Piperazine ring toxicity in three novel anti-breast cancer drugs: an in silico and in vitro metabolic bioactivation approach using olaparib as a case study.

Author: AbuelizzHatem A, AlsubiThamer A, AttwaMohamed W, DarwishHany W, KadiAdnan A

Paper Details 
Original Abstract of the Article :
The metabolic activation of small-molecule drugs into electrophilic reactive metabolites is widely recognized as an indicator of idiosyncratic adverse drug reactions (IADRs). Three novel anti-breast cancer drugs containing piperazine rings, ribociclib (Kisqali®, RCB), abemaciclib (Verzenio®, ABC), a...See full text at original site
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引用元:
https://doi.org/10.1007/s00210-023-02413-9

データ提供:米国国立医学図書館(NLM)

Piperazine Ring Toxicity: A Cautionary Tale in Anti-Cancer Drug Development

The development of new anti-cancer drugs is a complex and challenging endeavor. This study investigates the potential toxicity of piperazine rings, a common structural motif in anti-cancer drugs. The study employs in silico and in vitro approaches to evaluate the metabolic activation of piperazine rings and their potential to generate reactive metabolites that can contribute to adverse drug reactions.

The Double-Edged Sword: Piperazine Rings in Anti-Cancer Drugs

The study reveals that piperazine rings can be metabolically activated, generating reactive intermediates that may contribute to toxicity. The study highlights the importance of careful structural design and metabolic evaluation during drug development to minimize the risk of adverse drug reactions. The findings underscore the need for a balance between efficacy and safety in anti-cancer drug development.

Navigating the Desert of Drug Development: A Journey of Safety and Efficacy

This study serves as a reminder that drug development is a delicate balancing act between efficacy and safety. The findings highlight the importance of understanding the potential metabolic pathways and toxicity profiles of drug candidates. By carefully navigating the desert of drug development, we can ensure that new anti-cancer treatments are both effective and safe for patients.

Dr. Camel's Conclusion

This study emphasizes the importance of careful structural design and metabolic evaluation during drug development, reminding us that even seemingly innocuous structural features can harbor unexpected consequences. The findings underscore the need for a balance between efficacy and safety in the development of new drugs, ensuring that patients benefit from the advancements in medicine while minimizing the risk of adverse events. Just as a camel must carefully navigate a desert landscape to avoid danger, we must approach drug development with vigilance and attention to detail, ensuring that each step contributes to the creation of safe and effective treatments.
Date :
  1. Date Completed 2023-06-08
  2. Date Revised 2023-06-13
Further Info :

Pubmed ID

36738368

DOI: Digital Object Identifier

10.1007/s00210-023-02413-9

Related Literature

SNS
PICO Info
in preparation
Languages

English

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