Noora Sjöstedt
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View article: Impact of Obesity and <scp>MASH</scp> on Zonal Hepatocellular Statin Exposure: Pharmacodynamic Insights From a Permeability‐Limited Multicompartment Liver Model
Impact of Obesity and <span>MASH</span> on Zonal Hepatocellular Statin Exposure: Pharmacodynamic Insights From a Permeability‐Limited Multicompartment Liver Model Open
Statins are frequently prescribed for hyperlipidemia, a common comorbidity in patients with obesity and/or metabolic dysfunction‐associated steatohepatitis (MASH). However, limited knowledge exists on how MASH may alter statin disposition …
View article: Characterization of fecal deglucuronidation activity in healthy subjects and in patients treated with fecal microbiota transplantation
Characterization of fecal deglucuronidation activity in healthy subjects and in patients treated with fecal microbiota transplantation Open
View article: Dicloxacillin and flucloxacillin inhibit hepatic uptake transporters – in vitro investigations and physiologically based pharmacokinetic modelling
Dicloxacillin and flucloxacillin inhibit hepatic uptake transporters – in vitro investigations and physiologically based pharmacokinetic modelling Open
Dicloxacillin and flucloxacillin are β-lactamase-resistant penicillin antibiotics that have been in clinical use for over 50 years. While both antibiotics are known to induce cytochrome P450 enzymes, there is limited information available …
View article: Food Additives Inhibit Intestinal Drug Transporters but Have Limited Effect on In Vitro Drug Permeability
Food Additives Inhibit Intestinal Drug Transporters but Have Limited Effect on In Vitro Drug Permeability Open
Food additives are chemical substances that are added to processed food to improve its flavor, texture, or appearance. Food additives can inhibit intestinal transporters, such as breast cancer resistance protein (BCRP), multidrug resistanc…
View article: In vitro identification of decreased function genetic variants of ABCB1
In vitro identification of decreased function genetic variants of ABCB1 Open
The efflux transporter ABCB1 (P-glycoprotein, P-gp) has an important role in drug disposition, and thus, genetic variants that lead to decreased transport function might increase drug exposure. Complete loss of function of ABCB1 is rare bu…
View article: Exploring the effect of intracellular loop 1 genetic variants in human ABCG2 on transport activity and protein abundance
Exploring the effect of intracellular loop 1 genetic variants in human ABCG2 on transport activity and protein abundance Open
ABCG2 (breast cancer resistance protein, BCRP), can affect drug disposition, and thus, variation in the ABCG2 gene may alter drug exposure. We studied non-synonymous naturally occurring single-nucleotide variants (SNVs) in intracellular lo…
View article: Efflux and uptake of androgen sulfates using transporter-overexpressing HEK293 cells and membrane vesicles
Efflux and uptake of androgen sulfates using transporter-overexpressing HEK293 cells and membrane vesicles Open
Hydrophilic steroid conjugates require active and facilitated transport mechanisms for their distribution into tissues and excretion from the body. The ATP-binding cassette (ABC) and solute carrier organic anion (SLCO) transporters involve…
View article: Efflux and uptake transport and gut microbial reactivation of raloxifene glucuronides
Efflux and uptake transport and gut microbial reactivation of raloxifene glucuronides Open
Raloxifene has low bioavailability due to extensive glucuronidation in the intestine and the liver, and its pharmacokinetics is associated with high intra‐ and interindividual variability. Some of this variability could be explained by the…
View article: Alterations in zonal distribution and plasma membrane localization of hepatocyte bile acid transporters in patients with NAFLD
Alterations in zonal distribution and plasma membrane localization of hepatocyte bile acid transporters in patients with NAFLD Open
Background: NAFLD is highly prevalent with limited treatment options. Bile acids (BAs) increase in the systemic circulation and liver during NAFLD progression. Changes in plasma membrane localization and zonal distribution of BA transporte…
View article: Membrane transporters in drug development and as determinants of precision medicine
Membrane transporters in drug development and as determinants of precision medicine Open
View article: In vitro identification of decreased function phenotype ABCG2 variants
In vitro identification of decreased function phenotype ABCG2 variants Open
Reduced activity of efflux transporter ABCG2, caused e.g., by inhibition or decreased function genetic variants, can increase drug absorption and plasma levels. ABCG2 has one clinically significant single nucleotide variant Q141K (c.421C>A…
View article: Novel inhibitors of breast cancer resistance protein (BCRP, ABCG2) among marketed drugs
Novel inhibitors of breast cancer resistance protein (BCRP, ABCG2) among marketed drugs Open
Drug-drug interactions (DDIs) are a major concern for the safe use of medications. Breast cancer resistance protein (BCRP) is a clinically relevant ATP-binding cassette (ABC) transporter for drug disposition. Inhibition of BCRP increases t…
View article: Functional in vitro characterization of SLCO1B1 variants and simulation of the clinical pharmacokinetic impact of impaired OATP1B1 function.
