Epithalon

Overview

Epithalon is a synthetic tetrapeptide based on the natural peptide epithalamin, extracted from the pineal gland. Developed by Russian scientist Vladimir Khavinson, it has been studied for decades for its potential anti-aging and neuroprotective properties.

The peptide's primary mechanism—telomerase activation—addresses one of the fundamental aspects of cellular aging, making it one of the most studied anti-aging peptides.

Sequence: Ala-Glu-Asp-Gly (AEDG)

Mechanism of Action

Epithalon's mechanisms center on telomere biology and beyond:

Telomerase Activation

• Activates telomerase enzyme (hTERT)
• Extends telomere length in somatic cells
• Delays cellular senescence
• Restores proliferative capacity

Pineal Gland Function

• Stimulates melatonin production
• Regulates circadian rhythms
• Restores age-related pineal decline
• Supports sleep-wake cycles

Neuroprotection

• Protects neurons from oxidative stress
• Supports mitochondrial function
• May protect against age-related cognitive decline
• Antioxidant properties

Gene Expression

• Modulates expression of aging-related genes
• Influences DNA repair mechanisms
• Affects cell cycle regulation
• Epigenetic effects suggested

Research Summary

Telomere Studies

In Vitro

• Activated telomerase in human somatic cells
• Extended replicative lifespan of fibroblasts
• Increased telomere length in cell cultures
• Overcame Hayflick limit in some studies

Animal Studies

• Extended lifespan in rodent models
• Delayed age-related tissue changes
• Improved markers of biological aging

Longevity Studies

Cognitive and Neuroprotective

Age-Related Cognitive Decline

• Improved memory in aged animals
• Protected against neurodegeneration markers
• Maintained cognitive function with aging
• Enhanced neuroplasticity markers

Mechanisms

• Antioxidant effects in brain tissue
• Mitochondrial protection
• Melatonin-mediated neuroprotection
• Potential telomere protection in neurons

Clinical Experience (Russia)

Epithalon and its precursor epithalamin have been used clinically in Russia:

• Elderly patients with various conditions
• Reported improvements in physiological markers
• Used in gerontological protocols
• Combined with other geroprotectors

Key Limitations

• Limited Western clinical trials
• Most human data from Russian studies
• Long-term safety not fully established
• Optimal protocols not standardized
• Cancer considerations (telomerase in cancer cells)

Pharmacokinetics

Common Protocols

Note: Epithalon is a research compound. The following represents research community protocols.

Research Community Protocols

Typical Dosing Ranges:

• 5-10 mg daily, subcutaneous
• Total cycle: 50-100 mg
• Duration: 10-20 day cycles
• Frequency: 1-2 cycles per year

Cycle Structure:

• 10 days: 10 mg daily
• Or 20 days: 5 mg daily
• Rest period: 4-6 months between cycles

Administration

Subcutaneous (Primary)

• Most common route
• Injected in abdominal area
• Rotate injection sites
• Once daily, usually evening

Timing

• Evening administration often preferred
• Aligns with melatonin rhythm
• Some prefer morning

Reconstitution

• Supplied as lyophilized powder
• Reconstitute with bacteriostatic water
• Typical: 10 mg in 1-2 mL
• Store at 2-8°C

Side Effects

Commonly Reported

• Injection site reactions (mild)
• Fatigue (temporary, some reports)
• Vivid dreams (melatonin effect)
• Sleep changes (usually improvement)

Generally Well-Tolerated

• Long history of use in Russian research
• No significant adverse events in studies
• No hormonal disruption reported
• No dependence or withdrawal

Theoretical Concerns

Cancer Considerations

• Telomerase is active in cancer cells
• Theoretical concern about promoting existing cancers
• No evidence of carcinogenesis in available data
• Contraindicated with active malignancy

Interactions

Potential Interactions

• Melatonin (additive effects)
• Other geroprotectors (unknown interactions)
• Cancer treatments (contraindicated)

Contraindications

• Active cancer or history of cancer
• Pregnancy/nursing
• Autoimmune conditions (theoretical)
• Under 40 years (generally not indicated)

Community Insights

Aggregated from research community reports.

Commonly Reported Experiences

• Improved sleep quality
• Better energy levels
• Enhanced recovery
• Improved skin quality over time
• Subtle but cumulative effects
• Better sense of wellbeing

Practical Tips

• Run cycles rather than continuous use
• Evening dosing for sleep benefits
• Effects are long-term, not acute
• Consider once or twice yearly cycles
• Quality sourcing critical

Common Stacks

• Epithalon + GHK-Cu (anti-aging)
• Epithalon + BPC-157 (recovery/healing)
• Part of comprehensive longevity protocols

Expectations

• Not an immediate effect compound
• Benefits accumulate over time
• Aimed at long-term health optimization
• Subtle improvements in vitality

Who Uses It

• Adults 40+ interested in longevity
• Those focused on preventive health
• Part of biomarker-driven optimization
• Aging research enthusiasts

References

1. Khavinson VK, et al. Peptide regulation of gene expression: 20 years of research. Bull Exp Biol Med. 2006;141(3):380-6.

2. Anisimov VN, et al. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology. 2003;4(4):193-202.

3. Khavinson VK, et al. Epithalon peptide induces telomerase activity and telomere elongation in human somatic cells. Bull Exp Biol Med. 2003;135(6):590-2.

4. Goncharova ND, et al. Pineal peptides restore the age-related disturbances in hormonal functions of the pineal gland and the pancreas. Exp Gerontol. 2005;40(1-2):51-7.

5. Khavinson VK, Morozov VG. Peptides of pineal gland and thymus prolong human life. Neuro Endocrinol Lett. 2003;24(3-4):233-40.

6. Anisimov VN, et al. Epithalamin decelerates aging and the development of age-related diseases in rodents: Results of a 30-year study. Adv Gerontol. 2010;23(4):551-66.