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High-resolution image of a small transparent glass vial labeled "Epitalon 10 mg, Batch No.004, 28-06-2025", containing a white powder and sealed with a gray cap, displayed against a neutral background
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Epitalon 10mg vial

Epitalon 10mg vial

€25,00 EUR
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                                            NOT FOR HUMAN CONSUMPTION

Epitalon (Ala–Glu–Asp–Gly; AGAG) is a short tetrapeptide derived from the bovine-pineal extract “epithalamin,” developed by the St. Petersburg/Khavinson group. It’s marketed as a “geroprotective” peptide with proposed actions on telomerase activation, chromatin remodeling, circadian signaling, and stress-response pathways. It is not FDA/EMA-approved; human evidence consists mostly of small, regionally published trials and observational series.

Additional Benefits of Epitalon Now Under Investigation

Benefit Key take-aways
1 Telomerase / telomere dynamics In cell/animal studies, Epitalon up-regulates TERT and slows telomere attrition; limited human data report telomere length stabilization over months—methodology and durability remain debated.
2 Circadian & melatonin signaling Reported night-time melatonin increases, improved sleep quality, and seasonal rhythm normalization in older adults, consistent with pineal-axis modulation.
3 Immune function in aging Observational programs note higher T-cell counts and reduced respiratory infectionincidence in elderly cohorts receiving cyclic courses; controlled, blinded evidence is sparse.
4 Antioxidant / stress-response In models, peptide reduces lipid peroxidation, normalizes SOD/GPx, and modulates NF-κB/Nrf2 signalling; human biomarker data are small and heterogeneous.
5 Metabolic markers Signals for modest glycaemic and lipid improvements (↓ fasting glucose, TG) in some aging cohorts; confounded by concurrent lifestyle changes.
6 Ocular/retinal support Small studies suggest improved retinal electrophysiology and function in age-related ocular changes; needs replication with modern endpoints.
7 Reproductive/endocrine aging Limited data hint at gonadotropic and thyroid tone normalization in elderly; clinical relevance uncertain.
8 Onco-gerontology signal (prophylactic) Long follow-ups from Russian registries propose lower cancer incidence/mortality with multi-year peptide programs; absence of randomized, blinded designs limits inference.
9 Physical function & QoL Reports of improved exercise tolerance, sleep, and self-rated health in older adults on cyclic therapy; placebo-controlled confirmation is lacking.

2. Molecular Mechanism of Action

2.1 Proposed pharmacodynamics

  • Telomerase/epigenetic: Enhances TERT expression and may influence heterochromatin maintenance at telomeric/subtelomeric regions.

  • Pineal/circadian: Modulates melatonin synthesis and clock-gene output (e.g., BMAL1/Per axes), supporting sleep–wake regulation.

  • Stress/inflammation: Down-shifts NF-κB, supports Nrf2 antioxidant responses, improves mitochondrial redoxmetrics in models.

2.2 Down-stream biology

Pathway Functional outcome Context
TERT/telomere maintenance ↓ Replicative senescence markers In vitro, animal
Clock genes / melatonin Sleep consolidation, circadian alignment Older adults (signals)
Nrf2–ARE / antioxidant enzymes ↓ ROS, lipid peroxidation Liver, heart, brain (models)
NF-κB restraint ↓ Pro-inflammatory cytokines Immunosenescence
Mitochondrial function ↑ Membrane potential, ↓ mtROS Neurons/myocytes (models)

3. Pharmacokinetics

  • Route: Reported SC/IM injections (common in publications), intranasal, and occasional oral/sublingual use; no standardized formulation.

  • Absorption/half-life: Very short plasma t½ for the tetrapeptide (minutes–hours); hypothesized epigenetic/circadian effects may outlast exposure.

  • Distribution/clearance: Rapid tissue uptake and renal peptidase clearance expected; human PK is not well characterized.

4. Pre-clinical and Translational Evidence

4.1 Cellular/animal

  • In vitro: TERT up-regulation, telomere preservation, improved chromosomal stability, reduced β-gal senescence staining.

