Abbreviations

Adenosine triphosphate (ATP)-binding cassette transporter (gene superfamily)

ATP-binding cassette gene subfamily B

Gene encoding MDR1 or P-gp

Gene encoding BSEP

ATP-binding cassette gene subfamily C

Gene encoding MRP2

ATP-binding cassette gene subfamily G

Gene encoding BCRP

Absorption, distribution and elimination

Absorption, distribution, metabolism and elimination

Absorption, distribution, metabolism, elimination and toxicity

Adverse drug reaction

Aryl hydrocarbon receptor

Adenosine monophosphate

Active pharmaceutical ingredient

Aryl hydrocarbon nuclear translocator

Apical sodium dependent bile acid transporter

Adenosine triphosphate

Area under curve

Area under the first order moment curve

Bioavailability

Blood–brain barrier

Breast cancer resistance protein (gene ABCG2)

Biopharmaceutics classification system

Blood–cerebrospinal fluid barrier

Biopharmaceutics drug disposition classification system

Biliary excretion index

Brain like endothelial cell

Blood Retinal Barrier

Bile salt export pump (gene ABCB11)

human colon adenocarcinoma cell line

Constitutive androstane receptor (NR1I3)

Cholecystokinin-8

5-(and-6)-carboxy-2′,7′-dichloro-fluorescein

Cystic fibrosis transmembrane conductance regulator

Committee for Medicinal Products for Human Use

Chinese hamster ovary (cell line)

Conditionally immortalized proximal tubule epithelial cells

Clash-detection guided iterative search with rotamer relaxation

Clearance

Apical efflux clearance

Biliary clearance

Diffusional clearance

Active basolateral efflux clearance

Diffusional clearance in (i) or out (o) of the membrane

Intrinsic clearance

Passive clearance

Renal clearance

Active uptake clearance

Maximum observed blood concentration of drug

Substrate media concentration

Central nervous system

Concentrative nucleoside transporters (SLC28A subfamily)

Copy number variation

Concurrent medication

Canalicular membrane vesicles

Comparative molecular analysis

Comparative molecular similarity indices analysis

Chronic obstructive pulmonary disease

Choroid Plexus

Cluster regularly interspaced short palindromic repeats

Candidate selection

Cyclosporine A

Cerebrospinal fluid

Computed tomography

Clinical trial application

Common technical document

Cytochrome P450

Cytochrome P450 3A4

Dynamic contrast-enhanced magnetic resonance imaging

Drug–drug interaction

data independent acquisition

Drug induced liver injury

Drug metabolizing enzyme

Drug metabolism and pharmacokinetics

Deoxyribonucleic acid

Drug related material

Extracellular matrix

European Medicines Agency

Equilibrative nucleoside transporter (subfamily SLC29A)

Estradiol-17β-glucuronide

Endoplasmic reticulum

Embryonic stem cell

Estrone-1-sulfate

ethylene glycol tetraacetic acid

Equilibrative nucleoside transporter (SLC29A subfamily)

Bioavailability

Fraction of the dose that is absorbed from the intestinal lumen to the intestinal enterocytes

Fraction of the dose that escapes pre-systemic intestinal first pass elimination

Fumarylacetoacetate hydrolase

Foetal bovine serum

Fasted state simulated intestinal fluid

Fed state simulated intestinal fluid

(United States) Food and Drugs Administration

Fraction of dose absorbed

Fraction metabolized

Fraction transported

First time in human

Fraction unbound

Fraction unbound in blood

Farnesoid X receptor (NR1H4)

Grape fruit juice

Glomerular filtration rate

Gastro-intestinal tract

Glucose transporter

Genetically modified organism

glucocorticoid receptor (NR3C1)

Glutathione (reduced state)

Glutathione S-transferase enzyme

Human embryonic kidney cells

Human immunodeficiency virus

Human Genome Organisation Gene Nomenclature Committee

3-Hydroxy-3-methyl-glutaryl-Coenzyme A reductase

Hepatic nuclear factor 4alpha (NR2A1)

Human Genome Organisation

Inhibitor concentration

The concentration of inhibitor required to inhibit transport by 50%

injected dose

Immunohistochemistry

Maximum inhibitor concentration at the inlet to the liver

Investigational new drug

Induced pluripotent stem cell

Immediate release

brain interstitial fluid

International Transporter Consortium

In vitro–in vivo correlation

In vitro–in vivo extrapolation

Maximum number of APIs translocated across area per time by a given transporter

Absorption rate constant of the inhibitor

dissociation constant

Inhibitory constant

Michaelis constant in Michaelis–Menten kinetics (apparent)

Partition coefficient

l-type amino acid transporter

Liquid chromatography tandem mass spectrometry

Lethal dose

Lilly Laboratories Culture-Pig Kidney Type 1 (cell line)

logarithm of the partition coefficient, a measure of lipophilicity

Lead optimization and identification

Leukotriene C4

Liver X receptor (NR1H3)

Mass to charge ratio

Marketing authorization

Matrix assisted laser desorption ionization

Multidrug and toxin extrusion protein

Multidrug and toxin extrusion protein (gene SLC47A1)

