Results 31 to 40 of about 4,522 (127)

Identification and in vivo detection of side-chain hydroxylated metabolites of 4β-hydroxycholesterol

, 2023
Oxysterols are oxidized derivatives of cholesterol that are formed by enzymatic processes or through the action of reactive oxygen species. Several of these bioactive lipids have been shown to be affected and/or play a role in inflammatory processes.
Roumain, Martin, Guillemot-Legris, Owein, Al Houayek, Mireille, Muccioli, Giulio, Mireille Alhouayek, Ameraoui, Hafsa, Martin Roumain, Hafsa Ameraoui, Giulio G. Muccioli, Owein Guillemot-Legris   +9 more
core   +1 more source

Pharmacokinetic profiling of imatinib in relation to CYP3A4 activity in leukaemia patients. [PDF]

Br J Clin Pharmacol
Aim Imatinib pharmacokinetics exhibit large interindividual variability because of differences in CYP3A4 activity—the main imatinib‐metabolizing enzyme. While therapeutic drug monitoring is effective, it requires steady‐state conditions and frequent sampling.
Rasmussen ASB, Koch MR, Rank CU, Andersen CL, Weimann A, Thastrup M, Yang T, Lund TM, Christensen IJ, Nielsen F, Stage TB, Jensen SB, Andersen MK, Schmiegelow K, Dalhoff K.   +14 more
europepmc   +2 more sources

The CYP3A biomarker 4β-hydroxycholesterol does not improve tacrolimus dose predictions early after kidney transplantation. [PDF]

Br J Clin Pharmacol, 2017
Aims: Tacrolimus is a cornerstone in modern immunosuppressive therapy after kidney transplantation. Tacrolimus dosing is challenged by considerable pharmacokinetic variability, both between patients and over time after transplantation, partly due to ...
Størset E, Hole K, Midtvedt K, Bergan S, Molden E, Åsberg A.   +5 more
europepmc   +2 more sources

Quantitative analysis of 4β- and 4α‑hydroxycholesterol in human plasma and serum by UHPLC/ESI-HR-MS [PDF]

, 2020
Cholesterol oxidation product 4β‑hydroxycholesterol (4β‑OHC) may possibly be used as an endogenous biomarker of CYP3A enzyme activity and as CYP3A4 is involved in the metabolism of approximately 50% of the drugs in clinical use, the monitoring of CYP3A ...
Turpeinen, Miia, Mattila, Sampo, Hautajärvi, Heidi, Tolonen, Ari, Hukkanen, Janne   +4 more
core   +1 more source

On the rate of translocation in vitro and kinetics in vivo of the major oxysterols in human circulation

Journal of Lipid Research, 2002
Oxysterols possess powerful biological activities. Some of their effects on the regulation of key enzymes are similar to those of cholesterol, but are much more potent.
Steve Meaney, Karl Bodin, Ulf Diczfalusy, Ingemar Björkhem   +3 more
doaj   +1 more source

Risk assessment of drug–drug interaction potential for bintrafusp alfa with cytochrome P4503A4 substrates: A totality of evidence approach

Clinical and Translational Science, 2022
Bintrafusp alfa, a first‐in‐class bifunctional fusion protein composed of the extracellular domain of TGF‐βRII (a TGF‐β “trap”) fused to a human IgG1 mAb blocking PD‐L1, is being evaluated for efficacy and safety in solid tumor indications as monotherapy
Yulia Vugmeyster, George Locke, Christoph Helwig, P. Alexander Rolfe, Jennifer Q. Dong, Karthik Venkatakrishnan   +5 more
doaj   +1 more source

4β-hydroxycholesterol correlates with dose but not steady-state concentration of carbamazepine: indication of intestinal CYP3A in biomarker formation? [PDF]

Br J Clin Pharmacol, 2016
There is extensive interindividual variability in drug response and tolerability. One of the major reasons for this is differences in drug metabolism, which may reflect pharmacogenetic variability and/or environmental factors, such as age and drug-drug ...
Gjestad C, Huynh DK, Haslemo T, Molden E.   +3 more
europepmc   +2 more sources

Cholesterol 25-hydroxylation activity of CYP3A

Journal of Lipid Research, 2011
To date, many studies have been conducted using 25-hydroxycholesterol, which is a potent regulator of lipid metabolism. However, the origins of this oxysterol have not been entirely elucidated. Cholesterol 25-hydroxylase is one of the enzymes responsible
Akira Honda, Teruo Miyazaki, Tadashi Ikegami, Junichi Iwamoto, Tomomi Maeda, Takeshi Hirayama, Yoshifumi Saito, Tamio Teramoto, Yasushi Matsuzaki   +8 more
doaj   +1 more source

Investigation of CYP3A induction by PF‐05251749 in early clinical development: comparison of linear slope physiologically based pharmacokinetic prediction and biomarker response

Clinical and Translational Science, 2022
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.
Jian Lin, Francois Gaudreault, Nathaniel Johnson, Zhiwu Lin, Parya Nouri, Theunis C. Goosen, Aarti Sawant‐Basak   +6 more
doaj   +1 more source

A Japanese prospective multicenter study of urinary oxysterols in biliary atresia

Scientific Reports, 2021
Diagnosis of biliary atresia (BA) can involve uncertainties. In the present prospective multicenter study, we considered whether urinary oxysterols represent a useful marker for diagnosis of BA in Japanese children.
Ken-ichiro Konishi, Tatsuki Mizuochi, Hajime Takei, Ryosuke Yasuda, Hirotaka Sakaguchi, Jun Ishihara, Yugo Takaki, Masahiro Kinoshita, Naoki Hashizume, Suguru Fukahori, Hiromichi Shoji, Go Miyano, Koichiro Yoshimaru, Toshiharu Matsuura, Yukihiro Sanada, Takahisa Tainaka, Hiroo Uchida, Yumiko Kubo, Hiromu Tanaka, Hideyuki Sasaki, Tsuyoshi Murai, Jun Fujishiro, Yushiro Yamashita, Masaki Nio, Hiroshi Nittono, Akihiko Kimura   +25 more
doaj   +1 more source