Results 61 to 70 of about 16,133 (222)

Effect of developmental changes on pharmacokinetics of drugs used in the treatment of infant acute lymphoblastic leukaemia—A comprehensive review

British Journal of Clinical Pharmacology, EarlyView.
While the event‐free survival (EFS) of children treated for acute lymphoblastic leukaemia (ALL) has improved greatly in the last decades, the EFS for patients diagnosed with ALL before the age of one is still under 50%. This outcome further decreases when infants have a rearrangement in the gene encoding histone‐lysine N‐methyltransferase 2A (KMT2A ...
Tirsa de Kluis, Leiah J. Brigitha, Lidwien M. Hanff, Alwin D. R. Huitema, Inge M. van der Sluis, Meta H. M. Diekstra   +5 more
wiley   +1 more source

Low‐dose cannabidiol increases plasma concentrations of amitriptyline: A clinical drug–drug interaction study

British Journal of Clinical Pharmacology, EarlyView.
Abstract Aims Cannabidiol (CBD), the main non‐intoxicating compound from the cannabis plant, is regularly used by patients with chronic pain who also take analgesics. CBD has previously been shown to inhibit CYP‐mediated drug metabolism. This study aimed to characterize the potential pharmacokinetic interaction of CBD with amitriptyline and tramadol ...
Andriy A. Gorbenko, Titiaan E. Post, Pamela K. Strugala, Erica S. Klaassen, Linda E. Klumpers, Saco J. de Visser, Cristina Sempio, Jost Klawitter, Jules A. A. C. Heuberger, Geert J. Groeneveld   +9 more
wiley   +1 more source

Pharmacogenetic CYP2B6 variants affect steroid hormone metabolism in human breast cancer cells

British Journal of Clinical Pharmacology, EarlyView.
Common genetic CYP2B6 variants correlate with adverse breast cancer outcome. The oestrogen metabolites estriol and 16‐epiestriol, which are formed downstream of CYP2B6‐catalysed 16α/β‐hydroxytestosterone, may be linked to elevated breast cancer risk and might increase due to the demonstrated CYP2B6 variants‐related metabolic shifts.
Marco Hoffmann, Julian Peter Müller, Stefan Düsterhöft, Sabrina Yamoune, Katja Susanne Just, Julia Carolin Stingl   +5 more
wiley   +1 more source

Constitutive androstane receptor 1 is constitutively bound to chromatin and ‘primed’ for transactivation in hepatocytes [PDF]

, 2018
The constitutive androstane receptor (CAR) is a xenobiotic sensor expressed in hepatocytes that activates genes involved in drug metabolism, lipid homeostasis, and cell proliferation.
Acosta-Jimenez, Lourdes, Ding, Shaohong, Gerard, Marie-Apolline, Henderson, Colin J., McMahon, Michael, Moggs, Jonathan G., Terranova, Remi, Vitobello, Antonio, Wolf, C. Ronald   +8 more
core   +2 more sources

Effect of carbamazepine on the pharmacokinetics of vepdegestrant, a PROteolysis TArgeting Chimera estrogen receptor degrader, in healthy adults

British Journal of Clinical Pharmacology, EarlyView.
Aim To evaluate the effects of carbamazepine, a strong cytochrome P450 (CYP)3A4 inducer, on the pharmacokinetics and safety of vepdegestrant, a PROteolysis TArgeting Chimera estrogen receptor degrader. Methods This was a phase 1, open‐label, fixed‐sequence, two‐period study in healthy adult participants.
Hechuan Wang, Jennifer A. Winton, Kyle T. Matschke, Alexandre Stouffs, Kimberly C. Lee, Yuanyuan Zhang, Wenlian Qiao, Weiwei Tan   +7 more
wiley   +1 more source

CYP2B6 and Bupropion’s Smoking-Cessation Pharmacology: The Role of Hydroxybupropion [PDF]

Clinical Pharmacology & Therapeutics, 2012
Bupropion is indicated to promote smoking cessation. Animal studies suggest that the pharmacologic activity of bupropion can be mediated by its major metabolite, hydroxybupropion. We measured plasma bupropion and its metabolite levels in a double-blind, placebo controlled, randomized smoking-cessation trial.
Zhu, AZX, Cox, LS, Nollen, N, Faseru, B, Okuyemi, KS, Ahluwalia, JS, Benowitz, NL, Tyndale, RF   +7 more
openaire   +4 more sources

Cross-species comparison of CAR-mediated procarcinogenic key events in a 3D liver microtissue model [PDF]

, 2019
Characterisation of the mode of action (MOA) of constitutive androstane receptor (CAR)-mediated rodent liver tumours involves measurement 5 key events including activation of the CAR receptor, altered gene expression, hepatocellular proliferation, clonal
Ball, Graeme, Beaumont, Bobby, Cowie, David, Currie, Richard, McInnes, Liz, Peffer, Rich, Plummer, Simon, Wallace, Stephanie, Wright, Jayne   +8 more
core   +2 more sources

Pharmacokinetics and pharmacodynamics of intravenous and oral (S)‐ketamine: Investigating metabolite contribution to subjective effects

British Journal of Clinical Pharmacology, EarlyView.
Aims Oral administration of (S)‐ketamine for treatment‐resistant depression (TRD), as alternative to the registered intranasal or off‐label intravenous administrations, has high potential. However, it is characterized by an extensive first‐pass metabolism, resulting in low (S)‐ketamine exposure and high levels of active metabolites, including (S ...
Marije E. Otto, Gabriël E. Jacobs, Joost C. van Mechelen, Laura G. J. M. Borghans, Johan G. C. van Hasselt, Linda B. S. Aulin   +5 more
wiley   +1 more source

Role of CYP2B6 pharmacogenomics in bupropion-mediated smoking cessation [PDF]

Journal of Clinical Pharmacy and Therapeutics, 2018
Pharmacogenomics holds promise in smoking cessation because of its potential to shed light on the complexity of drug metabolism and improve treatments using therapeutic agents. The cytochrome P450 2B6 gene (CYP2B6) encodes CYP2B6 enzyme that has been found to mediate the hydroxylation of bupropion, a smoking cessation aid.
Andrew X, Tran, Teresa T, Ho, Sheeba, Varghese Gupta   +2 more
openaire   +2 more sources

Physiologically‐based pharmacokinetic modelling of uridine 5′‐diphosphoglucorosultransferase (UGT) substrate drugs in pregnant women

British Journal of Clinical Pharmacology, EarlyView.
Aims While pregnancy‐related changes in phase I enzyme activity are well‐documented, less is known about the impact on phase II enzymes. This study aimed to test the hypothesis that changes in the pharmacokinetics (PK) of uridine 5′‐diphosphoglucuronosyltransferase (UGT) substrates during pregnancy result from altered enzyme expression or activity ...
William Saffaf, Ymke van der Velde, Paul R. V. Malik, Jelmer R. Prins, Sanne J. Gordijn, Daan J. Touw, Paola Mian   +6 more
wiley   +1 more source