MEDICAL DISCLAIMER: Educational research guidelines only. Lyophilized peptides are investigational chemical compounds and are NOT approved for human consumption, diagnosis, or therapy. Consult a licensed physician before any research application.
Epitalon Dosage Chart, Schedule & Reconstitution Protocol
Quickstart Highlights
Epitalon (also written Epithalon) is a synthetic tetrapeptide with the sequence Ala-Glu-Asp-Gly (AEDG), designed by Khavinson and Anisimov at the Saint Petersburg Institute of Bioregulation and Gerontology as a short peptide bioregulator of the pineal gland and a synthetic analogue of the natural polypeptide pineal extract Epithalamin. Mechanistically, Epitalon translocates into cell nuclei, binds regulatory regions of double-stranded DNA, and modulates pineal and peripheral gene transcription, including reported induction of telomerase activity in human somatic cells (PMID: 12937682). Long-term rodent studies from the Anisimov group reported reduced spontaneous tumor incidence, median lifespan extension, and normalization of circadian melatonin rhythms in female CBA mice (PMID: 14523189). Researchers study Epitalon for age-associated decline in melatonin output, immunosenescence, retinopathy, and as the central pineal-targeted tetrapeptide of Khavinson longevity protocols.
Reconstitute: Add 2 mL bacteriostatic water → 5 mg/mL concentration.
Easy measuring: At 5 mg/mL, 1 unit = 0.01 mL = 0.0500 mg (50 mcg) on a U-100 insulin syringe.
Storage: Lyophilized frozen; reconstituted refrigerated; avoid repeated freeze–thaw.
Half-life: The tetrapeptide is cleared from plasma within minutes; effects on circadian melatonin output and gene expression are reported to persist for months after a single ten-day pulsed course.
Route: Subcutaneous or intramuscular injection in research and Russian clinical use; intranasal use appears anecdotally but lacks validated pharmacokinetic data.
Status: Khavinson-licensed research peptide; not FDA, EMA, or MHRA approved. The parent natural extract Epithalamin was used clinically in Russia, but synthetic Epitalon remains investigational outside the Russian Federation.
Quick Protocol Navigation
Reconstitution Instruction & Mixing Step-by-Step
Lyophilized powder must be reconstituted carefully. Agitating peptide chains can shear disulfide bonds and render the peptide biologically inert.
Draw 2.0 mL bacteriostatic water with a sterile syringe.
Inject slowly down the vial wall; avoid foaming.
Gently swirl/roll until dissolved (do not shake).
Inject slowly; wait a few seconds before withdrawing the needle.
Do not aspirate for subcutaneous injections; inject slowly and steadily[10].
Interactive Epitalon Syringe Calculator
Currently visualizing the Epithalon) (10 mg vial reconstituted with 2 mL bacteriostatic water. Adjust the target dose to dynamically render syringe units.
Reconstitution Calculation: 10mg dry powder in 2mL water yields 5.00 mg/mL. To evaluate a 250mcg dose, pull to 5.0 units (5 syringe ticks).
U-100 Syringe Representation
5.0 Units (5 Ticks)
Educational reference visual. Assumes standard U-100 insulin syringe where 1.0 mL volume = 100 units.
Titration & Dose Escalation Schedules
| Phase | Daily Dose (mcg) | Units (per injection) (mL) |
|---|---|---|
| Days 1–20 (Cycle On) | 5,000 mcg (5 mg) | 100 units (1.00 mL) |
| Weeks 4–26 (Cycle Off) | 0 mcg | — |
Administration guidelines: Refer to guidelines | 2 mL Reconstitution
Research Supplies Quantity Planner
Scientific mathematical planning of syringes, bacteriostatic water and dry vials needed for extended research blocks using the Epithalon) (10 mg vial.
Peptide Vials (Epitalon, 10 mg each):
- check20-day cycle (5 mg/day): 10 vials (each vial yields 2 doses)
Insulin Syringes (U-100):
- checkPer cycle: 20 syringes (1/day)
Bacteriostatic Water (10 mL bottles): Use 2.0 mL per vial for reconstitution.
- check20-day cycle (10 vials): 20 mL → 2 × 10 mL bottles
Alcohol Swabs: One for the vial stopper + one for the injection site each day.
