Anyone used Evista for PCT?
- 06-16-2006, 06:53 PM
- 06-16-2006, 07:03 PM
Welcome to AMINDS!! Not sure if you saw this or not so posted it anyways lol.. I have not tried it yet but from what I have heard it sounds good .. Bump for anyone who has used it ???
A better S.E.R.M. than tamoxifen(nolvadex)?
Selective Estrogen Receptor Modulators
Raloxifene (Evista) has the ability to bind to and activate the estrogen receptor while exhibiting tissue-specific effects distinct from estradiol.9 As a result, raloxifene is the first of a benzothiophene series of antiestrogens to be labeled a SERM. (Droloxifine, idoxifene and toremifene are similar SERM agents, but they are still considered experimental.) Raloxifene was specifically developed to maintain beneficial estrogenic activity on bone and lipids and antiestrogenic activity on endometrial and breast tissue. In December 1997, the U.S. Food and Drug Administration (FDA) labeled raloxifene for the prevention of osteoporosis.
Although the exact mechanism of action of raloxifene and other similar compounds has not yet been determined, it has been hypothesized that these agents work by inducing conformational changes in the estrogen receptor, resulting in differential expression of specific estrogen-regulated genes in different tissues.10 Activation of the estrogen receptor by these compounds may involve multiple molecular pathways that may result in gene expression of ligand-, tissue- and/or gene-specific receptors.11
Raloxifen (Evista) a different approach
Because SERMs are capable of inducing specific changes in the estrogen receptor, it is not surprising that they may mediate specific pharmacologic activity through their unique agonist or antagonist properties. For example, the agonistic properties of raloxifene on bone tissue were recently demonstrated by the specific activation of the human transforming growth factor-b3 gene, which is an important regulator of bone remodeling.12
Scientists discovered the link between raloxifene and breast cancer in a somewhat roundabout fashion. They were studying the drug's effectiveness in preventing and treating another disease — osteoporosis — when they discovered it could help in preventing breast cancer as well. In fact, the women enrolled in that three-year osteoporosis study experienced a 50 to 70 percent reduction in breast cancer rates compared to the general population. In addition, raloxifene — unlike tamoxifen — does not appear to increase the risk of endometrial cancer, nor does it appear to cause the eye problems (cataracts) associated with tamoxifen. The verdict is still out, however, on whether raloxifene — like tamoxifen — increases a person's risk for pulmonary embolism and deep-vein thrombosis. While some studies suggest it does, not all research supports this finding.
The less serious side effects associated with raloxifene are similar to those reported by women taking tamoxifen or undergoing hormone replacement therapy. In the case of raloxifene, the most common of these are hot flashes and leg cramps.
- 06-16-2006, 09:33 PM
Originally Posted by Supercellular
will be trying toremifene next.
nolva works for me, but not as well as an AI or even chlomid.
06-16-2006, 10:00 PM
Toremifene seems to be the preferred compound right now.Originally Posted by Supercellular
06-16-2006, 10:04 PM
Hey Yeah right. Do you know if Toremifene will increase PgR in breast tissue like nolva?? I have been trying to find something a study or anything on it but having no luck.. It is a SERM like nolva so I would guess it would .. Any info on it??
06-16-2006, 10:09 PM
Clin Cancer Res. 2004 Feb 1;10(3):1057-63. Related Articles, Links
Click here to read
A high serum matrix metalloproteinase-2 level is associated with an adverse prognosis in node-positive breast carcinoma.
Leppa S, Saarto T, Vehmanen L, Blomqvist C, Elomaa I.
Department of Oncology, Helsinki University Central Hospital, PO Box 180, FIN-00029 Helsinki, Finland. email@example.com
PURPOSE: The aim of this study was to determine whether serum matrix metalloproteinase (MMP) -2 and MMP-9 levels could predict overall and disease-free survival in primary node-positive breast cancer. EXPERIMENTAL DESIGN: MMP-2 and MMP-9 levels were quantitatively measured in serum after surgery from 133 patients with primary node-positive breast cancer using enzyme-linked immunoassays. All of the patients received adjuvant therapy, postmenopausal endocrine treatment (tamoxifen or toremifen for 3 years) and premenopausal six cycles of CMF chemotherapy. The follow-up time for all of the patients was 5 years. RESULTS: Overall survival (OS) and disease-free survival (DFS) rates were better among patients with low MMP-2 levels than in patients with high levels (OS, 91% versus 75%, P = 0.020; DFS, 82% versus 58%, P = 0.005). The appearance of bone and visceral metastases was also significantly lower in patients with low serum MMP-2 levels (bone metastases, 10% versus 23%, P = 0.050; visceral metastases, 12% versus 34%, P = 0.018). The prognostic value of MMP-2 levels was most pronounced among a subgroup of estrogen receptor-positive patients (OS, 96% versus 78%, P = 0.052; DFS, 85% versus 58%, P = 0.014), whereas no significant difference was found among estrogen receptor-negative patients (OS, 73% versus 69%, P = 0.25; DFS, 73% versus 63%, P = 0.32). In multivariate analysis, MMP-2 level together with nodal status (NS), progesterone receptor (PgR), and tumor size (T) remained independent predictors for DFS (NS, P = 0.002; PgR, P = 0.004; T, P = 0.023; MMP2, P = 0.039) and OS (NS, P = 0.0002; PgR, P = 0.004; T, P = 0.004; MMP2, P = 0.032). MMP-9 levels did not correlate with survival. CONCLUSIONS: The results suggest that serum postoperative MMP-2 level is a predictor of DFS and OS, and could help to stratify breast cancer patients with primary node-positive disease into low- and high-risk groups.
