Sökning: "OATP"

Hittade 5 avhandlingar innehållade ordet OATP.

  1. 1. Involvement of Membrane Transport Proteins in Intestinal Absorption and Hepatic Disposition of Drugs Using Fexofenadine as a Model Drug

    Författare :Niclas Petri; Hans Lennernäs; Geoffrey Tucker; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Biopharmacy; Fexofenadine; OATP; P-glycoprotein; Organic Anion Transporters; ATP-Binding Cassette Transporters; membrane transport proteins; Bioavailability; Biopharmaceutics; Biofarmaci; Biopharmacy; Biofarmaci;

    Sammanfattning : The aims of this thesis were to study the in vivo relevance of membrane transporters for intestinal absorption and the hepatic disposition of drugs in humans and preclinical models. Fexofenadine is a substrate for ABCB1 (P-glycoprotein) and members of the organic anion transporting polypeptide (OATP/SLCO) family. LÄS MER

  3. 2. Intestinal Permeability and Presystemic Extraction of Fexofenadine and R/S-verapamil

    Författare :Christer Tannergren; Hans Lennernäs; Dirk KF Meijer; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Biopharmacy; Bioavailability; Fexofenadine; Verapamil; P-glycoprotein; CYP3A4; OATP; Enantioselective; Permeability; Caco-2; Intestinal perfusion; Biofarmaci; Biopharmacy; Biofarmaci;

    Sammanfattning : The main objective of this thesis was to investigate the in vivo relevance of membrane transporters and cytochrome P450 (CYP) 3A4-mediated metabolism in the intestine and liver for the bioavailability of drugs in humans after oral administration.In the first part of the thesis, the main transport mechanisms involved in the intestinal absorption and bioavailability were investigated for fexofenadine, a minimally metabolized drug, which is a substrate for P-glycoprotein (P-gp) and members of organic anion transporting polypeptide (OATP) family. LÄS MER

  4. 3. The Hepatobiliary Transport of Rosuvastatin In Vivo

    Författare :Ebba Bergman; Hans Lennernäs; Ulf Bondesson; Jack Cook; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Rosuvastatin; Biliary excretion; Transport inhibition; Pharmacokinetics; Drug-drug interactions; Hepatobiliary transport; Organic anion transporting polypeptide; OATP; Statins; Gemfibrozil; Cyclosporine; Imatinib; Rifampicin; Canalicular transport; Sinusoidal transport; Hepatic uptake; Hepatic extraction; Biopharmacy; Biofarmaci; Biopharmaceutics; biofarmaci;

    Sammanfattning : In vivo studies of hepatobiliary disposition are challenging. The hepatobiliary system is complex, as its physiological localization, complex cellular structure with numerous transporters and enzymes, and the interindividual variability in protein expression and biliary flow will all affect the in vivo disposition of a drug under investigation. LÄS MER

  5. 4. In vitro and in silico Predictions of Hepatic Transporter-Mediated Drug Clearance and Drug-Drug Interactions in vivo

    Författare :Anna Vildhede; Per Artursson; Maria Karlgren; Maria Kjellsson; Ulf Norinder; Kim Brouwer; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; OATP1B1; OATP1B3; OATP2B1; NTCP; drug transporters; human hepatocytes; atorvastatin; pitavastatin; proteomics; sandwich-cultured human hepatocytes; SCHH; mechanistic modeling; in vitro-in vivo extrapolation; transport inhibition; hepatic uptake; hepatocyte isolation; transporter contribution; Biopharmaceutics; Biofarmaci;

    Sammanfattning : The liver is the major detoxifying organ, clearing the blood from drugs and other xenobiotics. The extent of hepatic clearance (CL) determines drug exposure and hence, the efficacy and toxicity associated with exposure. Drug-drug interactions (DDIs) that alter the hepatic CL may cause more or less severe outcomes, such as adverse drug reactions. LÄS MER

  7. 5. Characterization of parameters influencing intracellular bioavailability and prediction of intracellular drug exposure

    Författare :Andrea Treyer; Per Artursson; Gert Fricker; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; intracellular drug bioavailability; unbound drug concentration; drug disposition; ADME; drug transport; drug metabolism membrane partitioning; phospholipid; drug-drug interaction; antisense oligonucleotide; cell-penetrating peptide; Farmaceutisk vetenskap; Pharmaceutical Science;

    Sammanfattning : This thesis work investigates factors influencing intracellular drug disposition. An experimental method for measurement of intracellular bioavailability (Fic), was used throughout. Fic is defined as the ratio between the unbound drug concentration inside the cell and the compound concentration in the cell exterior. LÄS MER