- checkPer cycle: 40 swabs (2/day) → recommend 1 × 100-count box
Mechanism of Action (MOA)
Epitalon (Ala-Glu-Asp-Gly, AEDG) was developed by Khavinson and Morozov by analyzing the predominant amino acid composition of Epithalamin, the bovine pineal gland extract used in Russian clinical practice since the 1970s for neuroendocrine and age-related disorders. AEDG emerged as the shortest active peptide sequence reproducing many of Epithalamin's effects, allowing development of a defined synthetic analog suitable for industrial production and controlled investigation. Mechanistically, Epitalon operates through multiple convergent pathways. The most-cited effect is telomerase activation: Khavinson and Bondarev demonstrated in human fetal fibroblast cultures and pulmonary cell lines that Epitalon induces telomerase enzyme activity and produces measurable telomere elongation across multiple passages, an effect not produced by control peptides [3]. This was the first evidence that a short synthetic peptide could activate telomerase in human somatic cells outside germ-line and cancer contexts. A 2025 study extended this finding showing Epitalon increases telomere length in human cell lines through telomerase upregulation or alternative lengthening of telomeres (ALT) activity [7]. Beyond telomerase, Epitalon supports pineal function by restoring melatonin synthesis and circadian rhythm in aged animals and humans; Anisimov, Khavinson, and colleagues showed that elderly patients treated with Epitalon recover physiologic nocturnal melatonin secretion and improved sleep architecture. Animal studies demonstrate broad anti-aging effects: Anisimov et al. reported 12–13% extension of mean lifespan in female CBA mice receiving cyclic Epitalon administration, with reduced spontaneous tumor incidence and improved immune markers [4]. Khavinson and colleagues documented 11–16% lifespan extension in Drosophila melanogaster, supporting evolutionary conservation of the bioregulator effect [5]. In rodents Epitalon also normalized circadian melatonin profiles, reduced age-related elevation of cortisol, and improved performance on cognitive tests in old animals. Mechanistically, Epitalon is hypothesized — consistent with the broader Khavinson model — to penetrate cell and nuclear membranes and bind specific DNA sequences in promoter regions, modulating chromatin condensation and gene expression in a tissue-specific manner. Telomerase reverse transcriptase (TERT) is among the target genes upregulated; pineal-specific enzymes including hydroxyindole-O-methyltransferase and arylalkylamine-N-acetyltransferase are also upregulated, providing a molecular basis for restored melatonin synthesis. Pharmacokinetically, Epitalon has a very short plasma half-life (under 5 minutes when given subcutaneously), but biological effects on gene expression and telomere length persist for weeks to months after a treatment course, consistent with epigenetic rather than receptor-occupancy mechanism. Standard research and clinical protocols use 5–10 mg subcutaneously per day for 10–20 consecutive days, repeated 2–3 times per year. Higher cumulative-dose schedules (20 mg/day) have been investigated; longer continuous courses (more than 30 days) are uncommon in published practice. Intranasal and oral delivery have been used; oral bioavailability is poor but the cumulative bioregulator effect appears even with parenteral microgram-to-low-milligram dosing. Western mechanistic validation by ChIP-seq, ATAC-seq, and controlled human pharmacodynamic studies remains absent, and translation to human anti-aging therapy is not yet evidence-based.
Clinical Trial Efficacy Highlights
- starKhavinson and Bondarev demonstrated in human fetal somatic cell cultures that Epitalon induces telomerase enzyme activity and produces measurable telomere elongation across multiple cell passages, evidence not seen with control peptides [3].
- starA 2025 PMC study showed Epitalon increases telomere length in human cell lines through telomerase upregulation or alternative lengthening of telomeres (ALT) activity, with effects persisting over multiple passages [7].
- starAnisimov and colleagues reported that female CBA mice receiving cyclic Epitalon administration (5–6 month courses of 1 mcg subcutaneously, three times weekly) showed 12–13% extension of mean lifespan, reduced spontaneous tumor incidence, and improved immune markers compared to controls [4].
- starKhavinson and colleagues documented 11–16% lifespan extension in Drosophila melanogaster fed Epitalon-containing nutrient medium, supporting evolutionary conservation of the bioregulator effect across taxa [5].
- starRussian clinical observational studies of elderly patients treated with cyclic Epitalon report restoration of nocturnal melatonin secretion, improved sleep architecture on polysomnography, and normalization of cortisol diurnal patterns.
- starKorkushko, Khavinson, and Shatilo reported in a 6-year observational follow-up that elderly patients receiving cyclic Epitalon (in combination with Thymalin) showed reduced all-cause mortality compared to age-matched controls, though the study was not randomized [8].
- starEpitalon reduced the incidence of age-related chromosome abnormalities (micronucleus formation, aneuploidy) in peripheral lymphocytes from elderly subjects and increased markers of immune cell competence on flow cytometry.
- starAnisimov, Khavinson and colleagues reported that Epitalon administration to female rats reduced the development of mammary tumors and prolonged tumor-free survival in carcinogen-exposed cohorts, supporting cancer-protective rather than cancer-promoting activity despite telomerase activation [9].
Side Effects & Tolerability Profile
Clinical subjects transiently report mild side effects. Slowly escalating the titration dose represents the single most effective intervention to limit side effects.
- warningEpitalon is generally well tolerated in Russian clinical and observational use; reported adverse effects are infrequent and mild.
- warningThe most common reported effect is transient injection-site discomfort with subcutaneous administration, resolving spontaneously.
- warningOccasional reports of mild fatigue or sleep disturbance during early dosing have been described, possibly reflecting changes in circadian melatonin patterns as the peptide normalizes pineal function.
- warningMild headache has been reported in a minority of users, generally at higher doses, and typically resolves on dose adjustment.
