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Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs
TLDR
The findings explain some of the side effects in patients treated with a combination of carcinostatics and P-glycoprotein inhibitors and indicate that these inhibitors might be useful in selectively enhancing the access of a range of drugs to the brain. Expand
Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan.
TLDR
Bcrp1 mediates apically directed drug transport, appears to reduce drug bioavailability, and protects fetuses against drugs, and it is proposed that strategic application of BCRP inhibitors may lead to more effective oral chemotherapy with topotecan or other B CRP substrate drugs. Expand
The breast cancer resistance protein protects against a major chlorophyll-derived dietary phototoxin and protoporphyria
TLDR
The results indicate that humans or animals with low or absent BCRP activity may be at increased risk for developing protoporphyria and diet-dependent phototoxicity and provide a striking illustration of the importance of drug transporters in protection from toxicity of normal food constituents. Expand
An update on in vitro test methods in human hepatic drug biotransformation research: pros and cons.
TLDR
The practical aspects of selected in vitro human liver models are described and several more or less serious specific drawbacks for each model are described which prevents their widespread use and acceptance by the regulatory authorities as an alternative for in vivo screening. Expand
Multidrug-resistance protein 5 is a multispecific organic anion transporter able to transport nucleotide analogs.
TLDR
It is speculated that MRP5 might play a role in some cases of unexplained resistance to thiopurines in acute lymphoblastic leukemia and/or to antiretroviral nucleoside analogs in HIV-infected patients. Expand
Increased sensitivity to anticancer drugs and decreased inflammatory response in mice lacking the multidrug resistance-associated protein
TLDR
The results suggest that this ubiquitous GS-X pump, which mediates the cellular excretion of many drugs, glutathione S-conjugates of lipophilic xenobiotics and endogenous cysteinyl leukotrienes, is dispensable in mice, making treatment of MDR with MRP-specific reversal agents potentially feasible. Expand
Clinical Pharmacokinetics of Therapeutic Monoclonal Antibodies
TLDR
The parenteral administration, slow tissue distribution and long elimination half-life are the most pronounced clinical pharmacokinetic characteristics of mAbs. Expand
Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918.
TLDR
It is concluded that the affinities of topoisomerase I drugs for BCRP are, in decreasing order: SN-38 > topotecan > 9-aminocamptothecin > CPT-11 > NX211 > DX8951f > BNP1350 • GF120918. Expand
Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine.
TLDR
It is concluded that P-glycoprotein limits the oral uptake of paclitaxel and mediates direct excretion of the drug from the systemic circulation into the intestinal lumen. Expand
Piraña and PCluster: A modeling environment and cluster infrastructure for NONMEM
TLDR
A graphical user interface, Piraña, was developed that offers a complete modeling environment for NONMEM, enabling both novice and advanced users to increase efficiency of their workflow. Expand
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