Exemestane metabolites: Synthesis, stereochemical elucidation, biochemical activity and anti-proliferative effects in a hormone-dependent breast cancer cell line.

Author: AmaralCristina, CarvalhoRui A, Correia-da-SilvaGeorgina, CostaSaul C P, LopesAndreia, RoleiraFernanda M F, Tavares da SilvaElisiário, TeixeiraNatércia, VarelaCarla L

Paper Details 
Original Abstract of the Article :
Exemestane is a third-generation steroidal aromatase inhibitor that has been used in clinic for hormone-dependent breast cancer treatment in post-menopausal women. It is known that exemestane undergoes a complex metabolization, giving rise to some already identified metabolites, the 17β-hydroxy-6-me...See full text at original site
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引用元:
https://doi.org/10.1016/j.ejmech.2014.09.074

データ提供:米国国立医学図書館(NLM)

Exemestane's Metabolic Journey: Uncovering New Therapeutic Potential

The field of [oncology] is constantly exploring new ways to combat [breast cancer], particularly in post-menopausal women. This research delves into the [metabolic pathways] of [exemestane], a third-generation steroidal aromatase inhibitor, and their impact on its [anti-proliferative effects] in [hormone-dependent breast cancer cells]. The study focuses on identifying and characterizing various [metabolites] of exemestane, investigating their individual activities.

Exemestane's Metabolites: A Symphony of Activity

The study identifies [four metabolites] of exemestane, both [synthesized] and [acquired]. While some metabolites demonstrate [decreased potency] compared to exemestane, others, like [17-βHE], exhibit [significant increases in activity] against [MCF-7aro cells]. The study suggests that [exemestane's efficacy] may be attributed not only to the parent drug but also to the [active metabolites] produced during its metabolism.

New Avenues for Aromatase Inhibition

The findings of this study provide valuable information about the [mechanisms of action] of exemestane and its metabolites. This understanding opens new avenues for developing more effective [aromatase inhibitors] and understanding their impact on [breast cancer cells]. Further research is needed to fully understand the role of these metabolites in the treatment of breast cancer.

Dr.Camel's Conclusion

This study sheds light on the complex metabolism of exemestane, revealing that its metabolites contribute significantly to its anti-cancer activity. This discovery suggests that the efficacy of exemestane might be even greater than previously thought. Further research into the specific roles of these metabolites could lead to more targeted and effective therapies for hormone-dependent breast cancer.

Date :
  1. Date Completed 2015-07-24
  2. Date Revised 2016-11-25
Further Info :

Pubmed ID

25277066

DOI: Digital Object Identifier

10.1016/j.ejmech.2014.09.074

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