PHARMACOLOGY

Stefan OSWALD

SITE

    Dr. Oswald received his master in Pharmaceutical Sciences from the Humboldt University Berlin, Germany in 2001. After that, he worked in the pharmaceutical industry and pharmacies for two years. From 2004 to 2007, he completed his PhD thesis at the Department of Clinical Pharmacology, Greifswald, Germany. In 2007, he finished his advanced training in pharmaceutical analytics and became the head of the GLP-certified analytical laboratory of his department. From 2007 to 2012, he led the research project entitled “Drug transport-based concepts and drug-delivery-technologies for optimizing the clinical application of drugs” funded by the German Ministry of Education and Research (BMBF)

    In 2012, he was a visiting scholar at Pfizer Inc., Global Research and Development, Pharmacokinetics and Drug Metabolism in Groton, CT, USA and at the University of Washington, Department of Pharmaceutics (Prof. Jashvant Unadkat) in Seattle, WA, USA. In 2013, he was appointed as assistant professor of “Clinical Pharmacology of Transporter Proteins” at the Department of Clinical Pharmacology and became the head of the BMBF funded research project “Compartmental Drug Absorption and Transport (COM_DAT): Pharmacokinetic concepts to an individualized therapy” to optimize drug therapy and safety by generating predictive in vitro and in vivo models and estimating drug exposure and drug-drug interactions in humans. From 2015 to 2018, he led the Department of Clinical Pharmacology of the University Medicine Greifswald, Germany at the Center of Drug Absorption and Transport (C_DAT). In April 2020, he was nominated as a full Professor of Pharmacology at the Department of Pharmacology and Toxicology of the University Medicine Rostock. 

    His research interests are focused on the expression, regulation and function of transporter proteins and metabolizing enzymes in the human intestine and their impact on oral drug absorption, inter-subject variability, side effects, and drug-drug interactions. He worked for over 16 years in the field of Clinical Pharmacology and has authored about 80 papers in peer-review journals. His expertise focuses on bioanalytics (small molecules and mass-spectrometry-based targeted proteomics), pharmacokinetics and in vitro models of transporter function.

Int J Mol Sci. 2021;23:255. Expression and functional contribution of different Organic Cation Transporters to the cellular uptake of Doxorubicin into human breast cancer and cardiac tissue. Otter M, Csader S, Keiser M, Oswald S. PubMed

Clin Pharmacol Ther. 2022;In press. Regulation of drug transport proteins-from mechanisms to clinical impact: A white paper on behalf of the International Transporter Consortium. Brouwer KLR, Evers R, Hayden E, Hu S, Li CY, Meyer Zu Schwabedissen HE, Neuhoff S, Oswald S, Piquette-Miller M, Saran C, Sjöstedt N, Sprowl JA, Stahl SH, Yue W. PubMed

Pharmaceutics. 2021;13:1334. Gene expression and protein abundance of hepatic drug metabolizing enzymes in liver pathology. Drozdzik M, Lapczuk-Romanska J, Wenzel C, Szelag-Pieniek S, Post M, Skalski Ł, Kurzawski M, Oswald S. PubMed

Biomed Pharmacother. 2021;143:112125. Impact of kidney dysfunction on hepatic and intestinal drug transporters. Droździk M, Oswald S, Droździk A. PubMed

Drug Metab Dispos. 2021 Sep;49(9):750-759. doi: 10.1124/dmd.121.000430. Epub 2021 Jun 23. PMID: 34162690. Comparative hepatic and intestinal efflux transport of statins. Deng F, Tuomi SK, Neuvonen M, Hirvensalo P, Kulju S, Wenzel C, Oswald S, Filppula AM, Niemi M. PubMed

Pharmacol Rep. 2021;73:1427-1438. Hepatic drug-metabolizing enzymes and drug transporters in Wilson's disease patients with liver failure. Szeląg-Pieniek S, Oswald S, Post M, Łapczuk-Romańska J, Droździk M, Kurzawski M. PubMed

Front Pharmacol. 2021;12:648388.Organic Cation Transporter 1 an Intestinal Uptake Transporter: Fact or Fiction? Wenzel C, Drozdzik M, Oswald S. PubMed

Biomedicines. 2021;9:426. Membrane carriers and transporters in kidney physiology and disease. Drozdzik M, Drozdzik M, Oswald S. PubMed

