[HTML][HTML] In vitro models replicating the human intestinal epithelium for absorption and metabolism studies: A systematic review

A Fedi, C Vitale, G Ponschin, S Ayehunie… - Journal of Controlled …, 2021 - Elsevier
Absorption, distribution, metabolism and excretion (ADME) studies represent a fundamental
step in the early stages of drug discovery. In particular, the absorption of orally administered …

Coexistence of passive and carrier-mediated processes in drug transport

K Sugano, M Kansy, P Artursson, A Avdeef… - Nature reviews Drug …, 2010 - nature.com
The permeability of biological membranes is one of the most important determinants of the
pharmacokinetic processes of a drug. Although it is often accepted that many drug …

Renal drug transporters and drug interactions

A Ivanyuk, F Livio, J Biollaz, T Buclin - Clinical pharmacokinetics, 2017 - Springer
Transporters in proximal renal tubules contribute to the disposition of numerous drugs.
Furthermore, the molecular mechanisms of tubular secretion have been progressively …

The pharmacology and clinical pharmacology of 3, 4-methylenedioxymethamphetamine (MDMA,“ecstasy”)

AR Green, AO Mechan, JM Elliott, E O'Shea… - Pharmacological …, 2003 - ASPET
The amphetamine derivative (±)-3, 4-methylenedioxymethamphetamine (MDMA, ecstasy) is
a popular recreational drug among young people, particularly those involved in the dance …

The Caco-2 cell monolayer: usefulness and limitations

H Sun, ECY Chow, S Liu, Y Du… - Expert opinion on drug …, 2008 - Taylor & Francis
Background: The Caco-2 monolayer has been used extensively for the high-throughput
screening of drug permeability and identification of substrates, inhibitors, and inducers of …

Rational use of in vitro P-glycoprotein assays in drug discovery

JW Polli, SA Wring, JE Humphreys, L Huang… - … of Pharmacology and …, 2001 - ASPET
P-glycoprotein (Pgp) affects the absorption, distribution, and clearance of a variety of
compounds. Thus, identification of compounds that are Pgp substrates can aid drug …

Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers

BD Rege, JPY Kao, JE Polli - European journal of pharmaceutical sciences, 2002 - Elsevier
The objectives of this study were (1) to investigate the transporter inhibition activity of three
nonionic surfactants on P-glycoprotein, the human intestinal peptide transporter, and the …

Impact of drug transporter studies on drug discovery and development

N Mizuno, T Niwa, Y Yotsumoto, Y Sugiyama - Pharmacological reviews, 2003 - ASPET
Drug transporters are expressed in many tissues such as the intestine, liver, kidney, and
brain, and play key roles in drug absorption, distribution, and excretion. The information on …

In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system

B Feng, JB Mills, RE Davidson, RJ Mireles… - Drug Metabolism and …, 2008 - ASPET
Thirty-one structurally diverse marketed central nervous system (CNS)-active drugs, one
active metabolite, and seven non-CNS-active compounds were tested in three P …

Comparison of brain capillary endothelial cell-based and epithelial (MDCK-MDR1, Caco-2, and VB-Caco-2) cell-based surrogate blood–brain barrier penetration …

É Hellinger, S Veszelka, AE Tóth, F Walter… - European journal of …, 2012 - Elsevier
An accurate means of predicting blood–brain barrier (BBB) penetration and blood–brain
partitioning of NCEs (new chemical entities) would fulfill a major need in pharmaceutical …