Multidrug and toxin extrusion protein (gene SLC47A2)

Monocarboxylic acid transporter

Madin Darby canine kidney (cell line)

Madin Darby canine kidney, type II (cell line)

Multidrug resistance protein

Multidrug resistance protein 1 (also known as P-gp, gene ABCB1)

Ministry of Health, Labour and Welfare

Matrix metalloproteinases

1-methyl-4-phenylpyridinium

Model quality assessment programmes

Messenger riboxynucleic acid

Magnetic resonance imaging

Multidrug resistance associated protein

Multidrug resistance associated protein 2 (gene ABCC2)

Multidrug resistance associated protein 4 (gene ABCC4)

Molecular weight

Sodium dependent dicarboxylate transporter 3 (SLC13A3)

N-acetyltransferase

Nucleotide binding domain

New chemical entity

New drug application

Near infrared imaging

New molecular entity

Nuclear magnetic resonance

Sodium phosphate transporter 4

Nuclear receptor

Non-steroidal anti-inflammatory drug

Nephrogenic systemic fibrosis

Nutrient transporter

2-(2-nitro-4-fluoro-methylbenzoyl)-1,3-cyclohexanedione

Na-taurocholate co-transporting polypeptide

Number of hydrogen bond acceptors

Number of hydrogen bond donors

Organic anion transporter

Organic anion transporter 1 (gene SLC22A6)

Organic anion transporter 3 (gene SLC22A8)

Organic anion transporting polypeptide

Organic anion transporting polypeptide 1A2 (gene SLCO1A2)

Organic anion transporting polypeptide 1B1 (gene SLCO1B1)

Organic anion transporting polypeptide 1B3 (gene SLCO1B3)

Organic anion transporting polypeptide 2B1 (gene SLCO2B1)

Organic cation transporter

Organic cation transporter (gene SLC22A1)

Organic cation transporter (gene SLC22A2)

Organic cation/carnitine transporter

Organic cation/carnitine transporter 1 (gene SLC22A4)

Organic cation/carnitine transporter 2 (gene SLC22A5)

Organic solute transporter α/β (gene SLC51A/B)

Apparent permeability studied in vitro

Parallel artificial membrane permeability assay

Porcine brain endothelial cell

Physiologically based pharmacokinetic

saturable carrier-mediated permeability

Polymerase chain reaction

Pharmacodynamics

Protein Data Bank

passive diffusion

Prescription Drug User Fee Act

Polydimethylsiloxane

Effective permeability in humans studied in vivo

Peptide transporter

Peptide transporter 1 (gene SLC15A1)

Peptide transporter 2 (gene SLC15A2)

Positron emission tomography

P-glycoprotein (also known as MDR1, gene ABCB1)

Pharmacokinetics

Pharmacokinetics/pharmacodynamics

Pharmaceuticals and Medical Devices Agency (Japan)

Proof of concept

Passive diffusional driven permeability

Peroxisome proliferator activated receptor

Intrinsic biliary clearance

Intrinsic sinusoidal efflux clearance

Intrinsic uptake clearance

Pregnane X receptor (NR1I2)

Hepatic blood flow

Quantitative structure–activity relationship

Quantitative Whole Body Autoradiography

Research and development

relative activity factor

Recombinant activating gene

Rat brain endothelial

Rat bile salt export pump (gene ABCB11)

Research Collaboratory for Structural Bioinformatics

Relative expression factor

Receiver operating characteristics

Renal proximal tubule epithelial cells

Reverse transcriptase polymerase chain reaction

Retinoid X receptor

Sandwich-cultured hepatocytes

Sandwich-cultured human hepatocytes

Severe combined immunodeficiency

Serotonin transporter

Scaling factor

Sodium glucose linked transporter

Solute carrier gene superfamily

Solute carrier organic anion transporter gene subfamily

Solute carrier subfamily 22

Gene encoding MATE

Gene encoding OATP1A2

Gene encoding OATP1B1

Gene encoding OATP1B3

Gene encoding OATP2B1

Gene encoding NTCP

Gene encoding PEPT1

Gene encoding PEPT2

Gene encoding OCT1

Gene encoding OCT2

Gene encoding OCTN1

Gene encoding OCTN2

Gene encoding OAT1

Gene encoding OAT3

Gene encoding CNT

Gene encoding ENT

Gene encoding OSTα/β

estimate of logP by summing the contribution of atom-weighted solvent accessible surface areas (SASA) and correction factors

Molar refractivity (including implicit hydrogens). This property is an atomic contribution model that assumes the correct protonation state (washed structures).

Single nucleotide polymorphism(s)

Single photon emission computed tomography

Selected reaction monitoring

Sulfotransferase enzyme

Transcription activator-like effector nuclease

Transporter classification database

2,3,7,8-Tetrachlorodibenzo-p-dioxin

Tetraethylammonium

Transepithelial electrical resistance

Toxicokinetics

Time at which the C_max is observed

Trans-membrane domain

Topological polar surface area

Uridine 5′-diphosphate

Uridine 5′-diphospho-glucuronosyltransferase or UDP-glucuronosyltransferase

Urate transporter

Volume of distribution

Maximal velocity

Zinc-finger nucleases