Proc Natl Acad Sci U S A. 2021;118:e2020168118. Targeting OCT3 attenuates doxorubicin-induced cardiac injury. Huang KM, Zavorka Thomas M, Magdy T, Eisenmann ED, Uddin ME, DiGiacomo DF, Pan A, Keiser M, Otter M, Xia SH, Li Y, Jin Y, Fu Q, Gibson AA, Bonilla IM, Carnes CA, Corps KN, Coppola V, Smith SA, Addison D, Nies AT, Bundschuh R, Chen T, Lustberg MB, Wang J, Oswald S, Campbell MJ, Yan PS, Baker SD, Hu S, Burridge PW, Sparreboom A. PubMed

Pharmaceutics. 2020;12:E1201. Drug-Drug interactions involving intestinal and hepatic CYP1A enzymes. Klomp F, Wenzel C, Drozdzik M, Oswald S. PubMed

Drug Metab Dispos. 2020;48:1380-1392. Differences in Metformin and Thiamine uptake between human and mouse Organic Cation Transporter 1: Structural determinants and potential consequences for intrahepatic concentrations. Meyer MJ, Tuerkova A, Römer S, Wenzel C, Seitz T, Gaedcke J, Oswald S, Brockmöller J, Zdrazil B, Tzvetkov MV. PubMed

Int J Mol Sci. 2020;21:5737. Extrahepatic Drug transporters in liver failure: Focus on kidney and gastrointestinal tract. Droździk M, Oswald S, Droździk A. PubMed

Pharmacol Rep. 2020;72:1173-1194. Intestinal drug transporters in pathological states: an overview. Drozdzik M, Czekawy I, Oswald S, Drozdzik A. PubMed

Sci Rep. 2020;10:7248. The orphan solute carrier SLC10A7 is a novel negative regulator of intracellular calcium signaling. Karakus E, Wannowius M, Müller SF, Leiting S, Leidolf R, Noppes S, Oswald S, Diener M, Geyer J. PubMed

Mol Pharm. 2020;17:1987-1995. OATP1A2 and OATP2B1 are interacting with Dopamine-Receptor agonists and antagonists. Schäfer AM, Meyer Zu Schwabedissen HE, Bien-Möller S, Hubeny A, Vogelgesang S, Oswald S, Grube M. PubMed

Int J Mol Sci. 2020;21:1606. Monocarboxylate Transporter 1 (MCT1) in liver pathology. Droździk M, Szeląg-Pieniek S, Grzegółkowska J, Łapczuk-Romańska J, Post M, Domagała P, Miętkiewski J, Oswald S, Kurzawski M.  PubMed

Drug Metab Dispos. 2020;48:205-216. Induction of human intestinal and hepatic Organic Anion Transporting Polypeptides: Where is the evidence for its relevance in Drug-Drug Interactions? Rodrigues AD, Lai Y, Shen H, Varma MVS, Rowland A, Oswald S. PubMed

Clin Pharmacol Ther. 2019;107:1138-1148. Protein abundance of hepatic drug transporters in patients with different forms of liver damage. Drozdzik M, Szelag-Pieniek S, Post M, Zeair S, Wrzesinski M, Kurzawski M, Prieto J, Oswald S. PubMed

Int J Mol Sci. 2019;20(21). pii: E5303. Protein abundance of clinically relevant drug transporters in the human kidneys. Oswald S, Müller J, Neugebauer U, Schröter R, Herrmann E, Pavenstädt H, Ciarimboli G. PubMed

Mol Pharm. 2019;16:3823-3830. Transcriptional and post-transcriptional regulation of duodenal P-Glycoprotein and MRP2 in healthy human subjects after chronic treatment with Rifampin and Carbamazepine. Brueck S, Bruckmueller H, Wegner D, Busch D, Martin P, Oswald S, Cascorbi I, Siegmund W. PubMed

Pharmacol Rep. 2019;71:738-745. The reference liver - ABC and SLC drug transporters in healthy donor and metastatic livers. Kurzawski M, Szeląg-Pieniek S, Łapczuk-Romańska J, Wrzesiński M, Sieńko J, Oswald S, Droździk M. PubMed

Clin Pharmacol Ther. 2019;105:1204-1212. Protein abundance of clinically relevant drug transporters in the human liver and intestine: A comparative analysis in paired tissue specimens. Drozdzik M, Busch D, Lapczuk J, Müller J, Ostrowski M, Kurzawski M, Oswald S. PubMed

Pharmacol Ther. 2019;195:39-53. Organic Anion Transporting Polypeptide (OATP) transporter expression, localization and function in the human intestine. Oswald S. PubMed

