Epithalon: Safety Profile & Research Summary
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Preclinical Research Summary
Key Preclinical Studies
| Study | Model | Key Findings | Ref |
|---|---|---|---|
| Anisimov/Popovich et al. (2003) | SHR mice — 1 µg/mouse SC × 5d/month from 3 mo | Last 10% lifespan increased 13.3%; chromosomal aberrations ↓17.1%; leukemia inhibited 6-fold | [7] |
| Anisimov et al. (2002) | HER-2/neu transgenic mice — 1 µg/mouse SC monthly | HER-2/neu mRNA reduced 3.7-fold; breast adenocarcinoma incidence significantly reduced | [14] |
| Kossoy et al. (2006) | C3H/He mice — 0.1 µg/mouse SC × 5x/wk × 6.5 mo | Reduced tumor metastasis and multiplicity | [8] |
| Anisimov et al. (2001) | CBA mice — 0.1 µg/mouse SC monthly | Oldest treated mouse lived 34 months vs 24 mo control; mice reaching 23 mo increased 4-fold | [4] |
| Khavinson et al. (2002–03) | Campbell rats — 1 µg/rat parabulbar injection | Retinal function prolonged 43.9%; 90% of retinal layers preserved at day 41 vs complete destruction | [9] |
| Zamorskii et al. (2015) | Rats — cisplatin-induced acute renal failure | AEDG normalized diuresis, urinary creatinine and its excretion, GFR, and sodium resorption; reduced urinary protein | [13] |
| Goncharova et al. (2001–05) | Old female rhesus monkeys — 10 µg/kg IM | Restored nighttime melatonin synthesis; normalized cortisol circadian rhythm; improved glucose tolerance | [11] |
| Khavinson et al. (2000–01) | Drosophila — 0.00001–0.001% in medium | Mean lifespan +11–16%, max +14%; mortality ↓52%; SOD +41%, catalase +20% | [6] |
| Ullah et al. (2025) | Bovine oocytes in vitro | Activated telomerase; improved blastocyst hatching; reduced ROS | [10] |
Clinical / Human Studies
| Trial | Population | Intervention | Key Results | Ref |
|---|---|---|---|---|
| Retinal Degeneration | Patients with degenerative retinal lesions (n not stated in source abstract) | Not specified in source abstract | Authors report a positive clinical effect in 90% of cases; companion Campbell-rat arm showed preserved retinal morphology and bioelectric activity | [9] |
| Circadian Gene Expression | Adults with reduced melatonin-producing pineal function | Not specified in source abstract | Urinary 6-sulfatoxymelatonin excretion ↑1.7×; Clock and Csnk1e hyperexpression normalized 1.9–2.1×; Cry2 hypoexpression ↑2× | [15] |
| Telomere Elongation (in vitro) | Human fetal fibroblast culture — not human subjects | Peptide added to culture medium | Induced telomerase catalytic subunit expression and telomere elongation; treated cultures reached 44 passages vs 34 in control | [5][18] |
| Genome Instability in Pulmonary TB (ex vivo) | Mitogen-stimulated cell cultures from TB patients — peptide applied to cultures, not administered to patients | Peptide added to short-term culture | Reduced mean frequency of aberrant cells on the chromosome-aberration test; elevated chromosome fragility persisted | [16] |
Safety Summary
| Parameter | Finding |
|---|---|
| Long-term Animal Studies | No toxicity in mice/rats from 3 months of age until natural death; reduced mortality and spontaneous tumors |
| Human Studies | The published human reports cited here are small, largely single-centre, and do not report severe adverse events; they are not adequate to characterize a safety profile |
| Cancer Risk Paradox | Despite telomerase activation, animal studies consistently show ANTI-tumor and anti-metastatic effects |
| Degradation | N-terminal glutamic acid can cyclize to pyroglutamate; TFA salt affects net peptide content |
| Routes Studied | Subcutaneous, intramuscular, parabulbar (eye), sublingual, oral, intranasal |
In Vitro / Preclinical Disclaimer: The research findings described above were observed in laboratory (in vitro) and/or animal model studies. These results may not translate to human outcomes. No claims are made regarding human therapeutic applications.
Educational Use Only: This content is provided for informational and educational purposes only. It is not intended as medical advice and should not be used to diagnose, treat, cure, or prevent any disease or medical condition. Always consult qualified healthcare professionals for medical decisions.
