Femarelle (DT56a)

Femarelle (DT56a) is as a selective estrogen receptor modulator (SERM)^[1] for the treatment of menopause and bone health. DT56a is a standardized compound derived from soybean.^{[citation needed]}

Mode of Action

In animal models, Femarelle exerts agonistic (stimulatory) activity on estrogen receptors in the brain and bone.^[2][3] The compound has been reported to alleviate menopausal symptoms such as hot flushes^[4] and elevate bone mineral density (BMD),^[5] while having no proliferative effects on isolated breast cancer cell lines^[6] and uterine ^[3][7] tissues of rats. Femarelle was found to regenerate the bone through increased osteoblast activity,^[8] which makes it a possible agent for postmenopausal bone loss. Although stimulating estrogen receptors, Femarelle does not appear to change the hormonal blood profile.^[4] A recent study found that Femarelle has no effect on clotting in both healthy and thrombophilic women.^[9]

Trade Names

Femarelle (Finland, Greece, Italy, Spain, Israel, USA, India, Latvia, Lithuania, Estonia, Norway, Sweden)
Tofupill (Cyprus, Mexico)

References

1. ^ 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. 
2. ^ Somjen D, Yoles I (October 2003). "DT56a stimulates creatine kinase specific activity in vascular tissues of rats". J. Endocrinol. Invest. 26 (10): 966–71. PMID 14759068. 
3. ^ ^{a b} Somjen D, Yoles I (July 2003). "DT56a (Tofupill/Femarelle) selectively stimulates creatine kinase specific activity in skeletal tissues of rats but not in the uterus". J. Steroid Biochem. Mol. Biol. 86 (1): 93–8. doi:10.1016/S0960-0760(03)00252-8. PMID 12943748. http://linkinghub.elsevier.com/retrieve/pii/S0960076003002528. 
4. ^ ^{a b} 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. 
5. ^ 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. 
6. ^ 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. 
7. ^ 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. 
8. ^ 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. 
9. ^ 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. 

External links