J Pharm Sci. 2019;108:1035-1046. Dysregulation of mucosal membrane transporters and drug-metabolizing enzymes in ulcerative colitis. Erdmann P, Bruckmueller H, Martin P, Busch D, Haenisch S2, Müller J, Wiechowska-Kozlowska A, Partecke LI, Heidecke CD, Cascorbi I, Drozdzik M, Oswald S. PubMed

Basic Clin Pharmacol Toxicol. 2019;124:245-255. Expression of clinically relevant drug-metabolizing enzymes along the human intestine and their correlation to drug transporters and nuclear receptors: An intra-subject analysis. Fritz A, Busch D, Lapczuk J, Ostrowski M, Drozdzik M, Oswald S. PubMed

Drug Metab Dispos. 2018;46:1776-1786. CRISPR-Cas9: A new addition to the drug metabolism and disposition tool box. Karlgren M, Simoff I, Keiser M, Oswald S, Artursson P. PubMed

Mol Pharm. 2018;15:326-331. Affinity of Ketamine to clinically relevant transporters. Keiser M, Hasan M, Oswald S. PubMed

Mol Pharm. 2017;14:3142-3151. Variability in Mass Spectrometry-based quantification of clinically relevant drug transporters and drug metabolizing enzymes. Wegler C1, Gaugaz FZ, Andersson TB, Wiśniewski JR, Busch D, Gröer C, Oswald S, Norén A, Weiss F, Hammer HS, Joos TO, Poetz O, Achour B, Rostami-Hodjegan A, van de Steeg E, Wortelboer HM, Artursson P. PubMed

Curr Protoc Pharmacol. 2017;77:7. The Ussing chamber assay to study drug metabolism and transport in the human intestine. Kisser B, Mangelsen E, Wingolf C, Partecke LI, Heidecke CD, Tannergren C, Oswald S, Keiser M. PubMed

Mol Pharm. 2017;14:2245-2253. Clinically relevant multidrug transporters are regulated by microRNAs along the human intestine. Bruckmueller H, Martin P, Kähler M, Haenisch S, Ostrowski M, Drozdzik M, Siegmund W, Cascorbi I, Oswald S. PubMed

J Pharm Sci. 2017;106:2909-2913. A CRISPR-Cas9 generated MDCK cell line expressing human MDR1 without endogenous canine MDR1 (cABCB1): an improved tool for drug efflux studies. Karlgren M, Simoff I, Backlund M, Wegler C, Keiser M, Handin N, Müller J, Lundquist P, Jareborg AC, Oswald S, Artursson P. PubMed

J Pharm Sci. 2017;106:2657-2663. The Organic Anion-Transporting Peptide 2B1 is localized in the basolateral membrane of the human jejunum and Caco-2 monolayers. Keiser M, Kaltheuner L, Wildberg C, Müller J, Grube M, Partecke LI, Heidecke CD, Oswald S. PubMed

Equine Vet J. 2017;49:618-623. Pharmacological indices and pulmonary distribution of rifampicin after repeated oral administration in healthy foals. Berlin S, Kirschbaum A, Spieckermann L, Oswald S, Keiser M, Grube M, Venner M, Siegmund W. PubMed

Eur J Pharm Biopharm. 2017;112:187-195. Effects of frequently used pharmaceutical excipients on the organic cation transporters 1-3 and peptide transporters 1/2 stably expressed in MDCKII cells. Otter M, Oswald S, Siegmund W, Keiser M. PubMed

Curr Med Chem. 2016;23:4468-4489. Expression and regulation of drug transporters and metabolizing enzymes in the human gastrointestinal tract. Drozdzik M, Oswald S. PubMed

Biol Chem. 2017;398:175-192. Expression, regulation and function of intestinal drug transporters: an update. Müller J, Keiser M, Drozdzik M, Oswald S. PubMed

Biopharm Drug Dispos. 2017;38:115-126. Caco-2 cells - expression, regulation and function of drug transporters compared with human jejunal tissue. Brück S, Strohmeier J, Busch D, Drozdzik M, Oswald S. PubMed

Mol Pharm. 2016;13:1089-99. Pharmacokinetics and pulmonary distribution of Clarithromycin and Rifampicin after concomitant and consecutive administration in foals. Berlin S, Spieckermann L, Oswald S, Keiser M, Lumpe S, Ullrich A, Grube M, Hasan M, Venner M, Siegmund W. PubMed