Editorial Research Note
“Preclinical Research Summary Key Preclinical Studies StudyModelKey FindingsRef Anisimov/Popovich et al.”
References
- Al-Dulaimi S, Thomas R, Matta S, Roberts T. Epitalon increases telomere length in human cell lines through telomerase upregulation or ALT activity. Biogerontology. 2025;26(5):178.
- Araj SK, Brzezik J, Mądra-Gackowska K, Szeleszczuk Ł. Overview of Epitalon—Highly Bioactive Pineal Tetrapeptide with Promising Properties. Int J Mol Sci. 2025;26(6):2691.
- Khavinson V, Diomede F, Mironova E, et al. AEDG Peptide (Epitalon) Stimulates Gene Expression and Protein Synthesis during Neurogenesis: Possible Epigenetic Mechanism. Molecules. 2020;25(3):609.
- Anisimov VN, Khavinson VK. Peptide bioregulation of aging: results and prospects. Biogerontology. 2010;11(2):139-149.
- 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):590-592.
- Khavinson VK, Izmaylov DM, Obukhova LK, Malinin VV. Effect of epitalon on the lifespan increase in Drosophila melanogaster. Mech Ageing Dev. 2000;120(1):141-149.
- Anisimov VN, Khavinson VK, Popovich IG, 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.
- Kossoy G, Anisimov VN, Ben-Hur H, et al. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H/He mice. In Vivo. 2006;20(2):253-257.
- Khavinson V, Razumovsky M, Trofimova S, et al. Pineal-regulating tetrapeptide epitalon improves eye retina condition in retinitis pigmentosa. Neuro Endocrinol Lett. 2002;23(4):365-368.
- Ullah S, Haider Z, Perera CD, et al. Epitalon-activated telomerase enhance bovine oocyte maturation rate and post-thawed embryo development. Life Sciences. 2025;362:123381.
- Goncharova ND, Khavinson BK, Lapin BA. Regulatory Effect of Epithalon on Production of Melatonin and Cortisol in Old Monkeys. Bull Exp Biol Med. 2001;131(4):394-396.
- Gatta M, Dovizio M, Milillo C, et al. The Antioxidant Tetrapeptide Epitalon Enhances Delayed Wound Healing in an in Vitro Model of Diabetic Retinopathy. Stem Cell Rev Rep. 2025;21(6):1822-1834.
- Zamorskii II, Shchudrova TS, Lin'kova NS, Nichik TE, Khavinson VK. Peptides Restore Functional State of the Kidneys During Cisplatin-Induced Acute Renal Failure. Bull Exp Biol Med. 2015;159(6):736-739.
- Anisimov VN, Khavinson VK, Alimova IN, et al. Epithalon Decelerates Aging and Suppresses Development of Breast Adenocarcinomas in Transgenic HER-2/neu Mice. Bull Exp Biol Med. 2002;134(2):187-190.
- Ivko OM, Linkova NS, Ilina AR, Sharova AA, Ryzhak GA. AEDG peptide regulates human circadian rhythms genes expression during pineal gland accelerated aging. Adv Gerontol. 2020;33(3):429-435.
- Dzhokhadze TA, Buadze TZh, Rubanov KD, Kiriia NA, Lezhava TA. Genome instability in pulmonary tuberculosis before and after treatment. Georgian Med News. 2013;(224):77-81.
- Anisimov VN, Khavinson VK, Popovich IG, Zabezhinski MA. Inhibitory effect of peptide Epitalon on colon carcinogenesis induced by 1,2-dimethylhydrazine in rats. Cancer Letters. 2002;183(1):1-8.
- 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):503-506.
- Kozina LS, et al. Effects of vilon and epithalon peptides on neprilysin and insulin-degrading enzyme in neuroblastoma NB7 cells. Neurochem J. 2008;2(1):69-71.
- Yue X, Liu SL, Guo JN, et al. Epitalon protects against post-ovulatory aging-related damage of mouse oocytes in vitro. Aging (Albany NY). 2022;14(7):3191-3202.
- Khavinson VK, Lezhava TA, Monaselidze JR, et al. Peptide Epitalon activates chromatin at the old age. Neuro Endocrinol Lett. 2003;24(5):329-333.
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