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Basic
Information of Fulvestrant
Chemical Name: Fulvestrant
Cas No.: 129453-61-8
Molecular Formula: C32H47F5O3S
Chemical Structure:
Fulvestrant, sold under the brand name
Faslodex among others, is a medication used to treat hormone receptor
(HR)-positive metastatic breast cancer in postmenopausal women with disease
progression as well as HR-positive, HER2-negative advanced breast cancer in
combination with palbociclib in women with disease progression after endocrine
therapy. It is given by injection into a muscle.
Fulvestrant is a selective estrogen
receptor degrader (SERD) and was first-in-class to be approved. It works by
binding to the estrogen receptor and destabilizing it, causing the cell's
normal protein degradation processes to destroy it.
Fulvestrant is used for the treatment of
hormone receptor positive metastatic breast cancer or locally advanced
unresectable disease in postmenopausal women; it is given by injection. A 2017
Cochrane review found it is as safe and effective as first line or second line
endocrine therapy.
It is also used to treat HR-positive,
HER2-negative advanced or metastatic breast cancer in combination with
palbociclib in women with disease progression after first-line endocrine
therapy.
Hormones are chemical substances that are
produced by glands in the body, which enter the bloodstream and cause effects
in other tissues. For example, the hormone testosterone made in the testicles
and is responsible for male characteristics such as deepening voice and
increased body hair. The use of hormone therapy to treat cancer is based on the
observation that receptors for specific hormones that are needed for cell
growth are on the surface of some tumor cells.
Hormone therapies work by stopping the production of a certain hormone,
blocking hormone receptors, or substituting chemically similar agents for the
active hormone, which cannot be used by the tumor cell. The different types of hormone therapies are
categorized by their function and/or the type of hormone that is affected.
Many breast cancers have estrogen
receptors, and the growth of these tumors can be stimulated by estrogen.
Fulvestrant is an estrogen receptor downregulator, this means it binds to the
estrogen receptor site in competition with estrogen in the body. Once it binds to the site it causes the
receptors to break down, thereby preventing normal cellular response to
estrogen.
Fulvestrant is a selective estrogen
receptor degrader (SERD).
It works by binding to the estrogen
receptor and making it more hydrophobic, which makes the receptor unstable and
misfold, which in turn leads normal processes inside the cell to degrade it.
Fulvestrant is slowly absorbed and maximum
plasma concentrations (Cmax) are reached after about 5 days and the terminal
half-life is around 50 days. Fulvestrant is highly (99%) bound to plasma proteins
including very low density lipoprotein, low density lipoprotein, and high
density lipoprotein. It appears to be metabolized along the same pathways as
endogenous steroids; CYP3A4 may be involved, but non-cytochrome routes appear
to be more important. It does not inhibit any CYP450 enzymes. Elimination is
almost all via feces.
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References:
https://en.wikipedia.org/wiki/Fulvestrant
https://www.ncbi.nlm.nih.gov/pubmed/20156170
https://www.ncbi.nlm.nih.gov/pubmed/16198056
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