SERMORELIN

Peptide Data Sheet for Pharmacists and Compounding Professionals

BASIC INFORMATION

Name: Sermorelin (GRF 1-29)
Class: Growth hormone-releasing hormone (GHRH) analog
Structure: 29-amino acid peptide, N-terminal fragment of GHRH
Molecular Weight: 3357.9 g/mol
Sequence: Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-NH₂
Chemical Modifications:

  • C-terminal amidation
  • Represents the first 29 amino acids of the 44-amino acid human GHRH

Available Forms:

  • Previously FDA-approved as Geref® (discontinued in 2008)
  • Compounded formulations (subject to regulatory requirements)
  • Research peptide

REGULATORY STATUS

FDA Status

  • Previously FDA-approved for diagnostic evaluation of growth hormone deficiency in children
  • Geref® (sermorelin acetate) was discontinued in 2008 (not for safety reasons)
  • Currently not available as an FDA-approved medication
  • May be legally compounded by pharmacies under certain circumstances

Legal Considerations

  • Unlike some peptides, sermorelin has historical FDA approval
  • Compounding pharmacies may prepare sermorelin under appropriate prescribing
  • Must be prescribed by a licensed healthcare provider for a legitimate medical purpose
  • Subject to state pharmacy regulations and USP standards

MECHANISM OF ACTION

Sermorelin is a synthetic analog of growth hormone-releasing hormone (GHRH) that:

  • Binds to GHRH receptors in the anterior pituitary gland
  • Stimulates the synthesis and pulsatile release of endogenous growth hormone (GH)
  • Increases insulin-like growth factor 1 (IGF-1) production as a secondary effect
  • Preserves physiological pulsatile pattern of GH release (unlike exogenous GH)
  • May help maintain pituitary function

Unlike exogenous growth hormone administration, sermorelin:

  • Maintains negative feedback regulation of the GH axis
  • Allows for natural fluctuations in GH levels
  • May have a more physiological effect profile
Mechanism of Action

PHARMACOKINETICS

| Parameter | Value | Notes | |———–|——-|——-| | Absorption | Rapid after subcutaneous injection | Bioavailability: ~0.5-1.5% | | Distribution | Limited data available | Primarily acts on pituitary receptors | | Metabolism | Rapid enzymatic degradation | Primarily by dipeptidyl peptidase IV | | Elimination | Half-life: ~10-20 minutes | Rapid clearance limits duration of action |

CLINICAL APPLICATIONS

Historical FDA-Approved Indications

  • Diagnostic evaluation of growth hormone secretion in children

Potential Applications (Off-Label/Investigational)

Note: Evidence quality varies; clinical judgment required.

  • Age-related growth hormone decline
  • Body composition improvement
  • Sleep quality enhancement
  • Recovery from injury
  • Cognitive function (limited evidence)

DOSING GUIDELINES

Historical FDA-Approved Dosing

  • Diagnostic testing: 1 mcg/kg body weight, administered IV or SC

Common Off-Label Dosing Practices

Note: Not FDA-approved dosing regimens; clinical judgment required.

| Purpose | Typical Dose Range | Frequency | |———|——————-|———–| | GH stimulation | 100-500 mcg | Once daily, typically before bedtime | | Anti-aging protocols | 200-300 mcg | Once daily, typically before bedtime |

Administration Timing:

  • Typically administered in the evening to align with natural GH pulses
  • Consistent timing recommended for optimal effect

ADMINISTRATION

Routes

  • Subcutaneous injection (most common)
  • Intravenous injection (less common, primarily for diagnostic use)

Preparation and Administration

  • Reconstitute with bacteriostatic water or sterile saline
  • Store reconstituted solution refrigerated (2-8°C/36-46°F)
  • Administer using insulin syringe or similar
  • Rotate injection sites
  • Typical injection sites: abdomen, thigh, or deltoid

