ReviewBiochemical and Molecular Pharmacological Aspects of Transporters as Determinants of Drug Disposition
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Understanding peroral absorption: regulatory aspects and contemporary approaches to tackling solubility and permeability hurdles
2017, Acta Pharmaceutica Sinica BRelative contributions of presystemic and systemic peptidases to oral exposure of a novel metabotropic glutamate 2/3 receptor agonist (LY404039) after oral administration of prodrug Pomaglumetad methionil (LY2140023)
2015, Journal of Pharmaceutical SciencesCitation Excerpt :The most frequent treatment-related adverse events (≥10% incidence), following both treatments, were nervous system disorders, predominantly somnolence (which was reported as observational sleepiness and occurred predominantly during i.v. infusion). The general strategy of increasing the bioavailability of polar, pharmacologically active molecules that are recognized as peptide-like by human PEPT1 (SLC15A1) is well established and reflected in the therapeutic utility of cephalosporins and angiotensin-converting enzyme inhibitors.15,16 This approach has evolved to the design of ester prodrugs, such as valacyclovir, that are actively transported by PEPT1 and subsequently hydrolyzed by one or more abundant hydrolase enzymes in the enterocyte, liver, plasma, and most other tissues.17
Mechanistic interpretation of conventional Michaelis-Menten parameters in a transporter system
2014, European Journal of Pharmaceutical SciencesIntestinal drug transporters: An overview
2013, Advanced Drug Delivery ReviewsCitation Excerpt :Transporters are the gatekeepers for cells and organelles, controlling uptake and efflux of crucial compounds such as sugars, amino acids, nucleotides, inorganic ions and drugs [10]. Specific membrane transporters are expressed in the luminal and/or basolateral membranes of enterocytes, hepatocytes, renal tubular epithelial cells and other important barrier tissues, including the blood–brain barrier, blood–testis barrier and the placental barrier [11]. Transporter expression in the intestine and/or liver, the two major sites affecting how much of a drug will get into the systemic circulation after an oral dose, suggests that factors affecting their function will be important determinants of oral drug pharmacokinetics.
The promiscuous binding of pharmaceutical drugs and their transporter-mediated uptake into cells: What we (need to) know and how we can do so
2013, Drug Discovery TodayCitation Excerpt :In fact, as we discuss below, most proteins bind to multiple drugs and drug-like substances. However, we do not have to speculate whether it is ‘unlikely’ because we know the SLC families [220,221] and could determine, for each one, whether they do or do not transport a known drug (and note that new discoveries continue to emerge [222]), and very many do [1,5,99,223–225]. We would also point out, however, that this is not the correct question because, if even just one transporter type effected major flux for all anionic drugs and another type, say, for all cationic drugs, that alone would be sufficient to account for the transport of drugs by carriers rather than via trans-phospholipid diffusion.
Pharmaceutical drug transport: The issues and the implications that it is essentially carrier-mediated only
2011, Drug Discovery TodayCitation Excerpt :There is considerable and increasing evidence that drugs get into cells more or less solely by hitchhiking on carriers normally used for the transport of nutrients and intermediary metabolites [1–38].
This study was supported in part by a Grant-in-Aid for Scientific Research from MEXT (The Ministry of Education, Culture, Sports, Science, and Technology) of Japan, the “High-Tech Research Center” Project for Private Universities with matching fund subsidy from MEXT, 2004-2008, the “Open Research” Project for Private Universities with matching fund subsidy from MEXT, 2001-2005, and by grants from the Uehara Memorial Foundation, Takeda Science Foundation, and the Nagai Foundation, Tokyo.