Sermorelin Kit

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		Peptide Sciences	Liberty Peptides
Cost per milligram	$3.80 - $5.20	$8.33	$7.20
Purity	99.84%	99.3%	99.14%
Certified Endotoxin-safe	Yes	No	No
Independently Tested	Yes	No	No

Peptide Partners Manufacturer Id: WF03

Batch Id: SM20250723

Overview

(For educational purposes only)

Sermorelin is a synthetic peptide that functions as an analog of growth hormone-releasing hormone (GHRH), designed to stimulate the body's natural production of growth hormone. This 29-amino acid peptide represents the biologically active N-terminal fragment of the full 44-amino acid human GHRH molecule. Though it was once FDA-approved for diagnostic and therapeutic applications in pediatric growth disorders, sermorelin is no longer available as an approved drug product in the United States but may still be obtained through compounding pharmacies under certain circumstances.

Molecular Structure and Biochemical Properties

Sermorelin is a precisely designed synthetic peptide with specific biochemical characteristics that enable its growth hormone-stimulating functions.

Chemical Composition

Sermorelin is comprised of 29 amino acids in the sequence YADAIFTNSYRKVLGQLSARKLLQDIMSR, which corresponds to the first 29 amino acids of the natural human GHRH^[1][2]. The full chemical designation is sermorelin acetate, the acetate salt of an amidated synthetic peptide^[1]. This structure gives the compound its specific properties:

·         Molecular formula: C₁₄₉H₂₄₆N₄₄O₄₂S

·         Molecular weight: 3357.9 g/mol

·         Physical form: White to off-white solid

·         Melting point: >189°C (decomposes)

·         Solubility: Slightly soluble in acetic acid, trifluoroacetic acid, and water^[3]

The N-terminal sequence of GHRH is remarkably conserved across several mammalian species, including humans, pigs, and cattle, highlighting its evolutionary importance^[2]. Despite containing only the first 29 amino acids of the natural 44-amino acid hormone, sermorelin retains the full biological activity needed to stimulate growth hormone secretion.

Pharmacokinetic Profile

Sermorelin displays distinctive pharmacokinetic properties that influence its clinical application:

·         Absorption: After subcutaneous administration, peak concentrations are reached rapidly in 5-20 minutes

·         Bioavailability: Mean absolute bioavailability after subcutaneous administration is approximately 6%

·         Distribution: Following intravenous administration, the mean volume of distribution ranges between 23.7-25.8 liters

·         Half-life: Extremely short at 11-12 minutes after either intravenous or subcutaneous administration

·         Clearance: Rapid, with values in adults ranging between 2.4-2.8 L/min^[4]

These properties necessitate specific administration protocols to achieve therapeutic effects, despite the peptide's rapid clearance from circulation.

Mechanism of Action

Sermorelin operates through specific receptor-mediated pathways to stimulate growth hormone production and release.

Receptor Binding and Signaling

The primary mechanism of action involves direct interaction with specialized receptors in the anterior pituitary:

·         Sermorelin binds to the growth hormone-releasing hormone receptor (GHRH-R) on pituitary somatotroph cells

·         This binding mimics the activity of endogenous GHRH, activating the receptor's signaling cascade

·         The activated pathway stimulates the synthesis and secretion of growth hormone from the pituitary gland

·         Unlike synthetic growth hormone, sermorelin does not directly replace GH but rather promotes the body's natural production^[1][5]

This mechanism preserves the natural pulsatile pattern of growth hormone secretion, which may offer advantages over direct growth hormone replacement.

Physiological Effects

The stimulation of endogenous growth hormone production leads to several physiological responses:

·         Increased plasma growth hormone concentrations, typically in a pulsatile fashion

·         Subsequent elevation of insulin-like growth factor 1 (IGF-1) production, primarily in the liver

·         Enhanced protein synthesis in multiple tissues

·         Stimulation of cellular growth and division

·         Support for bone growth in pediatric patients with growth hormone deficiency^[1][5][6]

By working through the body's natural pathways, sermorelin potentially offers a more physiological approach to growth hormone augmentation compared to direct GH administration.

Historical Clinical Applications

Sermorelin has been used in various clinical contexts, though its approved applications in the United States have changed over time.

FDA-Approved Uses

When previously available as an approved drug (marketed as Geref), sermorelin had specific sanctioned uses:

·         Treatment of idiopathic or organic growth hormone deficiency in children with growth failure

·         Diagnostic evaluation of pituitary function to assess growth hormone secretory capacity^[1][5][4][7]

The FDA granted sermorelin acetate orphan drug designation in 1988 for "Treatment of idiopathic or organic growth hormone deficiency in children with growth failure," and it received marketing approval in September 1997^[7]. However, the manufacturer withdrew the product from the U.S. market in November 2002, and it is no longer available as an FDA-approved medication^[3].

Off-Label Applications

Beyond its previously approved uses, sermorelin has been investigated for several potential applications:

·         Prevention of HIV-induced weight loss

·         Management of age-related growth hormone decline

·         Support for muscle enhancement in athletic and fitness contexts

·         Improvement of overall well-being and vitality

·         Enhancement of sleep quality^[1][6][4]

These applications reflect growing interest in growth hormone modulation for both medical and wellness purposes, though clinical evidence supporting these uses varies considerably.

Current Regulatory Status

The regulatory landscape surrounding sermorelin has evolved significantly since its initial approval.