PMID: 14871985 [PubMed - indexed for MEDLINE]
06-16-2006, 10:10 PM
Cancer. 1990 Dec 1;66(11):2264-9. Related Articles, Links
Predictive value of tumor estrogen and progesterone receptor levels in postmenopausal women with advanced breast cancer treated with toremifene.
Valavaara R, Tuominen J, Johansson R.
Department of Radiotherapy, University of Turku, Finland.
The predictive value of estrogen receptor (ER) concentrations was evaluated in a group of 113 postmenopausal patients with estrogen-receptor-positive (ER greater than 7 fmol/mg protein) advanced breast cancer. In 103 patients, tumors were also sampled for progesterone receptor (PgR) determination. All patients were treated with toremifene, a novel antiestrogen, 60 mg daily. The median ER in 51 responders was 78 fmol/mg protein, and in 62 nonresponders, 51 fmol/mg protein; the median PgR levels were 40 and 37 fmol/mg protein, respectively. The response rate in patients with ER less than 50 fmol/mg protein was 38%, and 51% in the group with ER greater than 50 fmol/mg protein (not significant [NS]). The response rate in patients with PgR less than 10 fmol/mg protein was 42%, and in patients with greater than 10 fmol/mg protein, 44%. The duration of response in patients with ER greater than 50 fmol/mg protein was significantly longer than with lower ER levels (P = 0.002). PgR was not associated with the duration of response. In Cox's multiple regression analysis, ER was an independent prognostic factor (P = 0.005) for response duration. Thus, the ER concentration of tumor tissue predicts the duration of response but not the response rate to toremifene in patients with advanced breast cancer. The PgR status does not predict the response rate or the duration of response.
06-16-2006, 10:11 PM
Int J Cancer. 2001 Jul 1;93(1):20-5. Related Articles, Links
Click here to read
Cell-transforming activity and estrogenicity of bisphenol-A and 4 of its analogs in mammalian cells.
Kanai H, Barrett JC, Metzler M, Tsutsui T.
Department of Pharmacology, The Nippon Dental University, Tokyo, Japan.
Estrogenicity is an important mechanism in hormonal carcinogenesis but not sufficient to explain the carcinogenic activity of all estrogens. Additional mechanisms, related to genetic alterations, in conjunction with estrogenicity mediated through the estrogen receptor, have been suggested. An environmental estrogen bisphenol-A (BP-A) and its analogs are widespread in our living environment. Because of the potential for human exposure, the possible relationship between carcinogenicity and estrogenicity of these bisphenols was studied using mammalian cells. We quantitatively compared the cell-transforming activity of BP-A and 4 of its analogs (BP-2, BP-3, BP-4 and BP-5) in Syrian hamster embryo (SHE) cells lacking estrogen-receptor expression. The transforming activity determined by the morphological transformation frequencies in SHE cells treated with the bisphenols ranked: BP-4 > BP-5 > BP-3 > BP-A > BP-2. We also compared the estrogenicity of the 5 bisphenols in MCF7 human breast cancer cells as determined by cell proliferation or progesterone receptor (PgR) expression assayed by RT-PCR. When MCF7 cells were treated with the bisphenols, the proliferative potency ranked: BP-A > BP-5 > BP-4 > BP-3 = BP-2. The level of mRNA for PgR in cells treated with the bisphenols was BP-A > BP-5 > BP-4 > BP-3 > BP-2. These indicate that the transforming activity does not correlate with the estrogenicity of the bisphenols, except for BP-2 that has the weakest activity at the both endpoints. In addition, our results suggest that bisphenols with few, if any, transforming and estrogenic activities could be altered by a modification of the chemical structure. Published 2001 Wiley-Liss, Inc.
06-16-2006, 11:00 PM
Looks like Toremifene has minimal effects on PgR. Thanks for the studies Yeah Right!!
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