D-15414
D-15414' is a nonsteroidal compound belonging to the 2-phenylindole group, characterized as a weak estrogen that was never introduced to the market. It is primarily known as the major metabolite of the selective estrogen receptor modulator (SERM) zindoxifene (D-16726), a drug investigated for its potential in treating breast cancer but ultimately not approved for clinical use.
Pronunciation
Dee-One-Five-Four-One-Four
Etymology
The designation D-15414 follows the alphanumeric naming convention often used in pharmaceutical research, where D could represent the initial of the developing company or laboratory, and 15414 is a sequential number assigned to the compound during its discovery and development phase.
Pharmacodynamics
D-15414 exhibits high affinity for the estrogen receptor (ER), an attribute that enables it to inhibit the growth of ER-positive MCF-7 breast cancer cells in vitro. This action suggests potential therapeutic applications in conditions sensitive to estrogen levels, such as certain forms of breast cancer. However, its development was marred by contradictory findings; while initially identified as an antiestrogenic compound in the context of breast cancer cell growth, further research indicated that D-15414 produced fully estrogenic effects in vitro. These effects were noted to be similar to, but less active than, those induced by estradiol, the primary female sex hormone, without any observed antiestrogenic activity.
Research and Development
The initial interest in D-15414 stemmed from its relationship with zindoxifene, a SERM that was under investigation for its potential to treat breast cancer by selectively modulating the estrogen receptor. The discovery that D-15414, a metabolite of zindoxifene, exhibited estrogenic rather than antiestrogenic activity in vitro raised questions about the efficacy and safety of zindoxifene as a therapeutic agent. This unexpected estrogenic activity of D-15414 is speculated to have contributed to the failure of zindoxifene in clinical trials, highlighting the complexity of drug development and the importance of understanding the pharmacological profile of both active drugs and their metabolites.
Clinical Implications
The case of D-15414 underscores the challenges in developing SERMs and the critical role of metabolites in determining a drug's overall pharmacological effect. The discrepancy between the expected and observed effects of D-15414 points to the necessity for thorough methodological approaches in drug research, especially in understanding the mechanisms underlying estrogen receptor modulation.
Related Terms
See Also
External links
- Medical encyclopedia article on D-15414
- Wikipedia's article - D-15414
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