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
1.
Gardner I, Heikkinen A, Tang L, Lapham K, Goosen T
AAPS J
. 2025 Feb;
27(1):40.
PMID: 39904839
An updated physiologically based pharmacokinetic (PBPK) model was developed for lamotrigine by incorporating a component of metabolism due to a UDP-glucuronyltransferase (UGT) 2B isozyme. This was assigned to UGT2B10 based...
2.
Tang L, Lapham K, Goosen T
AAPS J
. 2024 Sep;
26(6):107.
PMID: 39322784
Lamotrigine is a phenyltriazine anticonvulsant that is primarily metabolized by phase II UDP-glucuronosyltransferases (UGT) to a quaternary N2-glucuronide, which accounts for ~ 90% of the excreted dose in humans. While...
3.
Lapham K, Ferguson N, Niosi M, Goosen T
Drug Metab Dispos
. 2024 Aug;
52(10):1083-1093.
PMID: 39142826
UGT2B4 is a highly expressed drug-metabolizing enzyme in the liver contributing to the glucuronidation of several drugs. To enable quantitatively assessing UGT2B4 contribution toward metabolic clearance, a potent and selective...
4.
Tseng E, Lin J, Strelevitz T, DaSilva E, Goosen T, Obach R
Drug Metab Dispos
. 2024 Feb;
52(5).
PMID: 38408867
In vitro time-dependent inhibition (TDI) kinetic parameters for cytochrome P450 (CYP) 1A2, 2B6, 2C8, 2C9, 2C19, and 2D6, were determined in pooled human liver microsomes for 19 drugs (and 2...
5.
Callegari E, Tse S, Doran A, Goosen T, Shaik N
J Clin Pharmacol
. 2023 Sep;
64(1):80-93.
PMID: 37731282
Glasdegib (DAURISMO) is a hedgehog pathway inhibitor approved for the treatment of acute myeloid leukemia (AML). Cytochrome P450 3A4 (CYP3A4) has been identified as a major metabolism and clearance pathway...
6.
Doran A, Burchett W, Landers C, Gualtieri G, Balesano A, Eng H, et al.
Drug Metab Dispos
. 2022 Jul;
50(9).
PMID: 35777846
The utility of chemical inhibitors in cytochrome P450 (CYP) reaction phenotyping is highly dependent on their selectivity and potency for their target CYP isoforms. In the present study, seventeen inhibitors...
7.
Doran A, Dantonio A, Gualtieri G, Balesano A, Landers C, Burchett W, et al.
Drug Metab Dispos
. 2022 Jul;
50(9).
PMID: 35777845
Cytochrome P450 reaction phenotyping to determine the fraction of metabolism values (f) for individual enzymes is a standard study in the evaluation of a new drug. However, there are technical...
8.
Lin J, Gaudreault F, Johnson N, Lin Z, Nouri P, Goosen T, et al.
Clin Transl Sci
. 2022 Jun;
15(9):2184-2194.
PMID: 35730131
PF-05251749 is a dual inhibitor of casein kinase 1 δ/ε under clinical development to treat disruption of circadian rhythm in Alzheimer's and Parkinson's diseases. In vitro, PF-05251749 (0.3-100 μM) induced...
9.
Bauman J, Doran A, King-Ahmad A, Sharma R, Walker G, Lin J, et al.
Drug Metab Dispos
. 2022 Jun;
50(8):1106-1118.
PMID: 35701182
Abrocitinib is an oral once-daily Janus kinase 1 selective inhibitor being developed for the treatment of moderate-to-severe atopic dermatitis. This study examined the disposition of abrocitinib in male participants following...
10.
Tseng E, Eng H, Lin J, Cerny M, Tess D, Goosen T, et al.
Drug Metab Dispos
. 2021 Jul;
49(10):947-960.
PMID: 34326140
Cytochrome P450 3A (CYP3A) is a frequent target for time-dependent inhibition (TDI) that can give rise to drug-drug interactions (DDI). Yet many drugs that exhibit in vitro TDI for CYP3A...