Species differences in drug transporters and implications for translating preclinical findings to humans
X Chu, K Bleasby, R Evers - Expert opinion on drug metabolism & …, 2013 - Taylor & Francis
Introduction: Drug transporters play an important role in the absorption, distribution, and
excretion (ADE) of many drugs. In the last several years it has become increasingly clear that …
excretion (ADE) of many drugs. In the last several years it has become increasingly clear that …
Transport of the dipeptidyl peptidase-4 inhibitor sitagliptin by human organic anion transporter 3, organic anion transporting polypeptide 4C1, and multidrug resistance …
XY Chu, K Bleasby, J Yabut, X Cai, GH Chan… - … of Pharmacology and …, 2007 - ASPET
Sitagliptin, a selective dipeptidyl peptidase 4 inhibitor recently approved for the treatment of
type 2 diabetes, is excreted into the urine via active tubular secretion and glomerular …
type 2 diabetes, is excreted into the urine via active tubular secretion and glomerular …
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia
RM Oballa, L Belair, WC Black, K Bleasby… - Journal of medicinal …, 2011 - ACS Publications
The potential use of SCD inhibitors for the chronic treatment of diabetes and dyslipidemia
has been limited by preclinical adverse events associated with inhibition of SCD in skin and …
has been limited by preclinical adverse events associated with inhibition of SCD in skin and …
Functional consequences of single nucleotide polymorphisms in the human organic anion transporter hOAT1 (SLC22A6)
K Bleasby, LA Hall, JL Perry, HW Mohrenweiser… - … of Pharmacology and …, 2005 - ASPET
The human organic anion transporter hOAT1 (SLC22A6) contributes to the uptake of a range
of small organic anions across the basolateral membrane of the renal proximal tubule and …
of small organic anions across the basolateral membrane of the renal proximal tubule and …
The complexities of interpreting reversible elevated serum creatinine levels in drug development: does a correlation with inhibition of renal transporters exist?
X Chu, K Bleasby, GH Chan, I Nunes, R Evers - Drug Metabolism and …, 2016 - ASPET
In humans, creatinine is formed by a multistep process in liver and muscle and eliminated
via the kidney by a combination of glomerular filtration and active transport. Based on current …
via the kidney by a combination of glomerular filtration and active transport. Based on current …
The organic cation transporter OCT2 mediates the uptake of β‐adrenoceptor antagonists across the apical membrane of renal LLC‐PK1 cell monolayers
AJ Dudley, K Bleasby… - British journal of …, 2000 - Wiley Online Library
Previous studies have shown that β‐adrenoceptor antagonists may be substrates of organic
cation transporters in kidney and lung. In this study we examined the transport of the β‐…
cation transporters in kidney and lung. In this study we examined the transport of the β‐…
[HTML][HTML] Islatravir is not expected to be a victim or perpetrator of drug-drug interactions via major drug-metabolizing enzymes or transporters
K Bleasby, R Houle, M Hafey, M Lin, J Guo, B Lu… - Viruses, 2021 - mdpi.com
Islatravir (MK-8591) is a nucleoside reverse transcriptase translocation inhibitor in development
for the treatment and prevention of HIV-1. The potential for islatravir to interact with …
for the treatment and prevention of HIV-1. The potential for islatravir to interact with …
QSAR Prediction of Passive Permeability in the LLC‐PK1 Cell Line: Trends in Molecular Properties and Cross‐Prediction of Caco‐2 Permeabilities
…, RP Sheridan, D Roberts, K Bleasby… - Molecular …, 2012 - Wiley Online Library
A QSAR model for predicting passive permeability (P app ) was derived from P app values
measured in the LLC‐PK1 cell line. The QSAR method and descriptor set that performed best …
measured in the LLC‐PK1 cell line. The QSAR method and descriptor set that performed best …
Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease
…, T Liang, KL Fillgrove, Y Kuo, K Bleasby… - ACS Medicinal …, 2023 - ACS Publications
Parkinson’s disease is the second most prevalent progressive neurodegenerative disorder
characterized by the loss of dopaminergic neurons in the substantia nigra. Loss-of-function …
characterized by the loss of dopaminergic neurons in the substantia nigra. Loss-of-function …
In Vitro Evaluation of the Drug Interaction Potential of Doravirine
K Bleasby, KL Fillgrove, R Houle, B Lu… - Antimicrobial Agents …, 2019 - Am Soc Microbiol
Doravirine is a novel nonnucleoside reverse transcriptase inhibitor for the treatment of
human immunodeficiency virus type 1 infection. In vitro studies were conducted to assess the …
human immunodeficiency virus type 1 infection. In vitro studies were conducted to assess the …