Anti Estrogen Steroids Toremifene Citrate / Fareston for Treating Cancer CAS 89778-27-8

Basic information:

TOREMIFENE CITRATE

Synonyms: FC 1157a; Fareston; NK 622; NSC 613680
CAS: 89778-27-8
Molecular Formula: C26H28ClNO.C6H8O7
Molecular Weight: 598.09
Melting Point: 158-164 ºC
Boiling Point: 535.1 ºC at 760 mmHg
Density: 1.045g/cm3
Refractive index: 1,416-1,418
Appearance: White or almost white powder
Usage:Originally developed to fight breast cancer, bodybuilders have used Fareston to successfully fight gynocomastia caused when testosterone converts to estrogen in the body and men grow breasts. This substance can be used for little else and other similar compounds, such as Nolvadex or Clomid, are much more effective in post-cycle-therapy.

Description:

Toremifene, sold under the brand name Fareston among others, is a medication which is used in the treatment of advanced breast cancer in postmenopausal women. It is taken by mouth.

Side effects of toremifene include hot flashes, sweating, nausea, vomiting, dizziness, vaginal discharge, and vaginal bleeding. It can also cause blood clots, irregular heartbeat, cataracts, visual disturbances, elevated liver enzymes, endometrial hyperplasia, and endometrial cancer. High blood calcium levels can occur in women with bone metastases.

The drug is a selective estrogen receptor modulator (SERM) and hence is a mixed agonist–antagonist of the estrogen receptor (ER), the biological target of estrogens like estradiol.It has estrogenic effects in bone, the liver, and the uterus and antiestrogenic effects in the breasts. It is a triphenylethylene derivative and is closely related to tamoxifen.

Toremifene was introduced for medical use in 1997 It was the first antiestrogen to be introduced since tamoxifen in 1978.It is not available as a generic medication in the United States.

Medical uses:

Toremifene is approved for the treatment of metastatic breast cancer in postmenopausal women with estrogen receptor-positive or unknown-status tumors.This is its only approved use in the United States.It shows equivalent effectiveness to tamoxifen for this indication.Toremifene has been found to be effective in the treatment of breast pain and may be a better drug than tamoxifen for this indication.Toremifene has been reported to significantly improve symptoms of gynecomastia in men.

Mechanism of Action:

Toremifene acts on the estrogen receptor (ER) and possibly activates transcription indirectly through induction of other transcription factors.

Two subtypes of the estrogen receptor are currently characterized including: ERα and ERβ. At ERα toremifene, due to its alkylaminoethoxyphenyl side chain, most likely opposes estrogen actions (antagonist) and at ERβ stimulates estrogen-like actions (agonist). The production of ERα and ERβ are tissue specific. ERα activity and ERβ polymorphisms have been identified in the pathogenesis of breast cancer and gynecomastia.

The antitumor actions of toremifene are believed to be mainly due to its antagonistic effects at ERα; however, other mechanisms may be involved. Toremifene competes with estrogen for binding sites in cancer cells, thereby blocking the growth-stimulating effects of estrogen in the tumor. Further, toremifene may have additional mechanisms which do not involve estrogen receptors. Toremifene also promotes the production of transforming growth factor beta (TGFβ), an inhibitory growth factor.19 TGFβ may cause growth retardation and tumor regression by enhancing cell death (apoptosis) and/or arresting cell proliferation.20 This mechanism of toremifene requires further investigation.

DOSAGE AND ADMINISTRATION:

The dosage of FARESTON is 60 mg, once daily, orally. Treatment is generally continued until disease progression is observed.

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