Results 31 to 40 of about 3,746 (131)

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

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

Predicting Pharmacokinetic Variability and Drug Interaction Risk Using Omics-Based Biomarkers. [PDF]

Clin Transl Sci
ABSTRACT Interindividual variability in drug pharmacokinetics and susceptibility to drug–drug interactions remain major barriers in precision dosing, particularly for narrow therapeutic index drugs. While genetic factors contribute, much variability arises from dynamic influences such as physiology, disease, age, diet, microbiome, and concomitant ...
Prasad B.
europepmc   +2 more sources

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

Highly sensitive quantification of key regulatory oxysterols in biological samples by LC-ESI-MS/MSs⃞

Journal of Lipid Research, 2009
We describe a highly sensitive and specific method for the quantification of key regulatory oxysterols in biological samples. This method is based upon a stable isotope dilution technique by liquid chromatography-tandem mass spectrometry (LC-MS/MS ...
Akira Honda, Kouwa Yamashita, Takashi Hara, Tadashi Ikegami, Teruo Miyazaki, Mutsumi Shirai, Guorong Xu, Mitsuteru Numazawa, Yasushi Matsuzaki   +8 more
doaj   +1 more source

Prediction of pyrotinib exposure based on physiologically-based pharmacokinetic model and endogenous biomarker

Frontiers in Pharmacology, 2022
Pyrotinib, a novel irreversible epidermal growth factor receptor dual tyrosine kinase inhibitor, is mainly (about 90%) eliminated through cytochrome P450 (CYP) 3A mediated metabolism in vivo.
Miao Zhang, Miao Zhang, Miao Zhang, Zhiheng Yu, Zhiheng Yu, Zhiheng Yu, Xueting Yao, Xueting Yao, Zihan Lei, Zihan Lei, Zihan Lei, Kaijing Zhao, Wenqian Wang, Xue Zhang, Xijing Chen, Dongyang Liu, Dongyang Liu   +16 more
doaj   +1 more source

Effect of CYP3A4 metabolism on sex differences in the pharmacokinetics and pharmacodynamics of zolpidem

Scientific Reports, 2021
To investigate pharmacokinetic and pharmacodynamic differences of zolpidem between males and females and their causes, including CYP3A4 activity. A single oral dose of zolpidem (10 mg) was administered to 15 male and 15 female healthy subjects.
Seonghae Yoon, Seongmee Jeong, Eben Jung, Ki Soon Kim, Inseung Jeon, Yujin Lee, Joo-Youn Cho, Woo-Yong Oh, Jae-Yong Chung   +8 more
doaj   +1 more source

Effect of Once-Daily Macitentan 75 mg on the Pharmacokinetics of Sildenafil, Riociguat, or Rosuvastatin in Healthy Male Participants. [PDF]

J Clin Pharmacol
Abstract Macitentan is an oral, dual ETA/ETB endothelin receptor antagonist, currently approved in adults for the treatment of pulmonary arterial hypertension (PAH) at a once‐daily dose of 10 mg. Pre‐clinical and clinical data suggest that greater ETB receptor inhibition may result in greater efficacy.
Csonka D, Gargano C, Goyal N, De Meulder M, Yartsev V, Ruixo JJP.   +5 more
europepmc   +2 more sources

PBPK modeling to predict drug‐drug interactions of ivosidenib as a perpetrator in cancer patients and qualification of the Simcyp platform for CYP3A4 induction

CPT: Pharmacometrics & Systems Pharmacology, 2021
Ivosidenib is a potent, targeted, orally active, small‐molecule inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) that has been approved in the United States for the treatment of adults with newly diagnosed acute myeloid leukemia (AML) who are ...
Jayaprakasam Bolleddula, Alice Ke, Hua Yang, Chandra Prakash   +3 more
doaj   +1 more source