PDA

View Full Version : Fareston~Toremifene Citrate



heavyiron
12-24-2010, 09:02 AM
Fareston~Toremifene Citrate

Fareston

(Toremifene Citrate)

Fareston is a Selective Estrogen Receptor Modulator (SERM), not unlike its more popular cousins Nolvadex and Clomid. Just as we see with Nolvadex, Fareston is used to treat breast cancer in post-menopausal women. It does this by exerting estrogen antagonistic effects in certain tissue, most notably, breast tissue. This is actually the same mechanism of action found in Nolvadex. This is why Nolvadex is often recommended to bodybuilders who are trying to avoid gynocomastia (growth of breast tissue in males). SERMs, in addition, have several other well known effects in men, which are not simply limited to preventing the abnormal growth of breast tissue.

At the hypothalamus and pituitary, estrogen acts in cooperation with the male body‚??s negative feedback loop to send a signal to decrease the secretion of LH, and when LH secretion is lowered, so are natural testosterone levels. SERMs, like Fareston, possibly act as an estrogen antagonist in the hypothalamus and pituitary, in order to increase testosterone production. Thus, although it hasn‚??t been studied to any great degree, it‚??s highly likely that Fareston is capable of increasing testosterone in the same way that Nolvadex it, as it‚??s androgenicity:estrogenicity ratio is 5x that of Nolvadex (1). It may also be better than Nolvadex for reasons that are of particular interest to steroid using athletes and bodybuilders.

Although anecdotal evidence on this compound is rare, bodybuilders who have already experimented with this stuff seem satisfied. In my estimation, it would seem to be a more potent and safer alternative to Nolvadex, for those who are worried about side effects. I‚??m also predicting that it may provide a greater increase in LH and therefore testosterone levels, in men when compared to Nolvadex (when an appropriate dose of each is utilized). This makes its use a strong possibility for PCT in the future, when studies on its ability to elevate testosterone is more fully studied and understood.
Fareston would also make a welcome addition to a cycle where Cholesterol issues may be a concern, or where something slightly stronger than Nolvadex may be required to prevent gyno.


References:
Breast Cancer Re Treat 1990 Aug;16 Suppl:S3-7. Introduction to toremifene. Kangas L.
Breast 2006 Apr;15(2):142-57. Epub 2005 Nov 9 Toremifene: An evaluation of its safety profile.

heavyiron
12-24-2010, 09:58 AM
Introduction to toremifene.

Kangas L (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Kangas%20L%22%5BAuthor%5D).
Farmos Group, Research Center, Turku, Finland.

Toremifene, a triphenylethylene antiestrogen first synthesized in 1981, binds to the estrogen receptor with an affinity about 5% that of estradiol. Its antiestrogenicity/estrogenicity ratio in animal models is about 5 times that of tamoxifen, though it requires somewhat higher doses for full effectiveness, and it is active against breast cancer in animal and cell culture models. It has a long elimination half-life and there are several metabolites, but the principal antitumor activity appears to be due to the unchanged drug. In Phase I and Phase II clinical trials, toremifene has shown good response rates in ER-positive or ER-unknown tumors, and significant responses after failure of tamoxifen or other hormonal or chemotherapeutic regimens, with rare and mild side effects.

PMID: 2149282 [PubMed - indexed for MEDLINE]

heavyiron
12-24-2010, 09:58 AM
Toremifene: an evaluation of its safety profile.

Harvey HA (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Harvey%20HA%22%5BAuthor%5D), Kimura M (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Kimura%20M%22%5BAuthor%5D), Hajba A (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Hajba%20A%22%5BAuthor%5D).
Division of Hematology/Oncology, Penn State College of Medicine, Penn State Milton S. Hershey Medical Center, 500 University Drive, Hershey, PA 17033, USA. hharvey@psu.edu (hharvey@psu.edu)

Toremifene has been in clinical use for 8 years for the treatment of advanced hormone-sensitive breast cancer and the adjuvant treatment of early breast cancer. More than 350,000 patient treatment years have accumulated, sufficient to allow evaluation of its longer-term safety profile in comparison with tamoxifen and, where possible, with raloxifene and aromatase inhibitors. We reviewed all preclinical and clinical safety data from 1978 to 2004 and comparative clinical safety data between October 1995 and the end of 2004. Secondary endometrial cancer incidence was lower with toremifene than with tamoxifen and was similar to that with raloxifene. It is speculated that toremifene may unmask existing endometrial tumors rather than induce new events. The risk of stroke, pulmonary embolism, and cataract may be lower with toremifene than with tamoxifen and the risk of pulmonary embolism and deep vein thrombosis lower than with raloxifene. Beneficial estrogen agonistic effects were equivalent to those of tamoxifen regarding bone mineral density and superior regarding lipid profiles.

PMID: 16289904 [PubMed - indexed for MEDLINE]