Considered to be one of the most protective estrogen metabolites, 2-MeOH E2 is also produced endogenously in small amounts. It is showing promise in a number of animal and human trials as an adjunctive treatment for several types of cancer. Current scientific understanding suggests it does not bind to estrogen receptors.
The biomarker 2-Methoxy-E2 is part of the phase 2 metabolism.
2-Methoxy estrogens is produced from 2-OH estrogens through the COMT enzyme. Anti-cancerogenic effects have been ascribed to 2-OH estrogensand particularly 2-Methoxy estrogens.
2-Methoxy-estrogen has shown antiproliferative effects in both hormone-dependent and hormone-independent breast cancer cells. These studies have shown that urinary 2-Methoxy estrogen levels were lower in breast cancer patients than controls.
Phase 2 metabolism (methylation):
After estrogens go through phase 1 detoxification, they move on to methylation which is part of phase 2 detoxification. Methylation, in essence, “neutralizes” the phase 1 metabolites and prepares them to be excreted out of the body instead of shuttling them back into circulation. Only 2-OH and 4-OH estrogens are methylated. 16-OH-E1 is not.
2-MeO Estradiol
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