Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4

CL Cummins, W Jacobsen, LZ Benet - Journal of Pharmacology and …, 2002 - ASPET
Drug efflux by intestinal P-glycoprotein (P-gp) is known to decrease the oral bioavailability of
many CYP3A4 substrates. We hypothesized that the interplay occurring between P-gp and …

Mechanisms of clinically relevant drug interactions associated with tacrolimus

U Christians, W Jacobsen, LZ Benet… - Clinical pharmacokinetics, 2002 - Springer
The clinical management of tacrolimus, a macrolide used as immunosuppressant after
transplantation, is complicated by its narrow therapeutic index in combination with inter- and …

Mechanisms controlling leaf retention of agricultural spray solutions

W Wirth, S Storp, W Jacobsen - Pesticide science, 1991 - Wiley Online Library
Active ingredient deposition as a whole during foliar spray application was studied by means
of microscopic and macroscopic methods. High‐speed photography of the impact of spray …

Lactonization is the critical first step in the disposition of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor atorvastatin

W Jacobsen, B Kuhn, A Soldner, G Kirchner… - Drug Metabolism and …, 2000 - ASPET
In an in vitro study, we compared the cytochrome P450 (CYP)-dependent metabolism and
drug interactions of the acid and lactone forms of the 3-hydroxy-3-methylglutaryl (HMG)-CoA …

Metabolism and drug interactions of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors in transplant patients: are the statins mechanistically similar?

U Christians, W Jacobsen, LC Floren - Pharmacology & therapeutics, 1998 - Elsevier
3-Hydroxy-3-methylglutaryl coenzyme A reductase (EC 1.1.1.88) inhibitors are the most
effective drugs to lower cholesterol in transplant patients. However, immunosuppressants and …

Automated, fast and sensitive quantification of drugs in blood by liquid chromatography–mass spectrometry with on-line extraction: immunosuppressants

U Christians, W Jacobsen, N Serkova, LZ Benet… - … of Chromatography B …, 2000 - Elsevier
We developed a universal LC–mass spectrometry assay with automated online extraction (LC/LC–MS)
to quantify the immunosuppressants cyclosporine, tacrolimus, sirolimus and SDZ-…

Comparison of cytochrome P-450-dependent metabolism and drug interactions of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitors lovastatin and pravastatin …

W Jacobsen, G Kirchner, K Hallensleben… - Drug metabolism and …, 1999 - ASPET
In an in vitro study, the cytochrome P-450 3A (CYP3A)-dependent metabolism and drug
interactions of the 3-hydroxy-3-methylglutaryl-Co A reductase inhibitors lovastatin and …

CYP3A4-transfected Caco-2 cells as a tool for understanding biochemical absorption barriers: studies with sirolimus and midazolam

CL Cummins, W Jacobsen, U Christians… - Journal of Pharmacology …, 2004 - ASPET
CYP3A4-transfected Caco-2 cells were used as an in vitro system to predict the importance
of drug metabolism and transport on overall drug absorption. We examined the transport and …

In vitro evaluation of the disposition of a novel cysteine protease inhibitor

W Jacobsen, U Christians, LZ Benet - Drug metabolism and disposition, 2000 - ASPET
K11777 (N-methyl-piperazine-Phe-homoPhe-vinylsulfone-phenyl) is a potent, irreversible
cysteine protease inhibitor. Its therapeutic targets are cruzain, a cysteine protease of the …

Sirolimus, but not the structurally related RAD (everolimus), enhances the negative effects of cyclosporine on mitochondrial metabolism in the rat brain

N Serkova, W Jacobsen, CU Niemann… - British journal of …, 2001 - Wiley Online Library
Clinical studies have shown enhancement of cyclosporine toxicity when co‐administered with
the immunosuppressant sirolimus. We evaluated the biochemical mechanisms underlying …