Current Approval Status

As of 2025, sermorelin is not FDA-approved for any indication in the United States^[6]. While it was previously marketed under the trade name Geref by Serono Laboratories, the FDA now lists it as a "discontinued drug product"^[3]. Important regulatory milestones include:

·         Orphan drug designation: September 14, 1988

·         Marketing approval: September 26, 1997

·         Market exclusivity ended: September 26, 2004

·         Voluntary market withdrawal: November 2002^[3][7]

This change in status significantly affects how patients can legally access the compound.

Availability and Prescription Pathways

Despite lacking FDA approval, sermorelin may still be legally available through specific channels:

·         Compounded formulations prescribed by licensed healthcare providers

·         Available only through a valid prescription following proper consultation and evaluation

·         Cannot be marketed with claims regarding safety or efficacy, as compounded medications are not FDA-reviewed

·         Banned by most sports organizations as a performance-enhancing substance^[6]

Patients seeking sermorelin treatment must typically complete a structured evaluation process, including comprehensive medical assessment, laboratory testing, and detailed health history review before receiving a prescription.

Administration and Dosing

Specific administration protocols are recommended for sermorelin therapy to maximize effectiveness and minimize side effects.

Delivery Methods

Sermorelin is typically administered through subcutaneous injection:

·         Most commonly injected into the abdomen (stomach) or thigh

·         Requires sterile, disposable syringes and needles of appropriate volume

·         Injection sites should be periodically rotated to prevent local irritation

·         Before administration, reconstitution with diluent is required, with careful attention to sterile technique^[8][4]

The subcutaneous route is preferred due to the peptide's poor oral bioavailability, as digestive enzymes would rapidly degrade the peptide if taken orally.

Recommended Dosing

Standard dosing recommendations for sermorelin include:

·         Typical dose: 0.2-0.3 mcg once daily

·         Administration timing: Preferably at bedtime to align with natural hormone production patterns

·         Reconstitution instructions: Inject diluent into the vial against the glass wall and swirl with gentle rotary motion until completely dissolved

·         Storage requirements: Refrigeration at temperatures between 36°F to 46°F (2°C to 8°C) to maintain potency^[8][6][4]

The evening administration schedule takes advantage of the body's natural circadian rhythm of growth hormone production, which typically peaks during early sleep phases.

Safety Profile and Adverse Effects

Understanding sermorelin's safety profile is essential for appropriate risk assessment and patient monitoring.

Common Side Effects

The most frequently reported adverse effects of sermorelin include:

·         Injection site reactions: pain, redness, swelling, itching, and irritation

·         Systemic effects: headaches, nausea, dizziness, and fatigue

·         Potential allergic reactions in sensitive individuals^[6][3]

Most of these effects are mild to moderate in severity and often diminish with continued treatment as the body adapts to the therapy.

Drug Interactions

Sermorelin may interact with several medications, potentially affecting either its efficacy or the action of concomitant drugs:

·         Thyroid medications (levothyroxine)

·         Cyclooxygenase inhibitors (aspirin)

·         Glucocorticoids (prednisone)

·         Insulin

·         Muscarinic antagonists (atropine)

·         Somatostatin-containing drugs or drugs that affect somatostatin (levodopa)^[3]

These potential interactions highlight the importance of comprehensive medication review before initiating sermorelin therapy and throughout the treatment course.

Special Considerations

Certain patient populations and conditions warrant particular attention when considering sermorelin:

·         Not appropriate for patients with active malignancy due to potential growth-promoting effects

·         Should be used with caution in patients with cardiovascular disease, diabetes, or thyroid disorders

·         May mask symptoms of hypothyroidism; thyroid function should be monitored during treatment

·         Potential for unwanted effects on glucose metabolism requires careful consideration in diabetic patients^[6]

Regular monitoring through laboratory testing and symptom tracking helps identify any developing concerns and allows for timely intervention when necessary.

Conclusion

Sermorelin represents an interesting approach to growth hormone modulation that works through stimulating the body's endogenous production rather than providing exogenous hormone replacement. As a synthetic 29-amino acid fragment of growth hormone-releasing hormone, it binds to specific receptors in the pituitary gland to promote natural growth hormone secretion in a pulsatile pattern.

Despite its previous FDA approval for treating growth hormone deficiency in children and for diagnostic evaluation of pituitary function, sermorelin is no longer available as an approved drug product in the United States. The manufacturer voluntarily withdrew it from the market in 2002, and its regulatory exclusivity expired in 2004. Currently, sermorelin can only be legally obtained through compounding pharmacies with a valid prescription from a licensed healthcare provider.

The compound's extremely short half-life of 11-12 minutes necessitates specific administration protocols, typically involving daily subcutaneous injections at bedtime to align with natural hormone production patterns. While generally well-tolerated, sermorelin may cause injection site reactions, headaches, nausea, and other side effects, and can interact with several common medications.

As research continues into growth hormone modulation and its effects on aging, metabolism, and physical performance, sermorelin remains a compound of interest for both clinical researchers and healthcare practitioners focused on hormonal optimization. However, its limited regulatory status and the emergence of newer growth hormone secretagogues present ongoing challenges to its widespread clinical application.

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1.       https://go.drugbank.com/drugs/DB00010     

2.      https://pubchem.ncbi.nlm.nih.gov/compound/sermorelin 

3.      https://www.chemicalbook.com/ChemicalProductProperty_EN_CB9474927.htm     

4.      https://www.rxlist.com/sermorelin-acetate-drug.htm    

5.       https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?tab=clinical&ligandId=6998  

6.      https://www.tryeden.com/post/is-sermorelin-fda-approved      

7.       https://www.accessdata.fda.gov/scripts/opdlisting/oopd/detailedIndex.cfm?cfgridkey=24687  

https://www.rupahealth.com/post/sermorelin-peptide-guide-for-practitioners-and-patients