EPITHALON (ALA-GLU-ASP-GLY)

Mechanism of Action
Epithalon (also known as Epitalon or Epithalone) is a synthetic tetrapeptide derived from extracts of the pineal gland and identified as the active component of the natural extract known as epithalamin. Its primary mechanism of action is activation of the enzyme telomerase, which promotes telomere elongation in human somatic cells. In cellular studies, Epithalon extended the lifespan of human fibroblasts beyond the Hayflick limit by lengthening their telomeres.
In addition, Epithalon modulates gene expression associated with aging. For example, it has been shown to restore melatonin secretion by the pineal gland in aging organisms, normalizing circadian rhythms in primates and elderly humans. It has also been attributed antioxidant and oncostatic properties (reduction of tumor formation) in animal models, possibly linked to decreased oxidative damage and regulation of aging-related gene expression.
 
Clinical Uses
Epithalon has been proposed as a geroprotective (anti-aging) therapy aimed at extending healthy lifespan. Although it is not an approved drug in most countries, its potential to improve aging biomarkers and prevent age-related diseases has been investigated. Pilot human studies suggest possible benefits: for instance, in older adults (60–80 years), Epithalon (and its precursor epithalamin) significantly increased telomere length in blood cells, which may correlate with slower biological aging.
It has also been studied in specific disorders; a clinical trial in patients with retinitis pigmentosa reported clinical improvement in approximately 90% of cases treated with Epithalon. Additionally, long-term Russian studies using similar pineal extracts (epithalamin) reported reduced mortality among elderly individuals treated over several years. These applications remain experimental and require independent confirmation.
 
Side Effects and Risks
Available data indicate that Epithalon is generally well tolerated at moderate doses. In two clinical trials lasting three years involving epithalamin (a related crude pineal extract), no serious adverse events were reported in treated older adults. Preclinical studies have not described cumulative toxicity, suggesting a favorable safety profile.
Possible mild side effects include injection-site irritation or redness and transient sleep disturbances (based on anecdotal reports). However, formal safety research is limited: large, controlled clinical trials have not been conducted to rule out rare or long-term adverse effects. Regulatory agencies (e.g., the FDA) have not approved its use and emphasize the need for more robust evidence before widespread application.