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Introduction
of Formestane
Formestane is a medicine that is known as an
aromastase inhibitor and it prevents the production of the
female hormone called oestrogen. It does this by inhibiting
the aromatase enzyme which is responsible for the conversion
of androgens to oestrogens. Formestane is a new mechanism
based aromatase inhibitor which irreversibly inactivates the
enzyme, preventing the conversion of androstenedione to
oestradiol and oestrone; its antitumour effect is mediated by
a reduction in oestrogen syntheses.
Formestane is a powerful suicide aromatase inhibitor. This
means that it decreases estrogen production by preventing the
aromatase enzyme from doing its thing with androgens such as
testosterone. It also decreases the receptor counts for both
estrogen and progesterone. Formestane is now
approved in Europe for the treatment of metastatic breast
cancer in women who have failed tamoxifen therapy. Formestane
is not orally bioavailable and is given intramuscularly each
month.
Adverse
Effects of Formestane
Intramuscular formestane was well tolerated in
clinical trials by the majority of postmenopausal patients
with advanced breast cancer. Local adverse effects at the
injection site have been reported in about 7% of patients. The
most common adverse events experienced by patients treated
with formestane were hot flushes, nausea and vomiting,
lethargy, skin rash/itching. Other adverse events reported
include dizziness, drowsiness, headache, peripheral oedema,
thrombophlebitis, muscle cramps, arthralgia and, rarely,
anaphylactoid reactions. There has been one report of
hypoglycaemia associated with formestane treatment.
Disclaimer:
Information on this page is provided for general
information purposes. You should not make a clinical treatment
decision based on information contained in this page without
consulting other references including the package insert of
the drug, textbooks and where relevant, expert opinion. We
cannot be held responsible for any errors you make in
administering drugs mentioned on this page, nor for use of any
erroneous information contained on this page.
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