Toremifene Citrate Breast Cancer Cure and Protection Fareston
|Appearance & Physical State:||White or almost white powder|
|Boiling Point:||535.1ºC at 760 mmHg|
|Storage Condition:||-20ºC Freezer|
|Half Life:||5 days|
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
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 anti-estrogens) are aromatase inhibitors, commonly abbreviated as AIs.
SERMs include compounds such as Toremifene, Nolvadex(Tamoxifen), and Clomid (Clomiphene Citrate). Aromatase inhibitors (AIs) include compounds
such as Arimidex (Anastrozole), Aromasin (Exemestane), and Letrozole (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.
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 needs estrogen, 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.
Related ANTI-ESTROGEN product:
|Tamoxifen Citrate (Nolvadex)||CAS:54965-24-1|
Warnings and Precautions
- Fareston has been shown to prolong the QT interval. Caution should
be exercised in patients with congestive heart failure, hepatic
impairment and electrolyte abnormalities. In patients at increased
risk, ECGs should be obtained at baseline and as clinically
- Hypercalcemia and tumor flare have been reported during the first
weeks of treatment with Fareston in some breast cancer patients
with bone metastases. If hypercalcemia is severe, Fareston
treatment should be discontinued.
- Patients with preexisting endometrial hyperplasia should not be
given long-term Fareston treatment, and patients at high risk for
endometrial cancer should be closely monitored.
- Patients with a history of thromboembolic diseases should not be
treated with Fareston.
- Leukocyte and platelet counts should be monitored when using
Fareston in patients with leukopenia and thrombocytopenia.
- Fareston can cause fetal harm when administered to a pregnant
- Fareston is only indicated for postmenopausal women. However,
premenopausal women prescribed Fareston should use effective
nonhormonal contraception and should be apprised of the potential
hazard to the fetus should pregnancy occur.