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Brain efflux index to investigate the influence of active efflux on brain distribution of pemetrexed and methotrexate.
Author: AgarwalSagar, ElmquistWilliam F, LiLi
Original Abstract of the Article :
Antifolates, in particular methotrexate (MTX), have been widely used in the treatment of primary and secondary tumors of the central nervous system (CNS). Pemetrexed (PMX) is a novel antifolate that also exhibits potent antitumor activity against CNS malignancies. Studies have shown that brain distr...See full text at original site
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引用元:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3920090/
データ提供:米国国立医学図書館(NLM)
Investigating Brain Efflux: The Case of Pemetrexed and Methotrexate
The brain, a complex and intricate organ, is often compared to a hidden oasis in the vast desert of the human body. This research explores the intricate pathways of drug transport across the blood-brain barrier (BBB), a protective membrane that controls what substances enter the brain. The study focuses on pemetrexed (PMX) and methotrexate (MTX), two antifolate drugs commonly used to treat brain tumors. These drugs face a challenging journey, trying to navigate the BBB's intricate network of transporters.
Unraveling the Brain's Gatekeepers
The study reveals that both PMX and MTX undergo saturable efflux transport at the BBB, meaning there are specific transporters actively pumping these drugs out of the brain. It's like encountering a vigilant guard at the entrance to an oasis, carefully scrutinizing each traveler before allowing them entry. The research identifies various efflux transporters, including breast-cancer resistance protein (Bcrp) and organic anion transporters, playing a crucial role in regulating the brain distribution of these antifolates.
Optimizing Treatment for Brain Tumors
This research provides valuable insights into the complex mechanisms governing drug transport in the brain, paving the way for more effective treatment strategies for brain tumors. It's like deciphering a map of a hidden desert route, enabling us to navigate the brain's intricate pathways more effectively. By understanding the role of efflux transporters, researchers can develop new strategies to enhance the delivery of drugs to the brain, improving the effectiveness of therapies for brain tumors.
Dr.Camel's Conclusion
This research is a reminder that the brain, while a hidden oasis in the body, is also a highly guarded territory. The study's findings provide a crucial understanding of the intricate mechanisms that regulate drug transport across the BBB, paving the way for more effective treatment strategies for brain tumors. It's like discovering a new path through the desert, leading us closer to a brighter future for those battling brain cancer.
Date :
- Date Completed 2013-07-12
- Date Revised 2021-12-03
Further Info :
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