CPY3A4-Mediated Lopinavir Bioactivation and Its Inhibition by Ritonavir
Drug Metabolism and Disposition, ISSN: 0090-9556, Vol: 40, Issue: 1, Page: 18-24
2012
- 31Citations
- 45Captures
Metric Options: CountsSelecting the 1-year or 3-year option will change the metrics count to percentiles, illustrating how an article or review compares to other articles or reviews within the selected time period in the same journal. Selecting the 1-year option compares the metrics against other articles/reviews that were also published in the same calendar year. Selecting the 3-year option compares the metrics against other articles/reviews that were also published in the same calendar year plus the two years prior.
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
Citation Benchmarking is provided by Scopus and SciVal and is different from the metrics context provided by PlumX Metrics.
Metrics Details
- Citations31
- Citation Indexes31
- 31
- CrossRef28
- Captures45
- Readers45
- 45
Article Description
The combination of lopinavir (LPV) and ritonavir (RTV) is one of the preferred regimens for the treatment of HIV infection with confirmed efficacy and relatively low toxicity. LPV alone suffers the poor bioavailability due to its rapid and extensive metabolism. RTV boosts the plasma concentration of LPV by suppressing its metabolism and thus increasing LPV efficacy. In the current study, we found that RTV also inhibits LPV bioactivation. LPV bioactivation was investigated in human liver microsomes and cDNA-expressed human cytochromes P450. Twelve GSH-trapped reactive metabolites of LPV were identified by using a metabolomic approach. Semicarbazide-trapped reactive metabolites of LPV were also detected. RTV effectively suppressed all pathways of LPV bioactivation via CYP3A4 inhibition. Our data together with previous reports suggest that LPV plus RTV is an ideal combination because RTV not only boosts LPV plasma concentration, but it decreases LPV bioactivation.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0090955624225770; http://dx.doi.org/10.1124/dmd.111.041400; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84455174621&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/21953914; https://linkinghub.elsevier.com/retrieve/pii/S0090955624225770; https://dx.doi.org/10.1124/dmd.111.041400; https://dmd.aspetjournals.org/content/40/1/18
Elsevier BV
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