In vitro selective inhibition of human UDP-glucuronosyltransferase (UGT) 1A4 by finasteride, and prediction of in vivo drug–drug interactions. Issue 2 (22nd January 2015)

• Record Type: Journal Article
• Authors: Lee, Seung Jun; Park, Jung Bae; Kim, Doyun; Bae, Soo Hyeon; Chin, Young-Won; Oh, Euichaul; Bae, Soo Kyung
• Is Part Of: Toxicology letters. Volume 232:Issue 2(2015)
• Page Start: 458
• Page End: 465
• Publication Date: 2015-01-22
• Subjects: Toxicology -- Periodicals; 363.179
• DOI: 10.1016/j.toxlet.2014.11.018
• Languages: English
• ISSNs: 0378-4274

Abstract

<abstract abstract-type="author-highlights" id="abs0005"> <title id="sect0005">Highlights</title> <sec> <p id="spar0040"> <list id="lis0005"> <list-item id="lsti0005"> <label></label> <p id="par0005">To our knowledge, inhibition of hepatic UGT isozymes by finasteride has not been explored.</p> </list-item> <list-item id="lsti0010"> <label></label> <p id="par0010">Of the seven hepatic UGTs, finasteride potently and selectively inhibited UGT1A4.</p> </list-item> <list-item id="lsti0015"> <label></label> <p id="par0015">Finasteride did not inhibit hepatic UGT1A1, 1A3, 1A6, 1A9, 2B7, and 2B15 activities.</p> </list-item> <list-item id="lsti0020"> <label></label> <p id="par0020">However, the <italic>C</italic>_max of finasteride in patients is much lower than <italic>K</italic>_i of finasteride for UGT1A4.</p> </list-item> <list-item id="lsti0025"> <label></label> <p id="par0025">Finasteride is unlikely to cause clinically significant drug–drug interactions <italic>via</italic> UGTs inhibition.</p> </list-item> </list> </p> </sec> </abstract>