USP Factory Manufacturer Toremifene citrate CAS NO.89778-27-8

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Fareston INDICATIONS AND USAGE

FARESTON is an estrogen agonist/antagonist indicated for the treatment of metastatic breast cancer in postmenopausal women with estrogen-receptor positive or unknown tumors.

DOSAGE AND ADMINISTRATION

60 mg once daily, orally

DOSAGE FORMS AND STRENGTHS

60 mg tablet is round, convex, unscored, uncoated, and white, or almost white, identified with TO 60 embossed on one side.

When This Medicine Should Not Be Used:

You should not use this medicine if you have had an allergic reaction to toremifene citrate, or if you are pregnant. You should not use this medicine if you have a low potassium or magnesium in the blood; or heart rhythm problems (such as congenital or acquired long QT syndrome). This medicine should not be given to men and children.

Toremifene Citrate Description:

Toremifene (also known under its brand and trade name of Fareston) is a member of a category, family, and class of drugs that are known as SERMs (Selective Estrogen Receptor Modulators). SERMs fall under an even broader category of drugs that are known as anti-estrogens, and the cousin family of SERMs (that also fall under Toremifene, Clomid (Clomiphene Citrate). Aromatase inhibitors (AIs) include compounds such as Arimidex (Anastrozole), Femara).

Although the two fall under the category of anti-estrogens, they are both sub-categories that branch off into their own families, as SERMs and AIs differ greatly in their mechanism of action within the human body concerning how they control or block Estrogen. There has been much misunderstanding and misconception in previous decades as to what each of these do, and this should always be first clarified to the reader before describing Toremifene.

Fareston Application

Toremifene is used in postmenopausal women to treat breast cancer that has spread to other parts of the body (metastatic breast cancer). It is usually used to treat cancerthat needsestrogen, a female hormone, in order to grow (estrogen-receptor positive). Toremifene is a nonsteroidal antiestrogen that blocks the effects of estrogen in thebreast tissue, thereby slowing or stopping the growth of cancer.

SERMs are true ‘Estrogen blockers’, while AIs are not. SERMs act to block the activity of Estrogen at their target receptor sites in different tissues (mainly breast tissue), and they do this by binding more strongly to the Estrogen receptors in these tissues than Estrogen itself, effectively taking the spot that Estrogen normally would. The SERMs will remain bound to the receptor site and remain inert (they will not activate the receptors or perform any actions) This results in the inability for Estrogen to bind to these receptors (as they are already occupied by the SERM).

While SERMs block Estrogenic activity at certain receptor sites, SERMs can and do also act as estrogens themselves in other receptor sites in other tissues in the body (such as in the liver, which can be beneficial). This is known as Estrogen agonist and Estrogen antagonist activity. In any case, SERMs do not serve to lower overall total circulating blood plasma levels of Estrogen in the body – they merely block its activity in certain tissues.

Aromatase inhibitors (AIs) are instead the compounds that will reduce total circulating levels of Estrogen in the body by way of binding to the enzyme responsible for the conversion (aromatization) of androgens into Estrogen. This enzyme is known as aromatase. AIs are more attractive as a substrate to the aromatase enzyme than the aromatase enzyme’s traditional substrate targets, which are androgens (such as Testosterone).

The result is that the aromatase enzyme is occupied with the AI, and therefore cannot engage in chemical reactions with androgens. This results in the inability for Estrogen to be manufactured at its root source, and therefore Estrogen levels as a whole are reduced in the body.

How to use toremifene

Take this medication by mouth with or without food, usually once daily or as directed by your doctor. Dosage is based on your medical condition and response to therapy.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.

Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.

Since this drug can be absorbed through the skin and lungs, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.