Results 81 to 90 of about 43,637 (267)

Effects of psoralen on the pharmacokinetics of anastrozole in rats

open access: yesPharmaceutical Biology, 2018
Context: Psoralen and anastrozole are always used together for breast cancer patients in Chinese clinics. Objective: This study investigates the effects of psoralen on the pharmacokinetics of anastrozole in rats and its potential mechanism. Materials and
Yuzhu Zhang   +4 more
doaj   +1 more source

Effect of CYP3A4 Methylation on Tacrolimus Pharmacokinetics

open access: yesTherapeutic Drug Monitoring
Background: Common genetic variants in CYP3A4 together only explain a limited amount of the variability in tacrolimus clearance. This cross-sectional study aimed to explore the extent to which pharmacokinetic variability can be explained by ...
Koudijs, K.K.M.   +7 more
openaire   +4 more sources

Repurposing Drugs for Malaria through a Human Dose Prediction: A Case Study with Berzosertib

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
Repurposing drugs whose clinical safety has been established offers a valuable approach to reduce the cost and time associated with the development of new drugs for malaria. Here, we investigate the potential to repurpose the anticancer kinase inhibitor berzosertib for the treatment of malaria, by assessing whether a predicted efficacious human dose ...
Devasha Redhi   +5 more
wiley   +1 more source

Characterization of Lysosomal Hydrolases and Transporters and Their Age‐Dependent Variability: Relevance to Drug Metabolism and Transport of Small Molecule and Biologic Drugs

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
Lysosomes play a key role in the accumulation, catabolism, and transport of endogenous and exogenous metabolites and proteins and are involved in drug metabolism and prodrug activation. However, the protein abundance and interindividual variability of lysosomal drug‐metabolizing enzymes and transporters (DMETs) remain underexplored.
Darshak Gadara   +20 more
wiley   +1 more source

Functional assessment of CYP3A4 allelic variants on lidocaine metabolism in vitro

open access: yesDrug Design, Development and Therapy, 2017
Ping Fang,1 Peng-fei Tang,1 Ren-ai Xu,2 Xiang Zheng,1 Jian Wen,1 Su-su Bao,1 Jian-ping Cai,3 Guo-xin Hu1 1Department of Pharmacology, School of Pharmacy, Wenzhou Medical University, 2Department of Pharmacy, The First Affiliated Hospital of Wenzhou ...
Fang P   +7 more
doaj  

Clinical Characterization of Enzyme and Transporter Precipitants to Evaluate Drug–Drug Interactions for Orforglipron, a Small Molecule Glucagon‐Like Peptide‐1 Receptor Agonist

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
Orforglipron is an orally administered, small‐molecule glucagon‐like peptide‐1 receptor agonist in clinical development for the treatment of type 2 diabetes and obesity. Orforglipron is a substrate of CYP3A4, organic anion transporting polypeptides (OATPs) 1B/1B3, and P‐glycoprotein (P‐gp); however, precipitants commonly used to define these mechanisms
Bridget L. Morse   +7 more
wiley   +1 more source

The Effect of Dicloxacillin Administration on Pharmacokinetics of Narrow Therapeutic Window Drugs: Phenytoin and Warfarin

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
Dicloxacillin is a penicillinase‐resistant beta‐lactam antibiotic and potent activator of the Pregnane X receptor (PXR), known to induce CYP2C9, CYP2C19, and CYP3A4 activity. Clinical data suggest it reduces anticoagulation in warfarin‐treated patients and increases the risk of thromboembolic events.
Chanan Shaul   +5 more
wiley   +1 more source

Integrated assessment of rifampicin‐mediated induction of transporters and drug‐metabolizing enzymes in a long‐term human liver tissue chip system

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
Rifampicin is a prototypical clinical inducer used in drug–drug interaction (DDI) studies. However, the clinical relevance and predictability of rifampicin‐mediated hepatic transporter induction remain poorly defined. Conventional hepatocyte culture models fail to capture clinically relevant regulation of transporters and drug‐metabolizing enzymes ...
Mattie E. Hartauer   +9 more
wiley   +1 more source

Influence of verapamil on the pharmacokinetics of oridonin in rats

open access: yesPharmaceutical Biology, 2019
Context: Oridonin has been traditionally used in Chinese treatment of various cancers, but its poor bioavailability limits its therapeutic uses. Verapamil can enhance the absorption of some drugs with poor oral bioavailability.
Jing Liu   +4 more
doaj   +1 more source

CYP3A4 Inhibitors Isolated from Licorice

open access: yesBiological and Pharmaceutical Bulletin, 2005
The extract of licorice (Glycyrrhiza uralensis FISHER, Leguminosae) showed CYP3A4 inhibitory activity with the IC50 value of 0.022 mg/ml. Bioassay-guided purification afforded nine compounds, 3-(p-hydroxyphenyl)propionic acid (1), isoliquiritigenin (2), (3R)-vestitol (3), licopyranocoumarin (4), 4-hydroxyguaiacol apioglucoside (5), liquiritin (6 ...
Tsukamoto, Sachiko   +5 more
openaire   +3 more sources

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