IPAMORELIN

Peptide Data Sheet for Pharmacists and Compounding Professionals

BASIC INFORMATION

Name: Ipamorelin
Class: Growth hormone secretagogue, synthetic ghrelin analog
Structure: Pentapeptide (5-amino acid peptide)
Molecular Weight: 711.85 g/mol
Sequence: Aib-His-D-2-Nal-D-Phe-Lys-NH₂
Chemical Modifications:

  • Contains non-natural amino acids (D-2-Nal, D-Phe)
  • C-terminal amidation
  • Aminoisobutyric acid (Aib) at position 1

Available Forms:

  • Research peptide
  • Compounded formulations (subject to regulatory requirements)
  • Not available as an FDA-approved medication

REGULATORY STATUS

FDA Status

  • Not FDA-approved for any medical condition
  • Classified as a research compound
  • FDA has clarified it is among peptides unlawful to use in making compounded medications
  • Included on FDA’s list of substances nominated for the 503B bulks list that raised significant safety concerns

Legal Considerations

  • Not approved for human use or consumption
  • Often marketed “for research purposes only”
  • Compounding pharmacies should be aware that FDA has specifically identified Ipamorelin as a substance that should not be used in compounding

MECHANISM OF ACTION

Ipamorelin is a selective growth hormone secretagogue that:

  • Binds to the ghrelin/growth hormone secretagogue receptor (GHS-R) in the pituitary gland
  • Stimulates the pulsatile release of growth hormone (GH)
  • Does not significantly affect other pituitary hormones (ACTH, cortisol, prolactin, LH, FSH, TSH)
  • Increases insulin-like growth factor 1 (IGF-1) production as a secondary effect
  • Unlike GHRP-2 and GHRP-6, does not stimulate appetite or significantly increase prolactin or cortisol

The selective nature of Ipamorelin distinguishes it from other growth hormone secretagogues, potentially offering a more targeted effect profile.

Mechanism of Action

PHARMACOKINETICS

| Parameter | Value | Notes | |———–|——-|——-| | Absorption | Rapid after subcutaneous injection | Complete bioavailability | | Distribution | Limited data available | Primarily studied in animal models | | Metabolism | Likely enzymatic degradation | Specific pathways not well characterized | | Elimination | Half-life: ~2 hours | Limited human data available |

Note: Pharmacokinetic data is primarily derived from animal studies; human data is extremely limited.

POTENTIAL APPLICATIONS (INVESTIGATIONAL)

Note: All applications are investigational and not FDA-approved. This information is provided for educational purposes only.

Endocrine

  • Growth hormone deficiency (investigational)
  • Age-related decline in growth hormone

Metabolic

  • Body composition improvement
  • Lean muscle mass preservation
  • Fat reduction

Other Investigational Areas

  • Recovery from injury
  • Sleep quality improvement
  • Bone mineral density enhancement
  • Anti-aging research

ADMINISTRATION (INVESTIGATIONAL)

Routes

  • Subcutaneous injection (most common)
  • Intramuscular injection (less common)

Investigational Dosing

Note: No established safe or effective dosing regimen exists. The following information is based on research protocols and is not a recommendation for clinical use.

| Purpose | Investigational Dose Range | Frequency | |———|—————————-|———–| | Research protocols | 200-300 mcg | 1-3 times daily | | Typically administered | Evening or before sleep | To align with natural GH pulses |

SAFETY PROFILE

Reported Adverse Effects

Note: Safety data is limited and primarily from small studies and anecdotal reports.

  • Injection site reactions (redness, pain, swelling)
  • Headache
  • Dizziness
  • Water retention
  • Numbness or tingling in extremities
  • Increased insulin resistance
  • Fatigue

Potential Risks and Concerns

  • Potential for growth promotion in pre-existing cancers
  • Glucose metabolism alterations
  • Fluid retention
  • Carpal tunnel syndrome
  • Gynecomastia
  • Unknown long-term effects
  • Lack of quality control in commercially available products

Contraindications (Theoretical)

  • Active malignancy
  • History of pituitary disorders
  • Uncontrolled diabetes
  • Pregnancy and lactation
  • Children and adolescents
  • Intracranial hypertension

SPECIAL POPULATIONS

Pregnancy and Lactation

  • No human data available
  • Avoid use due to unknown risks

Pediatric

  • No human data available
  • Not recommended for use in pediatric populations
  • Theoretical risk of affecting growth plates and development

Geriatric

  • No specific data available
  • Potentially higher risk of adverse effects
  • May have different response due to age-related changes in GH/IGF-1 axis

PHARMACIST GUIDANCE

Compounding Considerations

  • FDA has clarified that Ipamorelin is among peptides unlawful to use in making compounded medications
  • Pharmacists should be aware of regulatory restrictions
  • If compounding is legally permitted in specific circumstances:
    • Requires aseptic technique and sterile compounding environment
    • Stability affected by temperature and mechanical agitation
    • Adhere to USP <797> standards for sterile compounding

Storage and Handling (Research Settings)

  • Store lyophilized peptide at -20°C
  • Reconstituted solutions typically stored at 2-8°C
  • Use within 30 days of reconstitution
  • Avoid repeated freeze-thaw cycles
  • Protect from light

Patient Counseling Points

  • Not FDA-approved for any indication
  • Limited safety and efficacy data in humans
  • Unknown long-term effects
  • Potential for serious adverse effects
  • Importance of discussing all supplements and medications with healthcare providers
  • FDA has warned against its use in compounded medications

COMPARISON TO OTHER GROWTH HORMONE SECRETAGOGUES

| Feature | Ipamorelin | GHRP-2 | GHRP-6 | |———|————|——–|——–| | Selectivity | Highly selective for GH release | Less selective | Less selective | | Effect on Cortisol | Minimal | Significant increase | Significant increase | | Effect on Prolactin | Minimal | Moderate increase | Moderate increase | | Effect on Appetite | Minimal | Moderate increase | Significant increase | | Side Effect Profile | Generally milder | More pronounced | More pronounced |

ETHICAL AND PROFESSIONAL CONSIDERATIONS

For Pharmacists

  • Be aware of FDA position on Ipamorelin in compounding
  • Understand legal and ethical implications of dispensing non-FDA approved peptides
  • Maintain professional standards when discussing investigational compounds
  • Provide evidence-based information when consulted about Ipamorelin
  • Consider liability issues related to non-FDA approved compounds

For Researchers

  • Ensure proper informed consent in research settings
  • Follow institutional and regulatory guidelines for research peptides
  • Document and report adverse events
  • Maintain scientific integrity in research protocols

REFERENCES

  1. FDA. Certain Bulk Drug Substances for Use in Compounding May Present Significant Safety Risks. https://www.fda.gov/drugs/human-drug-compounding/certain-bulk-drug-substances-use-compounding-may-present-significant-safety-risks
  2. Raun K, et al. Ipamorelin, the first selective growth hormone secretagogue. Eur J Endocrinol. 1998;139(5):552-61.
  3. Gobburu JV, et al. Pharmacokinetics-pharmacodynamics of ipamorelin, a growth hormone releasing peptide, in human volunteers. J Clin Pharmacol. 1999;39(11):1150-6.
  4. Johansen PB, et al. The effects of growth hormone secretagogues on bone. Growth Horm IGF Res. 1999;9(Suppl A):18-22.
  5. FDA. Pharmacy Compounding of Human Drug Products Under Section 503A of the Federal Food, Drug, and Cosmetic Act. https://www.fda.gov/media/94393/download