D-15414 is a
nonsteroidal weak
estrogen of the
2-phenylindole group which was never marketed.
It is the major
metabolite
In biochemistry, a metabolite is an intermediate or end product of metabolism.
The term is usually used for small molecules. Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, c ...
of the
selective estrogen receptor modulator
Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonist/antagonists (ERAAs), are a class of drugs that act on the estrogen receptor (ER). A characteristic that distinguishes these substances from pure ER agonists a ...
(SERM)
zindoxifene
Zindoxifene (INN; former developmental code names D-16726, NSC-341952) is a nonsteroidal selective estrogen receptor modulator (SERM) that was under development in the 1980s and early 1990s for the treatment of breast cancer but was not marketed ...
(D-16726).
D-15414 has high
affinity
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* Affinity Credit Union, a Saskatchewan-based credit union
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for the
estrogen receptor (ER) and inhibits the growth of ER-positive
MCF-7 breast cancer cells ''
in vitro''.
However, contradictorily, subsequent research found that the drug produced fully
estrogenic effects ''in vitro'' similarly to but less actively than
estradiol, with no
antiestrogenic activity observed.
The reason for the discrepancy between the findings is unclear, though may be due to
methodology.
The unexpected estrogenic activity of D-15414 may be responsible for the failure of zindoxifene in
clinical trials as a treatment for
breast cancer.
References
Abandoned drugs
Indoles
Synthetic estrogens
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