Drug Metabolism in Drug Design and Development Basic Concepts and Practice
This chapter provides our current understanding of transporter types, methods involved in the assessment of their function, and ...
cell. The gene nomenclature, protein name, tissue distribution, driven force, substrate properties and the substrates, inhibitor ...
TABLE 6.1 Tissue distribution and substrate properties of major ABC and SLC transporters.Gene Protein name Tissue distribution S ...
Cisplatin is a substrate for MRP2 but not for MRP1.Folic acid and monovalentbile salts such as cholate,taurocholate, andglycocho ...
TABLE 6.1 ( Continued ) Gene Protein name Tissue distribution Substrate properties Selected inhibitor and (inducer) Driving forc ...
SLC10A2 ASBT Intestine, kidney Bile salts, such as taurocholate All major bile salts, BQ-123, CsA SLC15A1 PEPT1 Intestine, Kidne ...
TABLE 6.1 ( Continued ) Gene Protein name Tissue distribution Substrate properties Selected inhibitor and (inducer) Driving forc ...
TEA, carnitine, quinidine, verapamil SLC22A5 OCTN2, CT1 Kidney, skeletal muscle, prostate,lung, heart, pancreas,small intestine, ...
TABLE 6.1 ( Continued ) Gene Protein name Tissue distribution Substrate properties Selected inhibitor and (inducer) Driving forc ...
ivermectin, loperamide and UK-224671 (P-gp substrates (Chen et al., 2003a)), as well as topotecan, nitrofurantoin, ME-3229, GV-1 ...
excretion was not markedly different in wt and Mdr1a(-/-) mice. After IV administration of paclitaxel (10 mg/kg) to mice with a ...
the liver (Shitara and Sugiyama, 2003). Metformin, a biguanide antidiabetic drug, is distributed into the liver via Oct1 and int ...
6.2.3 Transporters in Drug Metabolism It has been recognized that there is a huge overlap of the substrate specificity and tissu ...
steady state the hepatic intrinsic clearance of pravastatin, a substrate for OATP2 and MRP2 (Tokui et al., 1999; Yamazaki et al. ...
where FR,fu, GFR, and CLsecare the reabsorbed fraction, protein unbound fraction in the blood, glomerular filtration rate and se ...
lactating woman was reported to be secreted into human milk (Merino et al., 2005). The underlying mechanism was demonstrated in ...
Many antiviral drugs (e.g., fialuridine; FIAU) produce clinically significant mitochondrial toxicity that limits their dosing or ...
CsA, PSC833, and quinine showed some overall survival benefit in several anticancer drug treatments in P-gp positive patients wi ...
TABLE 6.2 Outcome of some of the Phase III clinical trials with ABC transporter inhibitors.Year Trialgroup Number of patients Ca ...
(Grem, 1992), gemcitabine (Mackey et al., 1998b), 6-mercaptopurine (Fotoohi et al., 2006), and 6-thiolguanine (Fotoohi et al., 2 ...
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