Toremifene Citrate - Fareston Profile

Toremifene Citrate/Fareston Profile

Pharmaceutical Name: Toremifene Citrate
Drug Class: Selective Estrogen Receptor Modulator
Active Life: 5-7 days



Toremifene citrate is a non-steroidal triphenylethylene derivative that exhibits anti-estrogenic properties. It acts as an estrogen receptor antagonist and is quite comparable to tamoxifen citrate in both its actions and mechanisms by which they work. However it is the apparent improved safety of use that toremifene citrate offers that is the main benefit behind it for strength athletes, bodybuilders and other steroid users. Medically, toremifene citrate was developed and is still used to treat breast cancer and was first approved by the Food and Drug Administration for this use in the United States in 1995.

Similar to the other more commonly used selective estrogen receptor modulators used by steroids users, namely clomiphene citrate and tamoxifen citrate, the toremifene citrate molecule binds to estrogen receptors. Thus this leads to the estrogen being blocked from interacting with the receptor and it can not have any influence thereby remaining inactive in that tissue. By doing so an "anti-estrogenic" effect is achieved.

The difficulty in using toremifene citrate is the lack of research conducted using human subjects, and specifically male subjects. While it is possible to apply most of what is known about the other selective estrogen receptor modulators to toremifene citrate, independent research conducted with the drug itself is invaluable and therefore a risk is taken when using the drug because of the lack of information. Unfortunately toremifene citrate is possibly the least researched selective estrogen receptor modulator, with the possible exception of raloxifene.

Despite the lack of human-based research available, in terms of its use in steroid users, toremifene citrate can help in two ways. Firstly due to the binding affinity of the compound it is able to help in the prevention of gynocomastia. Toremifene citrate will compete with estrogen for the estrogen receptors in certain tissues, including the breast, and if it can bind to the receptor estrogen will not have an opportunity to interact with receptor and therefore gynocomastia should not be able to develop. When using anabolic steroids that can convert to estradiol (estrogen) this protection against gynocomastia can be invaluable. However it should be noted that toremifene citrate will not eliminate the estrogen or disallow the conversion to occur. Instead it attempts to counteract the effects of circulating estrogen in the body in those tissues that the drug effects. Therefore there is no evidence that toremifene citrate has any effects counteracting estrogenic side effects that are unrelated to the tissues not affected by the drug. Namely there is no real causal connection to any reduction in water retention and acne in users that begin taking toremifene citrate as it relates to estrogen.

The second, and possibly more beneficial, aspect of toremifene citrate for steroid users is its ability to increase the production of luteinizing hormone and follicle stimulating hormone, and therefore increasing testosterone. This ability is why it is often used by steroid users during their post-cycle therapy. Toremifene citrate would accomplish this by blocking the negative feedback inhibition caused by estrogen at the hypothalamus and pituitary, and this in turn will help to increase the production of these hormones. Currently there is no available research that directly links toremifene citrate to being able to raise testosterone levels in male users, however due to the nearly identical mechanisms that both tamoxifen and toremifene citrate use and the reactions that they produce in the body, it would be easy to extrapolate that both drugs should have similar effects in this respect as well. Anecdotally users have reported good results with toremifene citrate and say that they are at least comparable that those of tamoxifen citrate.

One area where it has seemingly been demonstrated that toremifene citrate outperforms tamoxifen citrate is in terms of its positive effects on the regulation of serum cholesterol (1, 2). It has been shown that toremifene citrate not only supports HDL synthesis, but also LDL reductions. This is due to the estrogenic action of the drug in the liver. While there is some evidence that tamoxifen citrate produces a somewhat similar response, this is significantly outweighed by the response produced by toremifene citrate. It appears that toremifene citrate would be a solid addition for cholesterol support during an anabolic steroid cycle, where the results produced by tamoxifen citrate in the available research are sometimes less then significant.


Use/Dosing

In terms of dosing, sixty milligrams of toremifene citrate has been shown to be similar in effect to that of approximately twenty milligrams of tamoxifen citrate in terms of estrogen receptor binding ability (3). From this it can be extrapolated that for treatment and/or prevention of gynocomastia sixty milligrams should be sufficient for treatment. The same could be said for use during post-cycle therapy when the user wants to raise his testosterone levels as quickly as possible. However, as stated earlier in this profile, no research is currently available that definitively states that there is a certain dosage of the drug that does indeed raise testosterone levels in users whose are suppressed.

In terms of dosing frequency, the drug has a fairly long active life therefore one could administer the compound once every few days. However to maintain fairly stable levels of the drug circulating in their system most users would be best served to administer the drug at least every other day or ideally every day. This ensures that there are no extreme spikes in the level of the drug and no severe tapering off.


Risks/Side Effects

In terms of the safety of toremifene citrate, there is some evidence that suggests that it is actually safer and presents less possible serious side effects then tamoxifen citrate (4). For example the risk of stroke, pulmonary embolism, and cataract are all lower when using toremifene citrate when compared to that of tamoxifen citrate (5), although the incident of ocular toxicity is fairly rare with both drugs (6).

There is no toxicity issues directly related to the use of toremifene citrate (2, 7). Any issues arising in this area were seemingly caused by the hormonal effects of the drug, rather then the properties of the drug itself. As well, most of these complications were connected to the disease, namely breast cancer, that the drug was being administered to treat. For the purposes of anabolic steroid users, toremifene citrate poses no potential toxicity issues.

The only major concern is that there is no available research on the long term effects of administration of this drug. Of course this is due to the drug only having been approved for use since the mid-1990s. Outside of these concerns however, it appears that toremifene is a relatively safe compound for use by most anabolic steroid users.



References

1. Saarto T, Blomqvist C, Ehnholm C, Taskinen MR, Elomaa I. Antiatherogenic effects of adjuvant antiestrogens: a randomized trial comparing the effects of tamoxifen and toremifene on plasma lipid levels in postmenopausal women with node-positive breast cancer. J Clin Oncol. 1996 Feb;14(2):429-33.

2. Kusama M, Miyauchi K, Aoyama H, Sano M, Kimura M, Mitsuyama S, Komaki K, Doihara H. Effects of toremifene (TOR) and tamoxifen (TAM) on serum lipids in postmenopausal patients with breast cancer. Breast Cancer Res Treat. 2004 Nov;88(1):1-8.

3. Valavaara R, Pyrhonen S, Heikkinen M, Rissanen P, Blanco G, Tholix E, Nordman E, Taskinen P, Holsti L, Hajba A. Toremifene, a new antiestrogenic compound, for treatment of advanced breast cancer. Phase II study. Eur J Cancer Clin Oncol. 1988 Apr;24(4):785-90.

4. Riggs BL, Hartman L. Selective estrogen-receptor modulators -- mechanism of action and application to clinical practice. N Engl J Med. 2003;348:618-629.

5. Harvey HA, Kimura M, Hajba A. Toremifene: An evaluation of its safety profile. Breast. 2005 Nov 8

6. Gianni L, Panzini I, Li S, Gelber RD, Collins J, Holmberg SB, Crivellari D, Castiglione-Gertsch M, Goldhirsch A, Coates AS, Ravaioli A; International Breast Cancer Study Group (IBCSG). Ocular toxicity during adjuvant chemoendocrine therapy for early breast cancer: results from International Breast Cancer Study Group trials. Cancer. 2006 Feb 1;106(3):505-13.

7. Gong C, Song E, Jia W, Qin L, Guo J, Jia H, Hu X, Su F. A double-blind randomized controlled trial of toremifen therapy for mastalgia. Arch Surg. 2006 Jan;141(1):43-7