SAFETY PROFILE

Adverse Effects

| Frequency | Adverse Effects | |———–|—————-| | Common | Injection site reactions (redness, pain, swelling)<br>Flushing<br>Headache<br>Dizziness | | Less Common | Nausea<br>Altered taste sensation<br>Hyperactivity<br>Dysphagia | | Rare | Hypersensitivity reactions<br>Antibody formation<br>Chest tightness |

Potential Risks and Concerns

  • Potential for growth promotion in pre-existing cancers (theoretical)
  • Glucose metabolism alterations
  • Fluid retention
  • Joint pain
  • Unknown long-term effects with extended use

Contraindications

  • Active malignancy
  • Intracranial lesions
  • Pregnancy and lactation
  • Hypersensitivity to sermorelin or mannitol
  • Uncontrolled diabetes mellitus

SPECIAL POPULATIONS

Pregnancy and Lactation

  • No adequate studies in pregnant women
  • Not recommended during pregnancy or lactation

Pediatric

  • Historically used diagnostically in children
  • Not recommended for off-label use in pediatric populations
  • May affect growth plates and development

Geriatric

  • No specific dose adjustments required
  • May have increased sensitivity to adverse effects
  • Monitor for fluid retention and arthralgia

DRUG INTERACTIONS

| Interacting Drug | Effect | Management | |——————|——–|————| | Glucocorticoids | May inhibit response to sermorelin | Monitor efficacy | | Opioid analgesics | May blunt GH response | Consider timing separation | | Somatostatin analogs | Antagonize sermorelin effects | Avoid combination | | Aromatase inhibitors | May enhance GH response | Monitor for enhanced effects | | Insulin/oral hypoglycemics | Potential for altered glucose metabolism | Monitor blood glucose |

PHARMACIST GUIDANCE

Compounding Considerations

  • Requires aseptic technique and sterile compounding environment
  • Stability affected by temperature and mechanical agitation
  • Typical beyond-use date: 30 days refrigerated after reconstitution
  • Adhere to USP <797> standards for sterile compounding
  • Consider preservative-free formulations for patients with sensitivities

Storage and Handling

  • Store lyophilized peptide at -20°C
  • Reconstituted solutions stored at 2-8°C
  • Protect from light
  • Avoid repeated freeze-thaw cycles
  • Discard if solution appears cloudy or contains particles

Patient Counseling Points

  1. Administration Technique
    • Proper subcutaneous injection technique
    • Importance of injection site rotation
    • Proper disposal of needles and syringes
  2. Storage Requirements
    • Keep refrigerated
    • Do not freeze reconstituted solution
    • Discard after beyond-use date
  3. Common Side Effects
    • Injection site reactions typically mild and transient
    • Headache and flushing usually resolve with continued use
    • When to contact healthcare provider
  4. Monitoring Parameters
    • Signs of fluid retention
    • Changes in blood glucose (diabetic patients)
    • Follow-up laboratory testing as directed
  5. Lifestyle Considerations
    • Optimal timing (evening administration)
    • Potential benefits of adequate sleep
    • Importance of consistent administration schedule

MONITORING RECOMMENDATIONS

Laboratory Parameters

  • IGF-1 levels (baseline and periodic)
  • Growth hormone stimulation (if clinically indicated)
  • Fasting blood glucose
  • Hemoglobin A1c (in diabetic patients)
  • Thyroid function tests

Clinical Monitoring

  • Body composition changes
  • Sleep quality
  • Energy levels
  • Adverse effects
  • Quality of life measures

REFERENCES

  1. Prakash A, Goa KL. Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency. BioDrugs. 1999;12(2):139-57.
  2. Walker RF. Sermorelin: a better approach to management of adult-onset growth hormone insufficiency? Clin Interv Aging. 2006;1(4):307-308.
  3. Merriam GR, et al. Growth hormone releasing hormone and growth hormone secretagogues in normal aging. Endocrine. 2003;22(1):41-8.
  4. FDA. Geref (sermorelin acetate) Prescribing Information (historical).
  5. Vittone J, et al. Effects of single nightly injections of growth hormone-releasing hormone (GHRH 1-29) in healthy elderly men. Metabolism. 1997;46(1):89-96.