection — Binds CD36 cardiac receptors, reducing infarct size and improving left ventricular function independent of GH
Anti-Fibrotic Effects — Reduces cardiac collagen deposition and fibrosis in heart failure models
Ischemia-Reperfusion Protection — Protects cardiac tissue from damage during ischemia and subsequent reperfusion

neuroprotection

Neurogenesis Support — Promotes hippocampal neurogenesis and survival of new adult-born neurons
Anti-Apoptotic Effects — Protects neurons from oxidative stress-induced cell death through Bcl-2 and caspase modulation
ALS Research — Shows protective effects in ALS cell models by reducing oxidative damage and inflammation

recovery

Muscle Preservation — Protects against chemotherapy-induced cachexia by improving mitochondrial function
Tissue Repair — Enhanced recovery through GH-mediated protein synthesis and cellular regeneration
Exercise Recovery — Supports post-workout recovery through growth factor cascade activation

metabolic

Lipid Metabolism — Improves lipid profiles by decreasing triglycerides and supporting healthy fat metabolism
Insulin Sensitivity — Research indicates improvements in insulin sensitivity and glucose regulation

Administration

injectable
nasal

Interactions

Synergistic
CJC-1295 (without DAC) — GHRP + GHRH combination provides complementary GH release through different receptor pathways. Studies show synergistic peak GH secretion rates greater than the arithmetic sum of isolated administration.
Synergistic
Sermorelin — GHRH analog enhances hexarelin's pulsatile GH release. Research demonstrates synergistic effects when co-administered, though synergy diminishes with repeated dosing.
Compatible
Ipamorelin — Both are GHRPs with different selectivity profiles. Combining may soften hexarelin's cortisol/prolactin elevation while maintaining GH output through complementary receptor activity.
Use Caution
GHRP-6 — Both GHRPs stimulate GH through similar pathways. Combination may cause excessive GH spikes and additive side effects including cortisol and prolactin elevation.
Use Caution
GHRP-2 — Structurally similar GHRPs with overlapping mechanisms. Combining provides diminishing returns with increased risk of hormonal side effects.
Use Caution
CJC-1295 with DAC — DAC version provides continuous GH elevation which may conflict with hexarelin's pulsatile release pattern, potentially reducing synergistic benefits and accelerating desensitization.
Monitor Combination
MK-677 — Both stimulate GH through ghrelin receptor. MK-677's continuous oral action combined with hexarelin may lead to excessive and prolonged GH elevation requiring monitoring.
Synergistic
Tesamorelin — FDA-approved GHRH analog works through complementary pathway. Studies on GHRH + hexarelin combinations show synergistic GH release significantly greater than either alone.
Avoid Combination
HGH — Exogenous HGH suppresses natural GH release pathways. Combining defeats hexarelin's purpose and may cause excessive GH levels with increased side effects.
Compatible
BPC-157 — Different mechanisms with no known interactions. BPC-157's tissue repair properties may complement hexarelin's recovery and cardioprotective effects.

Safety notes

Most potent GHRP but also highest side effect profile among GHRPs

Elevates cortisol and prolactin at standard doses - unlike Ipamorelin

May cause water retention, particularly in first 1-2 weeks

Can affect glucose metabolism - monitor if diabetic or pre-diabetic

Not recommended for those with active cancer due to growth-promoting effects

WADA prohibited substance - banned in competitive sports

Secondary hypogonadism possible with prolonged use due to prolactin elevation

Partial desensitization is normal and reversible with cycling

Research studies

Growth Hormone-Releasing Activity of Hexarelin in Humans (1994)

Human | 0.5-2 μg/kg IV | Single dose | 12 adult males

Double-blind, placebo-controlled dose-response study demonstrating dose-dependent GH release. Peak plasma GH at 30 minutes, returning to baseline within 240 minutes. Cmax values: 26.9 ng/ml (0.5 μg/kg), 52.3 ng/ml (1 μg/kg), 55.0 ng/ml (2 μg/kg) vs 3.9 ng/ml placebo.

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Hexarelin Treatment Preserves Myocardial Function After MI (2018)

Mouse model | 0.3 mg/kg/day SubQ | 21 days | LAD ligation

Demonstrated significant improvement in LV function after 14 days. Hexarelin treatment reduced LV collagen concentration by ~53%, decreased inflammatory cytokines (TNF-α, IL-1β), and shifted autonomic balance toward parasympathetic predominance.

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Protective Effects of Hexarelin in ALS Neuroblastoma Model (2023)

In vitro | 1 μM | Human neuroblastoma cells | SOD1-G93A mutation

Hexarelin protected cells from H2O2-induced cytotoxicity by increasing Bcl-2 expression, reducing caspase-3 activation, and modulating MAPK/Akt pathways. Significantly decreased γH2AX positive cells indicating DNA damage protection.

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Cardiovascular Action of Hexarelin Review (2014)

Review | Multiple studies | CD36 receptor mechanism

Comprehensive review establishing hexarelin's cardioprotective effects through CD36 cardiac receptor binding independent of GH release. Documented anti-apoptotic effects, reduced infarct size in ischemia-reperfusion, and improved LVEF by 6.7 percentage points in human volunteers.

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Hexarelin Desensitization Study (2000)

Human | SubQ twice daily | 16 weeks | 12 elderly subjects

Investigated long-term GH response attenuation. AUC-GH decreased significantly from baseline at weeks 4 and 16. Four weeks post-treatment, GH response recovered to baseline levels, demonstrating desensitization is partial and reversible.

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Hexarelin Pharmacokinetics in Rats (1999)

Rat model | IV and SubQ | Multiple doses | PK analysis

IV administration showed half-life of 75.9 min, clearance of 7.6 ml/min/kg, and Vd of 744 ml/kg. SubQ administration confirmed absence of accumulation with dose-independent clearance (12-15 ml/min/kg).

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Related compounds

GHRP-6MK-677IpamorelinCardiogen