Ipamorelin

Summary

Ipamorelin is a synthetic pentapeptide GH secretagogue with high selectivity for the ghrelin receptor. It promotes GH release in a pulsatile, physiologic manner with minimal off-target hormonal stimulation. Used extensively in research settings for body composition, recovery, and anti-aging applications. Not FDA-approved for human use but widely used in compounded formulations and research contexts.

Mechanism of Action

Selectively binds and activates the growth hormone secretagogue receptor (GHSR-1a), stimulating pulsatile release of growth hormone from the anterior pituitary without significantly affecting cortisol, prolactin, or ACTH levels. Acts synergistically with endogenous GHRH.

Routes of Administration

Goals & Uses

• Body Composition Improvement (Lean Mass / Fat Loss)Metabolic / Body CompositionLow
• Recovery and Tissue RepairRegenerative / RecoveryLow
• Increased Growth Hormone SecretionEndocrine / HormonalModerate
• Sleep Quality ImprovementNeurological / SleepLow
• Anti-aging / LongevityAgingLow
• Bone Density MaintenanceMusculoskeletalLow

Contraindications

• Active malignancyOncologyHighUse caution or avoid depending on agent and context
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Diabetic retinopathyOphthalmologyHigh
• Uncontrolled Diabetes MellitusMetabolic / EndocrineModerate
• Pituitary Tumor or Hypothalamic DiseaseNeurological / EndocrineHigh

Adverse Effects

• Injection site reactionsLocalCommon
• HeadacheNeurologicUncommonPain in the head or upper neck
• Water retention / edemaFluid BalanceCommon
• FlushingVascularCommonWarmth and redness of the skin
• Transient HypoglycemiaMetabolicUncommon
• Elevated IGF-1EndocrineCommon

Drug Interactions

• Insulin / antidiabetic agentsModerate
• CJC-1295 / GHRH AnaloguesModerate
• CorticosteroidsLow
• Thyroid hormone replacementLow

Population Constraints

• Elderly (>65 years)AgeRelative
• Pediatric patientsAgeRelative
• Lactating IndividualsReproductiveAbsolute
• Patients with history of cancerOncologyRelative
• Patients with Insulin Resistance or Type 2 DiabetesMetabolicRelative

Regulatory Status

• European UnionUnapprovedNot approved by EMA. Available only for research purposes.
• United StatesUnapprovedNot FDA-approved. Historically available through compounding pharmacies; FDA has moved to restrict compounded ipamorelin formulations (including CJC-1295/ipamorelin) as of 2023–2024 regulatory actions. Classified as a research compound.
• United KingdomUnapprovedNot approved by MHRA. Research use only.

Not approved by the FDA, EMA, or other major regulatory agencies for human therapeutic use. In 2023–2024, the FDA moved to restrict compounding of ipamorelin/CJC-1295 combinations. It remains classified as a research compound. Frequently used off-label in anti-aging and performance medicine clinics via compounding pharmacies.

Evidence & Sources

No sources recorded yet.