Fareston — toremifene citrate

Toremifene citrate is an anti-estrogenic drug, specifically classified as a Selective Estrogen-Receptor Modulator (SERM) with mixed agonist and antagonist properties. It is a nonsteroidal triphenylethylene derivative, similar in structure and action to bothNolvadex (tamoxifen citrate) andClomid (clomiphene citrate). Toremifene citrate is used for the treatment of breast cancer in postmenopausal women with estrogen-receptor positive or estrogen-receptor unknown (unsure if the cancer is estrogen responsive) tumors. It works by attaching to the estrogen receptor in various tissues in a competitive manner, blocking endogenous estrogen from exerting biological activity. As an anti-estrogen in many tissues, male bodybuilders and athletes may use toremifene citrate to counter some of the side effects associated with the use of aromatizable or estrogenic anabolic/androgenic steroids. This may include gynecomastia, body fat gain, and increased water retention.

The triphenylethylene compounds (toremifene citrate,tamoxifen citrate,clomiphene citrate) tend to be somewhat intrinsically estrogenic in the liver. This means that while they can block estrogenic activity in some areas of the body, they can actually act as estrogens in this other key area. Estrogenic action in the liver is important in the regulation of serum cholesterol (it tends to support HDL synthesis and LDL reductions). Since steroid-using bodybuilders are already dealing with the negative cardiovascular effects of these drugs, compounding the issue with aromatase inhibitors (which will lower total serum estrogen levels) may not always be the best option. Using a drug that blocks gynecomastia, for example, while at the same time supporting improved cholesterol values, might be much more ideal. In terms of which triphenylethylene agent is most effective in this regard, evidence suggests that the positive lipid altering benefits of toremifene are significantly stronger than those of tamoxifen, a drug normally favored for this purpose. Toremifene citrate may, therefore, be the preferred antiestrogen among those concerned about their lipid profiles.

Brand name Fareston, Toremifene citrate

Toremifene Citrate History

Toremifene citrate was approved by the FDA as a prescription drug in 1997. It is sold in the U.S. under the Fareston brand name, which is made by GTx, Inc. Fareston is also available in over two dozen other countries including Australia, Austria, Belgium, Czech Republic, Finland, France, Germany, Greece, Hungary, Ireland, Italy, Mexico, Netherlands, New Zealand, Portugal, Russia, South Africa, Spain, Sweden, Switzerland, Thailand, Turkey, and the United Kingdom.

How is Toremifene Citrate Supplied

Toremifene citrate is most commonly supplied in tablets of 88.4 mg, which are labeled as (and equate to) 60 mg of toremifene base.

Structural Characteristics of Toremifene Citrate

Toremifene citrate is classified as a selective estrogen receptor modulator, with both agonist and antagonist properties. It has the chemical designation 2-{p-[(Z)-4-chloro-1,2-diphenyl- 1-butenyl]phenoxy}-N,Ndimethylethylamine citrate (1:1).

Toremifene Citrate Side Effects

Toremifene citrate appears to be well tolerated, with a low incidence of serious side effects. In clinical trials, common side effects associated with its use included hot flashes (35%), sweating (20%), elevated liver enzymes (19%), nausea (14%), vaginal discharge (13%), dizziness (95%), edema (5%), vomiting (4%), and vaginal bleeding (2%). Other observed rare adverse events that may or may not be linked to toremifene citrate administration include low white blood cell and platelet counts, skin discoloration or dermatitis, constipation, difficulty breathing, partial motor paralysis, tremor, vertigo, itching, anorexia, visual disturbances, loss of strength, hair loss, depression, jaundice, and rigors (stiffening of the muscles). Anti-estrogens may harm the developing fetus and should never be used during pregnancy.

Toremifene Citrate Administration

Toremifene citrate is FDA approved for the treatment of metastatic breast cancer in postmenopausal women with estrogen-receptor positive or unknown tumors. The recommended dose is one 60 mg tablet administered once per day.

When used (off-label) to mitigate the estrogenic side effects of anabolic/androgenic steroid use, male athletes and bodybuilders may use 30 mg to 60 mg per day during steroid treatment.

Toremifene Citrate Availability

Toremifene citrate is widely available under the Fareston brand name. It is not commonly sold on the black market, nor is it a high profile item for counterfeiters.

References

Wlliam Llewellyn (2011) - Anabolics

Back to Steroid profiles

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