Functional in vitro characterization of SLCO1B1 variants and simulation of the clinical pharmacokinetic impact of impaired OATP1B1 function. Open
Organic Anion Transporting Polypeptide 1B1 is important to the hepatic elimination and distribution of many drugs. If OATP1B1 function is decreased, it can increase plasma exposure of e.g. several statins leading to increased risk of muscl…
View article: Considerations for Physiologically Based Modeling in Liver Disease: From Nonalcoholic Fatty Liver (NAFL) to Nonalcoholic Steatohepatitis (NASH)
Considerations for Physiologically Based Modeling in Liver Disease: From Nonalcoholic Fatty Liver (NAFL) to Nonalcoholic Steatohepatitis (NASH) Open
Nonalcoholic fatty liver disease (NAFLD), representing a clinical spectrum ranging from nonalcoholic fatty liver (NAFL) to nonalcoholic steatohepatitis (NASH), is rapidly evolving into a global pandemic. Patients with NAFLD are burdened wi…
View article: Regulation of Drug Transport Proteins—From Mechanisms to Clinical Impact: A White Paper on Behalf of the International Transporter Consortium
Regulation of Drug Transport Proteins—From Mechanisms to Clinical Impact: A White Paper on Behalf of the International Transporter Consortium Open
Membrane transport proteins are involved in the absorption, disposition, efficacy, and/or toxicity of many drugs. Numerous mechanisms (e.g., nuclear receptors, epigenetic gene regulation, microRNAs, alternative splicing, post‐translational…
View article: The Role of Uptake and Efflux Transporters in the Disposition of Glucuronide and Sulfate Conjugates
The Role of Uptake and Efflux Transporters in the Disposition of Glucuronide and Sulfate Conjugates Open
Glucuronidation and sulfation are the most typical phase II metabolic reactions of drugs. The resulting glucuronide and sulfate conjugates are generally considered inactive and safe. They may, however, be the most prominent drug-related ma…
View article: Identification of Key Amino Acids that Impact Organic Solute Transporter α/β (OSTα/β)
Identification of Key Amino Acids that Impact Organic Solute Transporter α/β (OSTα/β) Open
View article: Physiologically‐Based Pharmacokinetic Model of Morphine and Morphine‐3‐Glucuronide in Nonalcoholic Steatohepatitis
Physiologically‐Based Pharmacokinetic Model of Morphine and Morphine‐3‐Glucuronide in Nonalcoholic Steatohepatitis Open
Nonalcoholic steatohepatitis (NASH), the progressive form of nonalcoholic fatty liver disease, is increasing in prevalence. NASH‐related alterations in hepatic protein expression (e.g., transporters) and in overall physiology may affect dr…
View article: Role of Organic Solute Transporter Alpha/Beta in Hepatotoxic Bile Acid Transport and Drug Interactions
Role of Organic Solute Transporter Alpha/Beta in Hepatotoxic Bile Acid Transport and Drug Interactions Open
Organic solute transporter (OST) α/β is a key bile acid transporter expressed in various organs, including the liver under cholestatic conditions. However, little is known about the involvement of OSTα/β in bile acid-mediated drug-induced …
View article: Hepatic Transporter Alterations by Nuclear Receptor Agonist T0901317 in Sandwich-Cultured Human Hepatocytes: Proteomic Analysis and PBPK Modeling to Evaluate Drug-Drug Interaction Risk
Hepatic Transporter Alterations by Nuclear Receptor Agonist T0901317 in Sandwich-Cultured Human Hepatocytes: Proteomic Analysis and PBPK Modeling to Evaluate Drug-Drug Interaction Risk Open
View article: Mechanistic Modeling of the Hepatic Disposition of Estradiol-17β-Glucuronide in Sandwich-Cultured Human Hepatocytes
Mechanistic Modeling of the Hepatic Disposition of Estradiol-17β-Glucuronide in Sandwich-Cultured Human Hepatocytes Open
View article: Efflux transport of nicotine, cotinine and <i>trans</i>‐3′‐hydroxycotinine glucuronides by human hepatic transporters
Efflux transport of nicotine, cotinine and <i>trans</i>‐3′‐hydroxycotinine glucuronides by human hepatic transporters Open
Nicotine is the addiction causing alkaloid in tobacco, and it is used in smoking cessation therapies. Although the metabolic pathways of nicotine are well known and mainly occur in the liver, the transport of nicotine and its metabolites i…
View article: Endogenous, cholesterol-activated ATP-dependent transport in membrane vesicles from Spodoptera frugiperda cells
Endogenous, cholesterol-activated ATP-dependent transport in membrane vesicles from Spodoptera frugiperda cells Open
View article: In vitro evaluation of the pharmacokinetic effects of BCRP interactions
In vitro evaluation of the pharmacokinetic effects of BCRP interactions Open
Transport proteins embedded in the cell membranes of many organs can affect the absorption, distribution and elimination of numerous drugs. This can lead to the enhanced or restricted uptake or distribution of the drugs, nonlinear pharmaco…
View article: Transmembrane Domain Single-Nucleotide Polymorphisms Impair Expression and Transport Activity of ABC Transporter ABCG2
Transmembrane Domain Single-Nucleotide Polymorphisms Impair Expression and Transport Activity of ABC Transporter ABCG2 Open
These results indicate that the transmembrane region of ABCG2 is sensitive to amino acid substitution and that patients harboring these ABCG2 variant forms could suffer from unexpected pharmacokinetic events of ABCG2 substrate drugs or hav…
View article: The Effect of Albumin on MRP2 and BCRP in the Vesicular Transport Assay
The Effect of Albumin on MRP2 and BCRP in the Vesicular Transport Assay Open
The ABC transporters multidrug resistance associated protein 2 (MRP2) and breast cancer resistance protein (BCRP) are of interest in drug development, since they affect the pharmacokinetics of several drugs. Membrane vesicle transport assa…