Human biliary amount prediction using simple, bile flow-rate corrected and uridine diphosphate glucuronosyltransferase activity corrected allometric methods. (July 2017)

• Record Type: Journal Article
• Authors: Giri, Poonam; Patel, Harilal; Srinivas, Nuggehally R
• Is Part Of: International journal of pharmacokinetics. Volume 2:Number 3(2017)
• Page Start: 173
• Page End: 182
• Publication Date: 2017-07
• Subjects: allometry -- bile flow-rate -- biliary amounts -- drug discovery -- interspecies scaling -- pharmacokinetics -- UDPGT activity; Pharmacokinetics -- Periodicals; 615.705
• DOI: 10.4155/ipk-2016-0027
• Languages: English
• ISSNs: 2053-0846

Abstract

Aim: Retrospective scaling of human biliary amounts has been performed using allometry.Methods: Human biliary excretory data for 14 drugs were predicted using simple, bile flow-rate corrected and uridine diphosphate glucuronosyltransferase (UDPGT) activity corrected allometry methods. Allometry was performed using Y = aX b relationship with correction factors. Statistical tests consisting of fold difference (predicted/observed) and root-mean-square error (RMSE) computation were carried out.Results: UDPGT activity corrected allometry predicted higher biliary amounts in humans as compared with other methods. The RMSE values were 38, 32 and 81 for simple, bile flow-rate corrected and UDPGT activity corrected allometry, respectively.Conclusion: Although data showed the usefulness of the approaches for human biliary predictions in the decision process for nominating drug candidate(s) based on % RMSE and fold differences, for some drugs prediction appeared not satisfactory using any of the methods.