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• W2888370728 endingPage "154" @default.
• W2888370728 startingPage "147" @default.
• W2888370728 abstract "Background: Triptolide, a bioactive component in Tripterygium wilfordii extracts, possess strong antiproliferative activity on all 60-National Cancer Institute (NCI) cancer cell lines. However, the widespread use of triptolide in the clinical practice is greatly limited for its multi-organ toxicity and narrow therapeutic window. All the toxic characteristics of triptolide are associated with the pharmacokinetics especially its distribution and accumulation in the target organ. Methods: The literature review was done using PubMed search, SciFinder and Google Scholar databases with specific keywords such as triptolide, pharmacokinetics, drug-drug interaction, transporters, metabolism, modification to collect the related full-length articles and abstracts from 2000 to 2018. Results: Oral triptolide is rapidly and highly absorbed. Grapefruit juice affects oral absorption, increasing the area under the concentration-time curve (AUC) by 153 % and the maximum concentration (Cmax) by 141 %. The AUC and the Cmax are not dose proportional. Triptolide distributes into the liver, heart, spleen, lung and kidney. Biotransformation of triptolide in rats includes hydroxylation, sulfate, glucuronide, N-acetylcysteine (NAC) and Glutathione (GSH) conjugation and combinations of these pathways. Less than 4 % of triptolide was recovered from the feces, bile and urine within 24 h. After repeating dosage, triptolide was eliminated quickly without accumulation in vivo. As a substrate of P-glycoprotein (P-gp) and CYP3A4, triptolide could have clinically significant pharmacokinetic interactions with those proteins substrates/inhibitors. Conclusion: The findings of this review confirm the importance of pharmacokinetic character for understanding the pharmacology and toxicology of triptolide." @default.
• W2888370728 created "2018-08-31" @default.
• W2888370728 creator A5010922568 @default.
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• W2888370728 date "2019-04-30" @default.
• W2888370728 modified "2023-10-17" @default.
• W2888370728 title "Preclinical Pharmacokinetics of Triptolide: A Potential Antitumor Drug" @default.
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• W2888370728 doi "https://doi.org/10.2174/1389200219666180816141506" @default.
• W2888370728 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30112986" @default.
• W2888370728 hasPublicationYear "2019" @default.
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