  • In vivo (rodents): Improved survival curves in some strains, antioxidant enzyme normalization, tumor latencyshifts in specific models, and circadian improvements.

4.2 Human studies

  • Small, mostly open-label or regionally randomized trials report improved melatonin profiles, sleep, immune markers, and some metabolic indices; multi-year observational data suggest mortality reduction when combined with other “cytomedins,” but methodology limits causal claims.

Evidence quality note: Most human data are low–moderate quality, with limited blinded, placebo-controlled trials and variable assay rigor for telomeres and hormones.

5. Emerging Clinical Interests

Field Rationale Status
Insomnia/circadian disruption in aging Pineal–clock modulation Pilot trials
Immunosenescence/influenza risk T-cell support, inflammatory tone Observational
Metabolic syndrome in elderly Redox + circadian effects Exploratory
Neurodegeneration (supportive) Mitochondrial redox & sleep consolidation Preclinical → pilot
Onco-prevention (hypothesis) Telomere/homeostasis Observational only

6. Safety and Tolerability

  • Common: Injection-site discomfort, transient fatigue or alertness changes (timing-dependent), headache, mild GI upset with oral forms.

  • Endocrine: Possible melatonin-related daytime sleepiness if dosed late morning; rare vivid dreams.

  • Immunologic: No strong signals of immunosuppression; long-term immune stimulation vs regulation remains uncertain.

  • Oncology: Theoretical concern that telomerase activation might promote neoplastic cell persistence; animal data are mixed. Avoid in active cancer outside studies.

  • Drug interactions: Caution with sedatives (sleep synergy) and agents affecting circadian timing; minimal CYP interplay expected.

  • Special populations: Insufficient data in pregnancy, autoimmune disease, or active malignancy—avoid outside IRB protocols.

Comparative safety matrix

Concern Epitalon Melatonin Metformin (aging context)
Main action Telomerase/circadian/anti-inflammatory (proposed) Pineal hormone; circadian AMPK/mitochondrial; metabolic
Evidence in aging outcomes Low–moderate (regional) Moderate for sleep; limited for aging Mixed for aging; strong metabolic
Daytime sedation Low–moderate (timing-dependent) Possible Low
Oncologic theory Telomerase concern Neutral Mixed/neutral

7. Regulatory Landscape

  • Not approved by FDA/EMA for any indication.

  • Available via research-chemical vendors or compounding in some locales; quality varies.

  • Use should remain within research/IRB-guided settings; marketing claims of “anti-aging cure” are not evidence-based.

8. Practical Use & Future Directions

  • If studied (research context): Consider cyclic courses (e.g., 10–20 days per quarter) aligned to sleep schedule(evening dosing) and track sleep metrics, inflammatory markers, and (if relevant) telomere assays with consistent methodology.

  • Lifestyle stack: Prioritize sleep hygiene, daytime light, exercise, protein sufficiency, and metabolic health—these have stronger, proven effects on longevity markers.

  • Trials needed:

    • Multicenter, randomized, double-blind trials with actigraphy, melatonin profiles, immune panels, and clinical endpoints.

    • Standardized PK/PD and bioanalytical validation for telomerase/telomere outcomes.

    • Long-term safety focused on oncology and immune balance.

Selected References

  • Aging-related peptide literature from the St. Petersburg Institute (epithalamin/Epitalon): telomerase/telomere, circadian, and immune observations.

  • Redox Biology; Free Radical Biology & Medicine — Antioxidant and NF-κB/Nrf2 signaling under peptide geroprotectors (preclinical).

  • Chronobiology International; Sleep Medicine — Melatonin/circadian endpoints in older adults (context for pineal-axis modulation).

  • Immunity; Frontiers in Immunology — Immunosenescence frameworks relevant to peptide-mediated immune tuning.

  • Oncogene; Cancer Research — Telomerase biology and theoretical oncologic implications of telomerase activation.