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by Anthony Roberts - Toremifene Citrate (Fareston)
is a Selective Estrogen Receptor Modulator (SERM)
derived from triphenylethelyne. It is Licensed in
the United States under the brand name “Fareston”
and currently FDA approved for use in advanced (metastatic)
breast cancer. It is currently being studies for
use in prostate cancer as well.
Background
Toremifene Citrate was originally patented as
Fareston by the Orion Corporation of Finland, and
approved for the treatment of breast cancer in Europe
in 1996. In September of 1999, Roberts Pharmaceutical
Corporation was granted the rights to market the
drug in the United States of America.
Action
Toremifene Citrate exerts its effects by antagonizing
the estrogen receptor in some tissues, and agonizing
it in others. In this way, certain estrogenic pathways
are activated and others are blockaded. It seems
to exert estrogenic effects on blood lipids, reducing
LDL and total cholesterol, as well as estrogenic
effects on bone, improving density. It would also
appear to exert anti-estrogenic effects in breast
tissue, displacing the traditional effects of estrogen,
effectively helping prevent breast cancer in postmenopausal
women.
Technical Data
Fareston is a Selective Estrogen Receptor Modulator.
Other drugs in this class are
Clomid and
Nolvadex. SERMs act by
being an estrogen agonist in certain tissues and
an estrogen antagonist in others.
In men, at the hypothalamus and pituitary, estrogen
acts in cooperation with the body’s negative feedback
loop to send a signal to decrease the secretion
of LH. When LH secretion is lowered, so are natural
testosterone levels. SERMs, like Fareston, possibly
act as an estrogen antagonist in the hypothalamus
and pituitary, in order to increase testosterone
production. Thus, although it hasn’t been studied
to any great degree, it’s highly likely that Fareston
is capable (or better) of increasing testosterone
in the same way that Nolvadex it, as it’s androgenicity:estrogenicity
ratio is 5x that of Nolvadex (1). However, in terms
of improving bone mineral density, Fareston is roughly
equal to Nolvadex. (2) Fareston, like other SERMS,
would appear to have very beneficial effects on
blood lipid levels and other health markers.
User Notes
Although some of the research looks promising,
and it may be the case that Fareston can have potential
to elevate testosterone levels higher than other
SERMs being currently used by bodybuilders and athletes,
the jury is still out on that.
There simply have not been enough people using
Fareston for long enough to know where its place
in the steroid using milieu will eventually be.
For now, it can be considered to have potential,
but nothing more. I have high hopes for this drug
to live up to it’s potential, but only time will
tell.
If you’re considering adding it into a cycle,
just be sure to keep other ancillaries on hand,
just in case.
Toremifene Citrate is the chemical
name of active ingredient in Fareston. Fareston
is a registered trademark of U.S. of GTx, Inc. in
the United States and/or other countries.
Fareston Resources
Fareston Prescribing Information
| Trivial Name |
Toremifene Citrate |
| Systematic Name |
2-(p-[(Z)-4-chloro-1,2-diphenyl-1-butenyl]-phenoxy)-N,N-dimethylethylamine
citrate |
| CAS Number |
89778-26-7 |
| ATC Code |
L02BA02 |
| Merck Index Number |
|
| Chemical Formula |
C26H28CINO· C6H8O7 |
| Molecular Weight |
598.10 |
| Bioavailability |
2%+/- |
| Metabolism |
Hepatic |
| Elimination Half Life |
5 days |
| Excretion |
Fecal 90%, Urine 10% |
| Legal Status |
Controlled |
| Route of Administration |
Oral |
References
- Breast Cancer Re Treat. 1990 Aug;16 Suppl:S3-7.
Introduction to toremifene. Kangas L.
- Breast 2006 Apr;15(2):142-57. Epub 2005
Nov 9. Toremifene: An evaluation of its safety
profile. Harvey HA, Kimura , MHajba A
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