Theunis C Goosen
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Explore the profile of Theunis C Goosen including associated specialties, affiliations and a list of published articles.
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59
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1109
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Recent Articles
11.
Eng H, Tseng E, Cerny M, Goosen T, Obach R
Drug Metab Dispos
. 2021 Apr;
49(6):442-450.
PMID: 33811106
Time-dependent inhibition (TDI) of CYP3A is an important mechanism underlying numerous drug-drug interactions (DDIs), and assays to measure this are done to support early drug research efforts. However, measuring TDI...
12.
Callegari E, Lin J, Tse S, Goosen T, Sahasrabudhe V
CPT Pharmacometrics Syst Pharmacol
. 2020 Dec;
10(2):127-136.
PMID: 33314761
The sodium-glucose cotransporter 2 inhibitor ertugliflozin is metabolized by the uridine 5'-diphospho-glucuronosyltransferase (UGT) isozymes UGT1A9 and UGT2B4/2B7. This analysis evaluated the drug-drug interaction (DDI) following co-administration of ertugliflozin with the...
13.
Wong S, Ramsden D, Dallas S, Fung C, Einolf H, Palamanda J, et al.
Drug Metab Dispos
. 2020 Nov;
49(1):94-110.
PMID: 33139460
Translational and ADME Sciences Leadership Group Induction Working Group (IWG) presents an analysis on the time course for cytochrome P450 induction in primary human hepatocytes. Induction of CYP1A2, CYP2B6, and...
14.
Lapham K, Callegari E, Cianfrogna J, Lin J, Niosi M, Orozco C, et al.
Drug Metab Dispos
. 2020 Oct;
48(12):1350-1363.
PMID: 33020067
Ertugliflozin is primarily cleared through UDP-glucurosyltransferase (UGT)-mediated metabolism (86%) with minor oxidative clearance (12%). In vitro phenotyping involved enzyme kinetic characterization of UGTs or cytochrome P450 enzymes catalyzing formation of...
15.
Miners J, Rowland A, Novak J, Lapham K, Goosen T
Pharmacol Ther
. 2020 Sep;
218:107689.
PMID: 32980440
Enzymes of the UDP-glucuronosyltransferase (UGT) superfamily contribute to the elimination of drugs from almost all therapeutic classes. Awareness of the importance of glucuronidation as a drug clearance mechanism along with...
16.
Lin J, Goosen T, Tse S, Yamagami H, Malhotra B
J Clin Pharmacol
. 2019 May;
59(11):1505-1518.
PMID: 31090092
5-Hydroxymethyl tolterodine (5-HMT; the active fesoterodine metabolite) is metabolized via the cytochrome P450 (CYP) 2D6 and CYP3A pathways. Mirabegron is a moderate CYP2D6 inhibitor and weak CYP3A inhibitor. Potential drug-drug...
17.
Lapham K, Lin J, Novak J, Orozco C, Niosi M, Di L, et al.
Drug Metab Dispos
. 2018 Sep;
46(12):1836-1846.
PMID: 30194276
6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1-indole-3-carboxylic acid (PF-06409577) is a direct activator of the human 1-containing adenosine monophosphate-activated protein kinase (ΑMPK) isoforms. The clearance mechanism of PF-06409577 in animals and humans involves uridine diphosphoglucuronosyl transferase...
18.
Kenny J, Ramsden D, Buckley D, Dallas S, Fung C, Mohutsky M, et al.
Drug Metab Dispos
. 2018 Jul;
46(9):1285-1303.
PMID: 29959133
The Innovation and Quality Induction Working Group presents an assessment of best practice for data interpretation of in vitro induction, specifically, response thresholds, variability, application of controls, and translation to...
19.
Achour B, Dantonio A, Niosi M, Novak J, Al-Majdoub Z, Goosen T, et al.
Drug Metab Dispos
. 2018 Mar;
46(6):805-812.
PMID: 29581103
Quantitative proteomic methods require optimization at several stages, including sample preparation, liquid chromatography-tandem mass spectrometry (LC-MS/MS), and data analysis, with the final analysis stage being less widely appreciated by end-users....
20.
Tseng E, Fate G, Walker G, Goosen T, Obach R
Drug Metab Dispos
. 2018 Feb;
46(5):493-502.
PMID: 29475834
Maraviroc (MVC) is a CCR5 coreceptor antagonist indicated in combination with other antiretroviral agents for the treatment of CCR5-tropic human immunodefinciency virus-1 infection. In this study, the metabolism of MVC...