Circulating biomarkers instead of genotyping to establish metabolizer phenotypes

R Tremmel, U Hofmann, M Haag… - Annual Review of …, 2024 - annualreviews.org
Pharmacogenomics (PGx) enables personalized treatment for the prediction of drug
response and to avoid adverse drug reactions. Currently, PGx mainly relies on the genetic …

Physiologically based pharmacokinetic (PBPK) modeling of flurbiprofen in different CYP2C9 genotypes

SS Whang, CK Cho, EH Jung, P Kang, HJ Park… - Archives of Pharmacal …, 2022 - Springer
The aim of this study was to establish the physiologically based pharmacokinetic (PBPK)
model of flurbiprofen related to CYP2C9 genetic polymorphism and describe the …

Physiologically‐based pharmacokinetic modeling of quinidine to establish a CYP3A4, P‐gp, and CYP2D6 drug–drug–gene interaction network

D Feick, S Rüdesheim, FZ Marok… - CPT …, 2023 - Wiley Online Library
The antiarrhythmic agent quinidine is a potent inhibitor of cytochrome P450 (CYP) 2D6 and
P‐glycoprotein (P‐gp) and is therefore recommended for use in clinical drug–drug …

[HTML][HTML] Physiologically based pharmacokinetic (PBPK) modeling of the role of CYP2D6 polymorphism for metabolic phenotyping with dextromethorphan

J Grzegorzewski, J Brandhorst, M König - Frontiers in Pharmacology, 2022 - frontiersin.org
The cytochrome P450 2D6 (CYP2D6) is a key xenobiotic-metabolizing enzyme involved in
the clearance of many drugs. Genetic polymorphisms in CYP2D6 contribute to the large inter …

Pharmacogenomic variation in the Malagasy population: implications for the antimalarial drug primaquine metabolism

EY Cramer, J Bartlett, ER Chan, A Gaedigk… - …, 2023 - Future Medicine
Aim: Antimalarial primaquine (PQ) eliminates liver hypnozoites of Plasmodium vivax.
CYP2D6 gene variation contributes to PQ therapeutic failure. Additional gene variation may …

[HTML][HTML] Physiologically based pharmacokinetic modeling to describe the CYP2D6 activity score-dependent metabolism of paroxetine, atomoxetine and risperidone

S Rüdesheim, D Selzer, T Mürdter, S Igel, R Kerb… - Pharmaceutics, 2022 - mdpi.com
The cytochrome P450 2D6 (CYP2D6) genotype is the single most important determinant of
CYP2D6 activity as well as interindividual and interpopulation variability in CYP2D6 activity …

A commentary on the use of pharmacoenhancers in the pharmaceutical industry and the implication for DMPK drug discovery strategies

V Martins, L Fazal, A Oganesian, A Shah, J Stow… - Xenobiotica, 2022 - Taylor & Francis
Paxlovid, a drug combining nirmatrelvir and ritonavir, was designed for the treatment of
COVID-19 and its rapid development has led to emergency use approval by the FDA to …

[HTML][HTML] Prediction of Drug–Drug–Gene Interaction Scenarios of (E)-Clomiphene and Its Metabolites Using Physiologically Based Pharmacokinetic Modeling

C Kovar, L Kovar, S Rüdesheim, D Selzer, B Ganchev… - Pharmaceutics, 2022 - mdpi.com
Clomiphene, a selective estrogen receptor modulator (SERM), has been used for the
treatment of anovulation for more than 50 years. However, since (E)-clomiphene ((E)-Clom) …

[HTML][HTML] Hippophae rhamnoides reverses decreased CYP2D6 expression in rats with BCG-induced liver injury

H Zou, P Hao, Y Cao, L Li, R Ding, X Bai, Y Xue - Scientific Reports, 2023 - nature.com
In this study, we investigated the effect of Hippophae rhamnoides L.(HRP) on the activity of
CYP2D6 via the CAMP/PKA/NF-κB pathway in rats with Bacille Calmette–Guerin (BCG) …

Physiologically based pharmacokinetic (PBPK) modeling of pitavastatin in relation to SLCO1B1 genetic polymorphism

CK Cho, JY Mo, E Ko, P Kang, CG Jang, SY Lee… - Archives of Pharmacal …, 2024 - Springer
Pitavastatin, a potent 3-hydroxymethylglutaryl coenzyme A reductase inhibitor, is indicated
for the treatment of hypercholesterolemia and mixed dyslipidemia. Hepatic uptake of …