- warningTheoretical concerns about telomerase activation and oncogenic potential have not been borne out in published rodent or human data; Anisimov's studies actually show reduced spontaneous and induced tumor incidence in Epitalon-treated cohorts.
- warningNo tolerance, dependence, or withdrawal phenomena have been documented in chronic dosing protocols.
- warningHypersensitivity reactions are rare; allergic skin reactions to peptide preparations should prompt discontinuation.
- warningReproductive, pregnancy, and lactation safety data are absent; Epitalon use is not recommended during these periods given its hormonal and neuroendocrine modulating activity.
Subcutaneous Injection Technique
Most research peptides require subcutaneous injection into fatty tissue. Never inject directly into a blood vessel or deep muscle tissue unless clinically detailed.
1. Site Selection
Common locations include the abdomen (2 inches from navel), outer upper arms, or thighs.
2. Sanitization
Thoroughly clean the selected site, stopper and vial top using 70% isopropyl alcohol prep swabs.
3. Angle & Push
Pinch the skin and insert the needle at a 45 to 90-degree angle. Depress plunger smoothly.
4. Site Rotation
Rotate injection sites continuously to avoid lipodystrophy or tissue scarring.
Frequently Asked Questions
What is the typical Epitalon dosage?expand_more
Standard research and Russian clinical protocols use 5–10 mg subcutaneously per day for 10–20 consecutive days, repeated 2–3 times per year. Lower-dose protocols use 100–500 mcg/day; higher cumulative-dose schedules (20 mg/day) have been investigated. Continuous dosing beyond 30 days is uncommon.
How is Epitalon administered?expand_more
Epitalon is most commonly administered subcutaneously as a reconstituted lyophilized peptide. Intramuscular and intranasal delivery have been investigated. Oral capsule formulations are sold but have lower expected bioavailability; subcutaneous dosing remains the research and clinical standard.
Can Epitalon be stacked?expand_more
Epitalon is frequently combined with other Khavinson bioregulators (Thymalin, Pinealon, Cortagen) in Russian gerontology protocols. The classic Khavinson-Korkushko combination is Epitalon plus Thymalin for systemic neuroendocrine and immune rejuvenation. Western controlled-trial validation is absent.
What are the side effects of Epitalon?expand_more
Reported side effects are mild and infrequent: occasional injection-site discomfort, transient fatigue or sleep changes during dose initiation, and rare mild headache. No telomerase-related oncogenicity has been documented; in fact, Anisimov reported reduced tumor incidence in treated rodents.
Is Epitalon FDA approved?expand_more
No. Epitalon is registered in Russia under peptide-bioregulator legislation but is not approved by the FDA, EMA, or MHRA. In the United States and European Union it is sold only as a research chemical and is not licensed for human therapeutic use or for any anti-aging indication.
Academic References & Study Citations
Khavinson VK, Bondarev IE, Butyugov AA. Epithalon peptide induces telomerase activity and telomere elongation in human somatic cells. Bull Exp Biol Med. 2003;135(6):590-2. View Scientific Paper →
Khavinson VK. Peptides and ageing. Neuroendocrinol Lett. 2002;23 Suppl 3:11-144. View Scientific Paper →
Khavinson VK, Bondarev IE, Butyugov AA, Smirnova TD. Peptide promotes overcoming of the division limit in human somatic cell. Bull Exp Biol Med. 2004;137(5):503-6. View Scientific Paper →
Anisimov VN, Khavinson VK, Provinciali M, et al. Inhibitory effect of the peptide epitalon on the development of spontaneous mammary tumors in HER-2/neu transgenic mice. Int J Cancer. 2002;101(1):7-10. View Scientific Paper →
Khavinson VK, Izmaylov DM, Obukhova LK, Malinin VV. Effect of epitalon on the lifespan increase in Drosophila melanogaster. Mech Ageing Dev. 2000;120(1-3):141-9. View Scientific Paper →
Anisimov VN, Khavinson VK, Popovich IG, Zabezhinski MA. Inhibitory effect of peptide Epitalon on colon carcinogenesis induced by 1,2-dimethylhydrazine in rats. Cancer Lett. 2002;183(1):1-8. View Scientific Paper →
Epitalon increases telomere length in human cell lines through telomerase upregulation or ALT activity. PMC. 2025. View Scientific Paper →
Korkushko OV, Khavinson VK, Shatilo VB, Antonyk-Sheglova IA. Peptide geroprotector from the pituitary gland inhibits rapid aging of elderly people: results of 15-year follow-up. Bull Exp Biol Med. 2011;151(3):366-9. View Scientific Paper →
Anisimov VN, Khavinson VK. Peptide bioregulation of aging: results and prospects. Biogerontology. 2010;11(2):139-49. View Scientific Paper →
Khavinson VK, Pendina AA, Efimova OA, et al. Effect of peptide AEDG on telomere length and mitotic index of PHA-stimulated human blood lymphocytes. Bull Exp Biol Med. 2019;168(1):141-144. View Scientific Paper →