Raloxifene is a SERM , Selective Estrogen Receptor Modulator, much like tamoxifen and toremifene as well as clomiphene.. Serms, just as their name indicates, bind selectively to estrogen receptors in different tissues eliciting some interesting responses.
In order to understand how to treat gyno we first need to understand exactly what it is. Gynecomastia is abnormal development of breast tissue in males. The primary cause of this is high levels of estrogen. This excess estrogen begins eliciting its effects on the estrogen receptors in the breast tissue, causing tissue growth and development.
There have been many approaches to the prevention and treatment of gyno. More recently the use of an aromatase inhibitor has been advocated for such a purpose. An Aromatase inhibitor (AI) lowers circulating estrogen levels ***8211; therefore less estrogen ***8211; less binding to breast tissue. Absence of estrogen at the receptor site in breast tissue causes tissue cell death. That is one approach ***8211; however alone it may not be most effective.
Tamoxifen was/is another traditional approach to the treatment of gyno. Tamox acts as an estrogen, binding more strongly to selective estrogen receptors, like the receptors in breast tissue. This prevents the estrogen from exerting any effects on the receptor and the tissue effected. Pretty good treatment and it does work. There is plenty of data to support its effectiveness.
So we already said raloxifene is in the same family of compounds as tamoxifen. So what makes it any better for gyno treatment. Well raloxifene, it turns out, has about 10x the binding affinity for the estrogen receptor in breast tissue than tamoxifen does. It binds much more strongly to the receptor site, virtually eliminating the possibility of any estrogen reaching a receptor and exerting the undesired effect. There are head to head studies proving raloxifene is more effective at treating and relieving gyno than tamoxifen is.
Again there are different approaches to the treatment of gyno, but the approach of using a serm is definitely the most effective. It may be prudent to combine this with the use of an Aromatase inhibitor (AI) to lower estrogen as well, lessening the likelihood of the occurrence. However, for treatment a serm, specifically raloxifene , cannot be beat. Remember if no estrogen reaches the recptor in the brest tissue ***8211; the tissue dies. There is no way using an Aromatase inhibitor (AI) to eliminate all estrogen, however with a potent serm like raloxifene , you can prevent any from exerting its effects . If gyno is an issue in your research, it would be very wise to look into this often overlooked but valuable serm.
Get it here >> Raloxifene 120
Refs:
*Vogel, Victor; Joseph Constantino, Lawrence Wickerman et al. (2006-06-21). "Effects of Tamoxifen vs. Raloxifene on the Risk of Developing Invasive Breast Cancer and Other Disease Outcomes". The Journal of the American Medical Association 295 (23): 2727***8211;2741. doi:10.1001/jama.295.23.joc60074. PMID 16754727
*Biochem Pharmacol. 2001 Oct 1;62(7):953-61. Transcriptional activities of estrogen receptor alpha and beta in yeast properties of raloxifene. Jisa E, Dornstauder E, Ogawa S, Inoue S, Muramatsu M, Jungbauer A. Source Institute of Applied Microbiology, University of Agricultural Sciences, Vienna, Austria.
*J Pediatr. 2004 Jul;145(1):71-6. Beneficial effects of raloxifene and tamoxifen in the treatment of pubertal gynecomastia.Lawrence SE, Faught KA, Vethamuthu J, Lawson ML.SourceDepartment of Pediatrics, University of Ottawa, Ontario, Canada. slawrence@cheo.on.ca
*Molecular Characterization of the Microsomal Tamoxifen Binding Site*Blandine Kedjouar, Philippe de Médina, Mustapha Oulad-Abdelghani***8225;,Bruno Payré, Sandrine Silvente-Poirot, Gilles Favre, Jean-Charles Faye and Marc Poirot§ E-mail: poirot@icr.fnclcc.fr.
*http://humupd.oxfordjournals.org/content/6/3/212.full.pdf ***8211; Pharmacological Review of Selective Estrogen Recptor Modulators
Raloxifene 120
In order to understand how to treat gyno we first need to understand exactly what it is. Gynecomastia is abnormal development of breast tissue in males. The primary cause of this is high levels of estrogen. This excess estrogen begins eliciting its effects on the estrogen receptors in the breast tissue, causing tissue growth and development.
There have been many approaches to the prevention and treatment of gyno. More recently the use of an aromatase inhibitor has been advocated for such a purpose. An Aromatase inhibitor (AI) lowers circulating estrogen levels ***8211; therefore less estrogen ***8211; less binding to breast tissue. Absence of estrogen at the receptor site in breast tissue causes tissue cell death. That is one approach ***8211; however alone it may not be most effective.
Tamoxifen was/is another traditional approach to the treatment of gyno. Tamox acts as an estrogen, binding more strongly to selective estrogen receptors, like the receptors in breast tissue. This prevents the estrogen from exerting any effects on the receptor and the tissue effected. Pretty good treatment and it does work. There is plenty of data to support its effectiveness.
So we already said raloxifene is in the same family of compounds as tamoxifen. So what makes it any better for gyno treatment. Well raloxifene, it turns out, has about 10x the binding affinity for the estrogen receptor in breast tissue than tamoxifen does. It binds much more strongly to the receptor site, virtually eliminating the possibility of any estrogen reaching a receptor and exerting the undesired effect. There are head to head studies proving raloxifene is more effective at treating and relieving gyno than tamoxifen is.
Again there are different approaches to the treatment of gyno, but the approach of using a serm is definitely the most effective. It may be prudent to combine this with the use of an Aromatase inhibitor (AI) to lower estrogen as well, lessening the likelihood of the occurrence. However, for treatment a serm, specifically raloxifene , cannot be beat. Remember if no estrogen reaches the recptor in the brest tissue ***8211; the tissue dies. There is no way using an Aromatase inhibitor (AI) to eliminate all estrogen, however with a potent serm like raloxifene , you can prevent any from exerting its effects . If gyno is an issue in your research, it would be very wise to look into this often overlooked but valuable serm.
Get it here >> Raloxifene 120
Refs:
*Vogel, Victor; Joseph Constantino, Lawrence Wickerman et al. (2006-06-21). "Effects of Tamoxifen vs. Raloxifene on the Risk of Developing Invasive Breast Cancer and Other Disease Outcomes". The Journal of the American Medical Association 295 (23): 2727***8211;2741. doi:10.1001/jama.295.23.joc60074. PMID 16754727
*Biochem Pharmacol. 2001 Oct 1;62(7):953-61. Transcriptional activities of estrogen receptor alpha and beta in yeast properties of raloxifene. Jisa E, Dornstauder E, Ogawa S, Inoue S, Muramatsu M, Jungbauer A. Source Institute of Applied Microbiology, University of Agricultural Sciences, Vienna, Austria.
*J Pediatr. 2004 Jul;145(1):71-6. Beneficial effects of raloxifene and tamoxifen in the treatment of pubertal gynecomastia.Lawrence SE, Faught KA, Vethamuthu J, Lawson ML.SourceDepartment of Pediatrics, University of Ottawa, Ontario, Canada. slawrence@cheo.on.ca
*Molecular Characterization of the Microsomal Tamoxifen Binding Site*Blandine Kedjouar, Philippe de Médina, Mustapha Oulad-Abdelghani***8225;,Bruno Payré, Sandrine Silvente-Poirot, Gilles Favre, Jean-Charles Faye and Marc Poirot§ E-mail: poirot@icr.fnclcc.fr.
*http://humupd.oxfordjournals.org/content/6/3/212.full.pdf ***8211; Pharmacological Review of Selective Estrogen Recptor Modulators
Raloxifene 120
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