Tyrosine Kinase Inhibitors. 17. Irreversible Inhibitors of the Epidermal Growth Factor Receptor: 4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido[3,2-d] …
4-Anilinoquinazoline- and 4-anilinopyrido[3,2-d]pyrimidine-6-acrylamides substituted with
solubilizing 7-alkylamine or 7-alkoxyamine side chains were prepared by reaction of the …
solubilizing 7-alkylamine or 7-alkoxyamine side chains were prepared by reaction of the …
Development of a new permeability assay using low‐efflux MDCKII cells
…, RE Davidson, R Smith, EL Reyner… - Journal of …, 2011 - Elsevier
Permeability is an important property of drug candidates. The Madin–Darby canine kidney
cell line (MDCK) permeability assay is widely used and the primary concern of using MDCK …
cell line (MDCK) permeability assay is widely used and the primary concern of using MDCK …
Comparison of Intestinal Permeabilities Determined in Multiple in Vitro and in Situ Models: Relationship to Absorption in Humans
BH Stewart, OH Chan, RH Lu, EL Reyner… - Pharmaceutical …, 1995 - Springer
In vitro and in situ experimental models that are descriptive of drug absorption in vivo are
valuable tools in the discovery of new chemical entities that are bioavailable after oral …
valuable tools in the discovery of new chemical entities that are bioavailable after oral …
Atorvastatin coadministration may increase digoxin concentrations by inhibition of intestinal P‐glycoprotein‐mediated secretion
…, BH Stewart, X Wu, EL Reyner… - The Journal of …, 2000 - Wiley Online Library
The effect of atorvastatin on digoxin pharmacokinetics was assessed in 24 healthy volunteers
in two studies. Subjects received 0.25 mg digoxin daily for 20 days, administered alone for …
in two studies. Subjects received 0.25 mg digoxin daily for 20 days, administered alone for …
Variability in P-glycoprotein inhibitory potency (IC50) using various in vitro experimental systems: implications for universal digoxin drug-drug interaction risk …
…, C Lee, J Palm, YA Pak, ES Perloff, E Reyner… - Drug metabolism and …, 2013 - ASPET
A P-glycoprotein (P-gp) IC 50 working group was established with 23 participating
pharmaceutical and contract research laboratories and one academic institution to assess …
pharmaceutical and contract research laboratories and one academic institution to assess …
Design of a Potent Combined Pseudopeptide Endothelin-A/Endothelin-B Receptor Antagonist, Ac-dBhg16-Leu-Asp-Ile-[NMe]Ile-Trp21 (PD 156252): Examination …
…, SJ Haleen, DM Walker, EL Reyner… - Journal of medicinal …, 1997 - ACS Publications
The endothelins (ETs) are a family of bicyclic 21-amino acid peptides that are potent and
prolonged vasoconstrictors. It has been shown that highly potent combined ET A /ET B receptor …
prolonged vasoconstrictors. It has been shown that highly potent combined ET A /ET B receptor …
P-glycoprotein related drug interactions: clinical importance and a consideration of disease states
CA Lee, JA Cook, EL Reyner… - Expert opinion on drug …, 2010 - Taylor & Francis
Importance of the field: P-glycoprotein (P-gp) is the most characterized drug transporter in
terms of its clinical relevance for pharmacokinetic disposition and interaction with other …
terms of its clinical relevance for pharmacokinetic disposition and interaction with other …
Digoxin is not a substrate for organic anion-transporting polypeptide transporters OATP1A2, OATP1B1, OATP1B3, and OATP2B1 but is a substrate for a sodium …
…, L Chen, H Ellens, B Hirakawa, EL Reyner… - Drug metabolism and …, 2011 - ASPET
Digoxin, an orally administered cardiac glycoside cardiovascular drug, has a narrow
therapeutic window. Circulating digoxin levels (maximal concentration of ∼1.5 ng/ml) require …
therapeutic window. Circulating digoxin levels (maximal concentration of ∼1.5 ng/ml) require …
Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation
…, RA Ferre, S Nukui, M Ornelas, E Reyner - Bioorganic & medicinal …, 2010 - Elsevier
A novel series of potent thioether benzenesulfonamide inhibitors of carbonic anhydrases II
and IV was discovered using structure-based drug design. Synthesis, structure–activity …
and IV was discovered using structure-based drug design. Synthesis, structure–activity …
In vitro characterization of axitinib interactions with human efflux and hepatic uptake transporters: implications for disposition and drug interactions
EL Reyner, S Sevidal, MA West… - Drug Metabolism and …, 2013 - ASPET
Axitinib is an inhibitor of tyrosine kinase vascular endothelin growth factor receptors 1, 2, and
3. The ATP-binding cassette (ABC) and solute carrier (SLC) transport properties of axitinib …
3. The ATP-binding cassette (ABC) and solute carrier (SLC) transport properties of axitinib …