What are the benefits and dosing recommendations for Ipamorelin (growth hormone secretagogue)?

Ipamorelin Benefits and Dosing

Ipamorelin is not FDA-approved for human use and lacks sufficient clinical evidence to support its safety and efficacy for growth hormone stimulation in adults.

What is Ipamorelin?

• Ipamorelin is a synthetic pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) that functions as a growth hormone secretagogue (GHS) 1
• It was developed as a selective growth hormone releasing peptide that stimulates GH release via GHRP-like receptors 1
• Unlike other growth hormone secretagogues, ipamorelin demonstrates selectivity for GH release without significantly affecting ACTH or cortisol levels 1

Potential Benefits Based on Limited Research

• Bone Growth Effects:

  • In animal studies, ipamorelin has been shown to dose-dependently increase longitudinal bone growth rate in rats 2
  • May counteract glucocorticoid-induced decrease in bone formation, as demonstrated in adult rat models 3

• Body Composition Effects:

  • Paradoxically, ipamorelin has been shown to increase body fat in both GH-deficient and GH-intact mice 4
  • This increase in adiposity appears to be through GH-independent mechanisms that may include increased feeding and elevated serum leptin 4

Pharmacokinetics

• Short terminal half-life of approximately 2 hours 5
• Clearance of 0.078 L/h/kg and volume of distribution at steady-state of 0.22 L/kg 5
• Shows dose-proportional pharmacokinetics 5

Important Safety Considerations

• Growth hormone therapy in general carries risks of:
  • Intracranial hypertension (rare but serious) 6
  • Glucose metabolism alterations including hyperinsulinemia 6
  • Secondary hyperparathyroidism 6
  • Lipoatrophy at injection sites 6

Lack of Clinical Evidence and Regulatory Status

• There are no human clinical trials evaluating ipamorelin for growth hormone deficiency treatment
• Not approved by the FDA for human use
• The available evidence is primarily from animal studies and limited pharmacokinetic studies in humans 5, 2, 1
• Current clinical guidelines for growth hormone therapy do not mention ipamorelin as a treatment option 7

Contraindications (Based on General GH Therapy Guidelines)

• Known hypersensitivity to the active substance 6
• Active malignancy 6
• Closed epiphyses (in pediatric populations) 7
• Severe secondary hyperparathyroidism 7

Conclusion on Clinical Use

• Ipamorelin remains an experimental compound with insufficient clinical evidence to support its use in humans
• The benefits observed in animal studies (bone growth stimulation) 2 must be weighed against potential risks and lack of long-term safety data
• Any consideration of ipamorelin use should occur within a research context with appropriate ethical oversight