Toremifene (Fareston): A More Modern SERM
Toremifene Citrate is a selective estrogen receptor modulator (SERM) derived from triphenylethylene. It was patented and approved in Europe in the mid 1990's to treat metastatic ER+ breast cancer in postmenopausal women. Toremifene (Fareston) is an analogue of Tamoxifen and Clomid which can be used to replace these older compounds.
In bodybuilding toremifene citrate is used by men as a drug for post-cycle therapy (PCT) to counteract and/or block some of the effects of excessive estradiol in the body as a result of aromatization of various androgens used. In particular, toremifene is used to restore levels of endogenous testosterone in blood as well as to prevent the estrogen-related side effect of gynecomastia.
In its chemical structure toremifene is very similar to tamoxifen and clomiphene. However, toremifene is a new generation drug and has less toxic side effects than tamoxifen.
For a more effective boost in testosterone production toremifene dosage should be in the range of up to 120 mg per day. This dose can be maintained for a first week of PCT; then, 100mg/day for the second week of PCT; and, finally 60mg/day for the remaining 3 – 4 weeks of PCT. Of course, exact dosages should be determined individually based on blood work results.
Toremifene Information:
Toremifene Description (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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 non-steroidal triphenylethylene derivative, similar in structure and action to both Nolvadex (tamoxifen citrate) and Clomid (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.
History (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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.
Structural Characteristics (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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,N-dimethylethylamine citrate (1:1).
Side Effects (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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). Antiestrogens may harm the developing fetus and should never be used during pregnancy.
Administration (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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.
Availability (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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.
Toremifene Citrate is a selective estrogen receptor modulator (SERM) derived from triphenylethylene. It was patented and approved in Europe in the mid 1990's to treat metastatic ER+ breast cancer in postmenopausal women. Toremifene (Fareston) is an analogue of Tamoxifen and Clomid which can be used to replace these older compounds.
In its chemical structure toremifene is very similar to tamoxifen and clomiphene. However, toremifene is a new generation drug and has less toxic side effects than tamoxifen.
For a more effective boost in testosterone production toremifene dosage should be in the range of up to 120 mg per day. This dose can be maintained for a first week of PCT; then, 100mg/day for the second week of PCT; and, finally 60mg/day for the remaining 3 – 4 weeks of PCT. Of course, exact dosages should be determined individually based on blood work results.
Toremifene Information:
Toremifene Description (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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 non-steroidal triphenylethylene derivative, similar in structure and action to both Nolvadex (tamoxifen citrate) and Clomid (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.
History (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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.
Structural Characteristics (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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,N-dimethylethylamine citrate (1:1).
Side Effects (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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). Antiestrogens may harm the developing fetus and should never be used during pregnancy.
Administration (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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.
Availability (credit: Llewellyn, William. “ANABOLICS” 11th ed. 2017.):
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.
