akn
Musclechemistry Member
Description:
Formestane is classified as a selective irreversible steroidal
aromatase inhibitor.This agent is structurally a derivative of
androstenedione, differing from this well known
prohormone only by the addition of a 4-hydroxyl group.
This group, however, is responsible for causing an
irreversible attachment between formestane and
aromatase when the two come into contact with each
other. This means that formestane will bond with the
enzyme and never let it go, permanently deactivating it as
a result. The enzyme will need to be replaced, through
normal attrition, before the body will recover its lost
estrogen synthesizing capacity. This may take several days
or more following cessation of therapy. Given this mode of
action, formestane is also referred to as a "suicide"
aromatase inhibitor, as the drug essentially sacrifices itself
in the process of blocking estrogen conversion. As a class
of drugs, aromatase inhibitors are used (off-label) by male
bodybuilders and athletes to prevent the estrogenic side
effects of certain anabolic/androgenic steroids, and to
increase fat loss and muscle definition while dieting.
Because of its potent estrogen-suppressing action,
formestane has been used clinically to treat breast cancer
patients in a number of countries including England,
Germany, SWitzerland, Spain, Australia, New Zealand, Italy,
and Malaysia .It has been shown to be an effective
option as a second line of defense after tamoxifen, an
estrogen receptor antagonist, has failed to elicit a positive
response with patients, and produces an overall response
statistically similar to tamoxifen when administered as the
first-line therapy. In terms of overall potency, formestane
is not as strong as the selective third generation inhibitors
like Arimidex (anastrozole) or Femara (Ietrozole). One
study, for example, notes a 790/0 level of suppression of
estrogen levels with 4 weeks use of Arimidex 1 mg daily
(on par with levels noted with Femara use), but only a 580/0
level of suppression with intramuscular formestane
injections (250 mg every two weeks) . But next to estrogen
receptor antagonists like Clomid (clomiphene citrate) and
Nolvadex (tamoxifen citrate), formestane is significantly
more effective at blocking the effects of estrogen in the
body.
History:
Formestane was the first selective aromatase inhibitor to
be developed as a prescription drug, first appearing in
Europe during the mid-1990s under the Lentaron Depot
brand name. It was sold by Novartis, which marketed
Lentaron Depot in two-dozen countries including
Argentina, Austria, Belgium, Brazil, Canada, Chile, Czech
Republic, Denmark, France, Germany, Greece, Hong Kong,
Ireland, Israel, Italy, Malaysia, Netherlands, Portugal, South
Africa, Spain, Switzerland, Turkey, and the United Kingdom.
With the emergence of newer and more effective
aromatase inhibitors, however, formestane soon lost
market presence at a rapid rate. Most of the initial Lentaron
Depot preparations have since been discontinued. The
drug remains available today, but only in a small number of
nations. This includes Austria, Brazil, Czech Republic, Hong
Kong, and Turkey.
How Supplied:
Formestane is most commonly supplied in a sterile
solution containing 125 mg/mL of drug in a 2 mL ampule.
Structural Characteristics:
Formestane is classified a steroidal selective irreversible
aromatase inhibitor. It has the chemical designation 4Hydroxyandrost-
4-ene-3,17-dione.
Side Effects:
Common side effects associated with the use of an
aromatase inhibitor include hot flashes, joint pain,
weakness, fatigue, mood changes, depression, high blood
pressure, swelling of the arms/legs, and headache.
Aromatase inhibitors may also decrease bone mineral
density, which may lead to osteoporosis and an increase in
fractures in susceptible patients. Some individuals may also
respond to the medication with gastrointestinal side
effects including nausea and vomiting. Aromatase
inhibitors can harm the development of an unborn fetus,
and should never be taken or handled during pregnancy.
When taken by men (as an off-label use) to reduce
estrogenicity during prolonged periods of steroid
treatment, aromatase inhibitors may increase
cardiovascular disease (CVD) risk by retarding some
beneficial properties of estrogen on cholesterol values.
Studies have demonstrated that when an aromatizable
steroid such as testosterone enanthate is taken in
conjunction with an aromatase inhibitor, suppression of
HDL (good) cholesterol levels becomes significantly more
pronounced. Since the estrogen receptor
agonist/antagonist Nolvadex® generally does not display
the same anti-estrogenic (negative) effect on cholesterol
values, it is usually favored over aromatase inhibitors for
estrogen maintenance by male bodybuilders and athletes
concerned with cardiovascular health.
Administration:
Formestane is indicated for the treatment of advanced
breast cancer in postmenopausal women. The
recommended dosage is 250 mg by intramuscular
injection (buttock) every two weeks. Although not a
medically approved form of the drug, studies have
demonstrated that a similar level of estrogen suppression
can also be achieved with oral use of formestane. Due to
poor bioavailability, however, the dose needed is around
250 mg per day. When used (off-label) to mitigate the
estrogenic side effects of anabolic/androgenic steroid use
or increase muscle definition, male athletes and
bodybuilders often take 250 mg every two weeks by
injection, or 250 mg per day orally.
Availability:
Formestane is not widely available as a prescription drug,
and consequently is rarely circulated in the athletic
community. Note that a small number of oral preparations
can be found in the United States, where they are
occasionally marketed as nutritional supplements.
