Results 1 to 10 of about 20,150 (206)

Efavirenz and CYP2C9 Genetic Polymorphisms Reduce CYP2C9 Activity in Healthy Participants [PDF]

open access: yesClinical and Translational Science
Efavirenz's effects on cytochrome P450 2C9 (CYP2C9) activity have not been formally characterized in vivo. We conducted the first clinical drug–drug interaction (DDI) study to test the effect of chronic efavirenz dosing on CYP2C9 activity, using ...
Jason D. Kim   +4 more
doaj   +2 more sources

Selection of an Optimal Metabolic Model for Accurately Predicting the Hepatic Clearance of Albumin-Binding-Sensitive Drugs [PDF]

open access: yesPharmaceuticals
Background/Objectives: Hepatic clearance is important in determining clinical drug administration strategies. Achieving accurate hepatic clearance predictions through in vitro-to-in vivo extrapolation (IVIVE) relies on appropriate model selection, which ...
Ren-Jong Liang   +7 more
doaj   +2 more sources

Live Cell Monitoring of Phosphodiesterase Inhibition by Sulfonylurea Drugs [PDF]

open access: yesBiomolecules
Sulfonylureas (SUs) are a class of antidiabetic drugs widely used in the management of diabetes mellitus type 2. They promote insulin secretion by inhibiting the ATP-sensitive potassium channel in pancreatic β-cells.
Filip Berisha   +2 more
doaj   +2 more sources

Development and Validation of a Quantitative LC-MS/MS Method for Measuring CYP4V2 Enzyme Activity via 12-Hydroxylauric Acid in rAAV-hCYP4V2 Gene Therapy Products [PDF]

open access: yesMolecules
Bietti crystalline dystrophy (BCD) is a hereditary retinal disease caused by loss-of-function mutations in the CYP4V2 gene. Gene replacement therapy using rAAV-hCYP4V2 represents a promising therapeutic strategy, requiring robust bioassays for product ...
Ge Ren   +8 more
doaj   +2 more sources

Identification and Enzymatic Activity Evaluation of a Novel CYP2C9 Allelic Variant Discovered in a Patient

open access: yesFrontiers in Pharmacology, 2021
Warfarin is a widely prescribed anticoagulant but the doses required to attain the optimum therapeutic effect exhibit dramatic inter-individual variability. Pharmacogenomics-guided warfarin dosing has been recommended to improve safety and effectiveness.
Xiao-Yang Zhou   +14 more
doaj   +1 more source

Solubility Enhancement of Antidiabetic Drugs Using a Co‐Crystallization Approach

open access: yesChemistryOpen, 2021
The co‐crystallization approach has been used to enhance specific desirable properties of active pharmaceutical ingredients (APIs) such as solubility, dissolution rate, and stability.
Dr. Eustina Batisai
doaj   +1 more source

Gut microbiota and host Cyp450s co-contribute to pharmacokinetic variability in mice with non-alcoholic steatohepatitis: Effects vary from drug to drug

open access: yesJournal of Advanced Research, 2022
Introduction: Pharmacokinetic variability in disease state is common in clinical practice, but its underlying mechanism remains unclear. Recently, gut microbiota has been considered to be pharmacokinetically equivalent to the host liver.
Jing Guo   +9 more
doaj   +1 more source

Inhibition and Induction by Poziotinib of Different Rat Cytochrome P450 Enzymes In Vivo and in an In Vitro Cocktail Method

open access: yesFrontiers in Pharmacology, 2021
Poziotinib is an orally active, irreversible, pan-HER tyrosine kinase inhibitor used to treat non-small cell lung cancer, breast cancer, and gastric cancer.
Jinhui Wang   +10 more
doaj   +1 more source

ATP-gated potassium channels contribute to ketogenic diet-mediated analgesia in mice

open access: yesNeurobiology of Pain, 2023
Chronic pain is a substantial health burden and options for treating chronic pain remain minimally effective. Ketogenic diets are emerging as well-tolerated, effective therapeutic strategies in preclinical models of chronic pain, especially diabetic ...
Jonathan D. Enders   +7 more
doaj   +1 more source

Quantitation of Diclofenac, Tolbutamide, and Warfarin as Typical CYP2C9 Substrates in Rat Plasma by UPLC-MS/MS and Its Application to Evaluate Linderane-Mediated Herb-Drug Interactions

open access: yesJournal of Analytical Methods in Chemistry, 2022
Linderane (LDR), the main active and distinctive component of L. aggregate, is a mechanism-based inactivator of CYP2C9 in vitro, indicating the occurrence of herb-drug interactions.
Tingting Zhang   +4 more
doaj   +1 more source

Home - About - Disclaimer - Privacy