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Download e-book for iPad: Drug Transporters: Volume 1: Role and Importance in ADME and by Glynis Nicholls, Kuresh Youdim (eds.)

By Glynis Nicholls, Kuresh Youdim (eds.)

ISBN-10: 1782620699

ISBN-13: 9781782620693

Understanding and quantifying the results of membrane transporters in the human physique is key for modulating drug security and drug efficacy. during this first quantity on Drug Transporters, the present wisdom and methods within the transporter sciences and their relatives to drug metabolism and pharmacokinetics are comprehensively reviewed. the second one quantity of the booklet is in particular devoted to rising technology and applied sciences, highlighting strength parts for destiny advances in the drug transporter field.


The subject matters lined in either volumes make sure that all proper points of transporters are defined around the drug improvement strategy, from in silico types and preclinical instruments via to the capability effect of transporters within the medical institution. Contributions are incorporated from professional leaders within the box, at-the-bench commercial scientists, popular lecturers and overseas regulators. Case reviews and rising advancements are highlighted, including the benefits and obstacles of the on hand tools and instruments, and huge references to reports on particular in-depth subject matters also are integrated for these wishing to pursue their wisdom additional.


As such, this article serves as an important guide of knowledge for postgraduate scholars, lecturers, business scientists and regulators who desire to comprehend the function of transporters in absorption, distribution, metabolism, and excretion procedures. moreover, it's also an invaluable reference instrument at the types and calculations essential to are expecting their impact on human pharmacokinetics and pharmacodynamics.

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Extra info for Drug Transporters: Volume 1: Role and Importance in ADME and Drug Development

Example text

Typically, this is achieved by nuclear receptors sensing intracellular ligand levels. These ligands can be drugs, environmental chemicals or endogenous ligands such as bile salts. 172 This is discussed further in Drug Transporters: Volume 2: Recent Advances and Emerging Technologies, Chapter 2. 2 Pharmacogenetics Several genetic polymorphisms (gene sequence variations that occur within a population) of transporter genes are known, some of which may cause disease, while others may have no obvious impact but are capable of influencing drug response (by increasing or decreasing the activity of the transporter protein, or by lack of expression).

208,209 However, considerable knowledge has been obtained for species used in drug development, such as mice and rats. 199,210 In disease states, transporter expression levels may be affected secondary to an underlying disease. 4 Dietary, Environmental and Lifestyle Factors Dietary effects on drug PK are well documented in the literature. Mechanisms responsible for food–drug interactions may include physiological alterations in intestinal motility, gastric pH, gastric emptying or modulation of disposition pathways by dietary constituents.

1b–f). 2B). Members of the SLC family of transporters can belong to either of these classes of passive or active transport. 2B). The driving forces for some transporters have been demonstrated and, although the principles of primary, secondary or tertiary transport discussed below are valid, the precise mechanisms for many transporters remain unknown, particularly for SLCs. 2B). 1c). 1d combined). g. 1e). 116 The driving force is the sodium gradient, which is A. Passive/Facilitated Transport High Low B.

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Drug Transporters: Volume 1: Role and Importance in ADME and Drug Development by Glynis Nicholls, Kuresh Youdim (eds.)


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