Ontogeny of hepatic transporters and drug-metabolizing enzymes in humans and in nonclinical species

BD Van Groen, J Nicolaï, AC Kuik… - Pharmacological …, 2021 - ASPET
The liver represents a major eliminating and detoxifying organ, determining exposure to
endogenous compounds, drugs, and other xenobiotics. Drug transporters (DTs) and drug …

[HTML][HTML] Vascular drug delivery using carrier red blood cells: focus on RBC surface loading and pharmacokinetics

PM Glassman, CH Villa, A Ukidve, Z Zhao, P Smith… - Pharmaceutics, 2020 - mdpi.com
Red blood cells (RBC) have great potential as drug delivery systems, capable of producing
unprecedented changes in pharmacokinetics, pharmacodynamics, and immunogenicity …

[HTML][HTML] Duodenum Intestine-Chip for preclinical drug assessment in a human relevant model

M Kasendra, R Luc, J Yin, DV Manatakis, G Kulkarni… - Elife, 2020 - elifesciences.org
Induction of intestinal drug metabolizing enzymes can complicate the development of new
drugs, owing to the potential to cause drug-drug interactions (DDIs) leading to changes in …

Integrating the impact of lipophilicity on potency and pharmacokinetic parameters enables the use of diverse chemical space during small molecule drug optimization

RR Miller, M Madeira, HB Wood… - Journal of medicinal …, 2020 - ACS Publications
Lipophilicity has a dominant effect on many parameters that determine unbound drug
exposure as well as drug potency. Despite this, analysis of a large body of drug data …

Human transporters, PEPT 1/2, facilitate melatonin transportation into mitochondria of cancer cells: An implication of the therapeutic potential

X Huo, C Wang, Z Yu, Y Peng, S Wang… - Journal of pineal …, 2017 - Wiley Online Library
Melatonin is present in virtually all organisms from bacteria to mammals, and it exhibits a
broad spectrum of biological functions, including synchronization of circadian rhythms and …

Glucuronidation: driving factors and their impact on glucuronide disposition

G Yang, S Ge, R Singh, S Basu, K Shatzer… - Drug metabolism …, 2017 - Taylor & Francis
Glucuronidation is a well-recognized phase II metabolic pathway for a variety of chemicals
including drugs and endogenous substances. Although it is usually the secondary metabolic …

Blockade of organic anion transport in humans after treatment with the drug probenecid leads to major metabolic alterations in plasma and urine

JC Granados, V Bhatnagar… - Clinical Pharmacology & …, 2022 - Wiley Online Library
Probenecid is used to treat gout and hyperuricemia as well as increase plasma levels of
antiviral drugs and antibiotics. In vivo, probenecid mainly inhibits the renal SLC22 organic …

[HTML][HTML] Potential applications of chitosan-based nanomaterials to surpass the gastrointestinal physiological obstacles and enhance the intestinal drug absorption

N Pathomthongtaweechai, C Muanprasat - Pharmaceutics, 2021 - mdpi.com
The small intestine provides the major site for the absorption of numerous orally
administered drugs. However, before reaching to the systemic circulation to exert beneficial …

[HTML][HTML] Predicting drug extraction in the human gut wall: assessing contributions from drug metabolizing enzymes and transporter proteins using preclinical models

SA Peters, CR Jones, AL Ungell, OJD Hatley - Clinical pharmacokinetics, 2016 - Springer
Intestinal metabolism can limit oral bioavailability of drugs and increase the risk of drug
interactions. It is therefore important to be able to predict and quantify it in drug discovery …

Metabolomic and genome‐wide association studies reveal potential endogenous biomarkers for OATP1B1

SW Yee, MM Giacomini, CH Hsueh… - Clinical …, 2016 - Wiley Online Library
Transporter‐mediated drug‐drug interactions (DDIs) are a major cause of drug toxicities.
Using published genome‐wide association studies (GWAS) of the human metabolome, we …