Femarelle (DT56a) was a botanical drug candidate that failed regulatory review in Europe as treatment of menopause and to promote bone health. Its active ingredient was 322 mg DT56a (a tofu extract) and 108 mg flaxseed powder, which acted as a selective estrogen receptor modulator (SERM)
Mode of action
In animal models, Femarelle exerts agonistic (stimulatory) activity on estrogen receptors in the brain and bone. The compound has been reported to alleviate menopausal symptoms such as hot flushes and elevate bone mineral density (BMD), while having no proliferative effects on isolated breast cancer cell lines and uterine  tissues of rats. Femarelle was found to regenerate the bone through increased osteoblast activity, which makes it a possible agent for postmenopausal bone loss. Although stimulating estrogen receptors, Femarelle does not appear to change the hormonal blood profile. A recent study found that Femarelle has no effect on clotting in both healthy and thrombophilic women.
Quality issues and regulatory concerns
Femarelle is not a standardized drug. According to an European Food Safety Authority panel, the food/constituent for which the claim is made, i. e. Femarelle, has not been sufficiently characterized and the presented studies by the manufacturer do not support its purported effects.
Femarelle (Finland, Greece, Italy, Spain, Israel, USA, India, Latvia, Lithuania, Estonia, Norway, Sweden)
Tofupill (Cyprus, Mexico)
- Poluzzi E, et al Phytoestrogens in postmenopause: the state of the art from a chemical, pharmacological and regulatory perspective. Curr Med Chem. 2014;21(4):417-36. PMID 24164197 PMC 3963458
- Maneesh Pharmaceuticals Product Femarelle
- Somjen D; Katzburg S; Knoll E et al. (May 2007). "DT56a (Femarelle): a natural selective estrogen receptor modulator (SERM)". J. Steroid Biochem. Mol. Biol. 104 (3–5): 252–8. doi:10.1016/j.jsbmb.2007.03.004. PMID 17428655.
- Somjen D, Yoles I (October 2003). "DT56a stimulates creatine kinase specific activity in vascular tissues of rats". J. Endocrinol. Invest. 26 (10): 966–71. doi:10.1007/bf03348193. PMID 14759068.
- Yoles I, Yogev Y, Frenkel Y, Hirsch M, Nahum R, Kaplan B (2004). "Efficacy and safety of standard versus low-dose Femarelle (DT56a) for the treatment of menopausal symptoms". Clin Exp Obstet Gynecol 31 (2): 123–6. PMID 15266766.
- Yoles I, Yogev Y, Frenkel Y, Nahum R, Hirsch M, Kaplan B (2003). "Tofupill/Femarelle (DT56a): a new phyto-selective estrogen receptor modulator-like substance for the treatment of postmenopausal bone loss". Menopause 10 (6): 522–5. doi:10.1097/01.GME.0000064864.58809.77. PMID 14627860.
- Yoles I, Lilling G (January 2007). "Pharmacological doses of the natural phyto-SERM DT56a (Femarelle) have no effect on MCF-7 human breast cancer cell-line". Eur. J. Obstet. Gynecol. Reprod. Biol. 130 (1): 140–1. doi:10.1016/j.ejogrb.2006.02.010. PMID 16580119.
- Oropeza MV, Orozco S, Ponce H, Campos MG (2005). "Tofupill lacks peripheral estrogen-like actions in the rat reproductive tract". Reprod. Toxicol. 20 (2): 261–6. doi:10.1016/j.reprotox.2005.02.007. PMID 15878261.
- Somjen D, Katzburg S, Lieberherr M, Hendel D, Yoles I (January 2006). "DT56a stimulates gender-specific human cultured bone cells in vitro". J. Steroid Biochem. Mol. Biol. 98 (1): 90–6. doi:10.1016/j.jsbmb.2005.08.002. PMID 16243521.
- Margaret J. Nachtigall, MD, Rebecca H. Jessel, BA, Robert Flaumenhaft, MD, PhD, Richard Nachtigall, MD, Israel Yoles, MD, Frederick Naftolin, MD, PhD, and Lila E. Nachtigall, MD I (July 2010). "The selective estrogen receptor modulator DT56a (Femarelle) does not affect platelet reactivity in normal or thrombophilic postmenopausal women". Menopause: the Journal of the North American Menopause Society 18 (3): 1–4. doi:10.1097/gme.0b013e3181f2f01a. PMID 21037489.
- efsa journal doi:10.2903/j.efsa.2008.785