Formestane is classified as a selective irreversible steroidal
aromatase inhibitor.This agent is structurally a derivative of
androstenedione, differing from this well known
prohormone only by the addition of a 4-hydroxyl group.
This group, however, is responsible for causing an
irreversible attachment between formestane and
aromatase when the two come into contact with each
other. This means that formestane will bond with the
enzyme and never let it go, permanently deactivating it as
a result. The enzyme will need to be replaced, through
normal attrition, before the body will recover its lost
estrogen synthesizing capacity. This may take several days
or more following cessation of therapy. Given this mode of
action, formestane is also referred to as a "suicide"
aromatase inhibitor, as the drug essentially sacrifices itself
in the process of blocking estrogen conversion. As a class
of drugs, aromatase inhibitors are used (off-label) by male
bodybuilders and athletes to prevent the estrogenic side
effects of certain anabolic/androgenic steroids, and to
increase fat loss and muscle definition while dieting.
Because of its potent estrogen-suppressing action,
formestane has been used clinically to treat breast cancer
patients in a number of countries including England,
Germany, SWitzerland, Spain, Australia, New Zealand, Italy,
and Malaysia .It has been shown to be an effective
option as a second line of defense after tamoxifen, an
estrogen receptor antagonist, has failed to elicit a positive
response with patients, and produces an overall response
statistically similar to tamoxifen when administered as the
first-line therapy. In terms of overall potency, formestane
is not as strong as the selective third generation inhibitors
like Arimidex (anastrozole) or Femara (Ietrozole). One
study, for example, notes a 790/0 level of suppression of
estrogen levels with 4 weeks use of Arimidex 1 mg daily
(on par with levels noted with Femara use), but only a 580/0
level of suppression with intramuscular formestane
injections (250 mg every two weeks) . But next to estrogen
receptor antagonists like Clomid (clomiphene citrate) and
Nolvadex (tamoxifen citrate), formestane is significantly
more effective at blocking the effects of estrogen in the
body.
History:
Formestane was the first selective aromatase inhibitor to
be developed as a prescription drug, first appearing in
Europe during the mid-1990s under the Lentaron Depot
brand name. It was sold by Novartis, which marketed
Lentaron Depot in two-dozen countries including
Argentina, Austria, Belgium, Brazil, Canada, Chile, Czech
Republic, Denmark, France, Germany, Greece, Hong Kong,
Ireland, Israel, Italy, Malaysia, Netherlands, Portugal, South
Africa, Spain, Switzerland, Turkey, and the United Kingdom.
With the emergence of newer and more effective
aromatase inhibitors, however, formestane soon lost
market presence at a rapid rate. Most of the initial Lentaron
Depot preparations have since been discontinued. The
drug remains available today, but only in a small number of
nations. This includes Austria, Brazil, Czech Republic, Hong
Kong, and Turkey.
How Supplied:
Formestane is most commonly supplied in a sterile
solution containing 125 mg/mL of drug in a 2 mL ampule.
Structural Characteristics:
Formestane is classified a steroidal selective irreversible
aromatase inhibitor. It has the chemical designation 4Hydroxyandrost-
4-ene-3,17-dione.
Side Effects:
Common side effects associated with the use of an
aromatase inhibitor include hot flashes, joint pain,
weakness, fatigue, mood changes, depression, high blood
pressure, swelling of the arms/legs, and headache.
Aromatase inhibitors may also decrease bone mineral
density, which may lead to osteoporosis and an increase in
fractures in susceptible patients. Some individuals may also
respond to the medication with gastrointestinal side
effects including nausea and vomiting. Aromatase
inhibitors can harm the development of an unborn fetus,
and should never be taken or handled during pregnancy.
When taken by men (as an off-label use) to reduce
estrogenicity during prolonged periods of steroid
treatment, aromatase inhibitors may increase
cardiovascular disease (CVD) risk by retarding some
beneficial properties of estrogen on cholesterol values.
Studies have demonstrated that when an aromatizable
steroid such as testosterone enanthate is taken in
conjunction with an aromatase inhibitor, suppression of
HDL (good) cholesterol levels becomes significantly more
pronounced. Since the estrogen receptor
agonist/antagonist Nolvadex® generally does not display
the same anti-estrogenic (negative) effect on cholesterol
values, it is usually favored over aromatase inhibitors for
estrogen maintenance by male bodybuilders and athletes
concerned with cardiovascular health.
Administration:
Formestane is indicated for the treatment of advanced
breast cancer in postmenopausal women. The
recommended dosage is 250 mg by intramuscular
injection (buttock) every two weeks. Although not a
medically approved form of the drug, studies have
demonstrated that a similar level of estrogen suppression
can also be achieved with oral use of formestane. Due to
poor bioavailability, however, the dose needed is around
250 mg per day. When used (off-label) to mitigate the
estrogenic side effects of anabolic/androgenic steroid use
or increase muscle definition, male athletes and
bodybuilders often take 250 mg every two weeks by
injection, or 250 mg per day orally.
Availability:
Formestane is not widely available as a prescription drug,
and consequently is rarely circulated in the athletic
community. Note that a small number of oral preparations
can be found in the United States, where they are
occasionally marketed as nutritional supplements.
