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Results From Drug–Drug Interaction Studies In Vitro and In Vivo Investigating the Inhibitory Effect of Finerenone on the Drug Transporters BCRP, OATP1B1, and OATP1B3
Background and ObjectivesIn vitro and in vivo studies were performed with the novel, selective, nonsteroidal mineralocorticoid receptor antagonist...
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In Vitro and In Silico ADME Prediction
Pharmacokinetic issues have been identified as a major cause for the attrition of new chemical entities in drug discovery. High development costs and...
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Incorporating Uremic Solute-mediated Inhibition of OAT1/3 Improves PBPK Prediction of Tenofovir Renal and Systemic Disposition in Patients with Severe Kidney Disease
BackgroundDose modification of renally secreted drugs in patients with chronic kidney disease (CKD) has relied on serum creatinine concentration as a...
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Relevance of Transporters in Clinical Studies
It has become clear that drug disposition is not just a result of passive diffusion and metabolizing enzymes. Numerous transporters were identified...
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Targeting Transporters for Drug Delivery to the Brain: Can We Do Better?
Limited drug delivery to the brain is one of the major reasons for high failure rates of central nervous system (CNS) drug candidates. The...
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Neurovascular unit disruption and blood–brain barrier leakage in MCT8 deficiency
BackgroundThe monocarboxylate transporter 8 (MCT8) plays a vital role in maintaining brain thyroid hormone homeostasis. This transmembrane...
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Protein Expression of Amino Acid Transporters Is Altered in Isolated Cerebral Microvessels of 5xFAD Mouse Model of Alzheimer’s Disease
Membrane transporters such as ATP-binding cassette (ABC) and solute carrier (SLC) transporters expressed at the neurovascular unit (NVU) play an...
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Pharmacokinetic Interactions in Synergistic Herb-Drug Combinations
The phytoconstituents either in the crude or pure form may affect the bioavailability of the drugs; absorption, distribution, metabolism, and...
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Drug Metabolizing Enzymes and Transporters of the Mesentery
Recent research has shown that the mesentery, which was classified as a new organ in 2016, is indeed an unfragmented structure. The mesentery is now...
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Strategies for enhanced bioavailability of oxime reactivators in the central nervous system
Oxime reactivators of acetylcholinesterase are commonly used to treat highly toxic organophosphate poisoning. They are effective nucleophiles that...
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A systematic review of the drug-drug interaction between Statins and Quinolones
BackgroundStatins are widely used in cardiovascular disease (CVD) as a common lipid-lowering drug, while quinolones are widely used for the treatment...
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Assessment of the Effects of Inhibition or Induction of CYP2C19 and CYP2C9 Enzymes, or Inhibition of OAT3, on the Pharmacokinetics of Abrocitinib and Its Metabolites in Healthy Individuals
Background and ObjectiveAbrocitinib is a Janus kinase 1-selective inhibitor for the treatment of moderate-to-severe atopic dermatitis. Abrocitinib is...
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Voriconazole injection may induce delayed methotrexate excretion: a case report and experimental study
BackgroundWe report a case of delayed excretion of methotrexate (MTX) in a pediatric patient on high-dose MTX therapy in response to a change in the...
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Biophysical and Pharmacological Insights to CLC Chloride Channels
The CLC family encompasses two functional categories of transmembrane proteins: chloride conducting channels and proton-chloride antiporters. All...
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Conversion of Olmesartan to Olmesartan Medoxomil, A Prodrug that Improves Intestinal Absorption, Confers Substrate Recognition by OATP2B1
PurposeOlmesartan medoxomil (olmesartan-MX), an ester-type prodrug of the angiotensin II receptor blocker (ARB) olmesartan, is predominantly anionic...
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Mechanistic Study on the Effect of Renal Impairment on the Pharmacokinetics of Vildagliptin and its Carboxylic Acid Metabolite
PurposeTo clarify the mechanism of renal impairment leading to different degrees of increased plasma exposure to dipeptidyl peptidase 4 inhibitor...
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Advances in the structure, mechanism and targeting of chemoresistance-linked ABC transporters
Cancer cells frequently display intrinsic or acquired resistance to chemically diverse anticancer drugs, limiting therapeutic success. Among the main...
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Entry and Deposit of Aluminum in the Brain
Aluminum is considered a well-established neurotoxin and has a link between exposure and the development of neurological diseases, including...
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Characterizing the toxicological responses to inorganic arsenicals and their metabolites in immortalized human bladder epithelial cells
Arsenic is highly toxic to the human bladder. In the present study, we established a human bladder epithelial cell line that closely mimics normal...
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Transporter-Mediated Drug-Drug Interactions and Their Significance
Drug transporters are considered to be determinants of drug disposition and effects/toxicities by affecting the absorption, distribution, and...