Solitary Inhibition of the Breast Cancer Resistance Protein Efflux Transporter Results in a Clinically Significant Drug-Drug Interaction with Rosuvastatin by Causing up to a 2-Fold Increase in Statin Exposure.

Author: ElsbyRobert, FennerKatherine, MartinPaul, SharmaPradeep, SurryDominic

Paper Details 
Original Abstract of the Article :
The intestinal efflux transporter breast cancer resistance protein (BCRP) restricts the absorption of rosuvastatin. Of the transporters important to rosuvastatin disposition, fostamatinib inhibited BCRP (IC50 = 50 nM) and organic anion-transporting polypeptide 1B1 (OATP1B1; IC50 > 10 μM), but not or...See full text at original site
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引用元:
https://doi.org/10.1124/dmd.115.066795

データ提供:米国国立医学図書館(NLM)

Drug-Drug Interactions: Unveiling the Hidden Effects of Transporter Inhibition

The world of drug interactions is a complex and intricate desert, full of hidden pathways and unexpected encounters. This research delves into the potential for drug-drug interactions caused by the inhibition of efflux transporters, specifically the breast cancer resistance protein (BCRP), which plays a crucial role in drug absorption and elimination. Researchers investigated the effect of fostamatinib, a drug that inhibits BCRP, on the pharmacokinetics of rosuvastatin, a statin medication used to lower cholesterol levels. They discovered that fostamatinib significantly increased the exposure to rosuvastatin, highlighting the importance of considering transporter inhibition when predicting drug-drug interactions.

Navigating the Desert of Drug Interactions

This research emphasizes the importance of understanding the role of efflux transporters in drug disposition and considering potential drug-drug interactions caused by transporter inhibition. The study highlights the need for careful evaluation of potential interactions, particularly for medications that rely on transporters for their absorption and elimination.

Safeguarding Medication Interactions

This research serves as a reminder that even seemingly unrelated medications can interact in complex ways. It underscores the importance of consulting with healthcare professionals to ensure the safe and effective use of medications, particularly when taking multiple drugs.

Dr.Camel's Conclusion

Just like a camel needs to navigate a treacherous desert landscape, navigating the world of drug interactions requires careful consideration of the potential for hidden pathways and unexpected encounters. This research highlights the importance of understanding the role of transporters in drug disposition to ensure safe and effective medication use.

Date :
  1. Date Completed 2016-10-24
  2. Date Revised 2021-12-03
Further Info :

Pubmed ID

26700956

DOI: Digital Object Identifier

10.1124/dmd.115.066795

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SNS
PICO Info
in preparation
Languages

English

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