Mol Pharm. 2015;12:171-8. Expression of drug transporters and drug metabolizing enzymes in the bladder urothelium in man and affinity of the bladder spasmolytic trospium chloride to transporters likely involved in its pharmacokinetics. Bexten M, Oswald S, Grube M, Jia J, Graf T, Zimmermann U, Rodewald K, Zolk O, Schwantes U, Siegmund W, Keiser M. PubMed

Pharmacogenet Genomics. 2015;25:8-18. Function-impairing polymorphisms of the hepatic uptake transporter SLCO1B1 modify the therapeutic efficacy of statins in a population-based cohort. Meyer zu Schwabedissen HE1, Albers M, Baumeister SE, Rimmbach C, Nauck M, Wallaschofski H, Siegmund W, Völzke H, Kroemer HK. PubMed

Invest Radiol. 2014;49:78-86. IMAGING. Characterization of the intestinal and hepatic uptake/efflux transport of the magnetic resonance imaging contrast agent gadolinium-ethoxylbenzyl-diethylenetriamine-pentaacetic acid. Jia J, Puls D, Oswald S, Jedlitschky G, Kühn JP, Weitschies W, Hosten N, Siegmund W, Keiser M. PubMed

Mol Pharm. 2014;11:3547-55. Protein abundance of clinically relevant multidrug transporters along the entire length of the human intestine. Drozdzik M, Gröer C, Penski J, Lapczuk J, Ostrowski M, Lai Y, Prasad B, Unadkat JD, Siegmund W, Oswald S. PubMed

Clin Radiol. 2014;69:1027-33. IMAGING. Feasibility of gadoxetate disodium-enhanced MR cholangiography in chronic cholestatic biliary disease. Kühn JP, Spoerl M, Nassif A, Mester M, Weitschies W, Siegmund W, Hosten N, Mensel B. PubMed

AAPS J. 2013;15:1128-40. Mass spectrometry-based targeted proteomics as a tool to elucidate the expression and function of intestinal drug transporters. Oswald S, Gröer C, Drozdzik M, Siegmund W. PubMed

J Pharm Biomed Anal. 2013;85:253-61. LC-MS/MS-based quantification of clinically relevant intestinal uptake and efflux transporter proteins. Gröer C, Brück S, Lai Y, Paulick A, Busemann A, Heidecke CD, Siegmund W, Oswald S. PubMed

Mol Pharm. 2012;9:2577-81. Pharmaceutical excipients influence the function of human uptake transporting proteins. Engel A, Oswald S, Siegmund W, Keiser M. PubMed

Radiology. 2012;264:741-50.  IMAGING. Visualization of hepatic uptake transporter function in healthy subjects by using gadoxetic acid-enhanced MR imaging. Nassif A, Jia J, Keiser M, Oswald S, Modess C, Nagel S, Weitschies W, Hosten N, Siegmund W, Kühn JP. PubMed

J Chromatogr B Analyt Technol Biomed Life Sci. 2012;891-892:20-6.  IMAGING. A LC-MS/MS method to evaluate the hepatic uptake of the liver-specific magnetic resonance imaging contrast agent gadoxetate (Gd-EOB-DTPA) in vitro and in humans. Jia J, Keiser M, Nassif A, Siegmund W, Oswald S. PubMed

Clin Pharmacol Ther. 2012;91:506-13. Impact of efavirenz on intestinal metabolism and transport: insights from an interaction study with ezetimibe in healthy volunteers. Oswald S, Meyer zu Schwabedissen HE, Nassif A, Modess C, Desta Z, Ogburn ET, Mostertz J, Keiser M, Jia J, Hubeny A, Ulrich A, Runge D, Marinova M, Lütjohann D, Kroemer HK, Siegmund W. PubMed

Drug Metab Dispos. 2012;40:522-8. Clarithromycin is absorbed by an intestinal uptake mechanism that is sensitive to major inhibition by rifampicin: results of a short-term drug interaction study in foals. Peters J, Eggers K, Oswald S, Block W, Lütjohann D, Lämmer M, Venner M, Siegmund W. PubMed

Clin Pharmacol Ther. 2011;89:524-8. Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers. Oswald S1, Nassif A, Modess C, Keiser M, Ulrich A, Runge D, Hanke U, Lütjohann D, Engel A, Weitschies W, Siegmund W. PubMed

Handb Exp Pharmacol. 2011;201:403-47. In vivo probes of drug transport: commonly used probe drugs to assess function of intestinal P-glycoprotein (ABCB1) in humans. Oswald S, Terhaag B, Siegmund W. PubMed

Drug Metab Dispos. 2010;38:1024-8. IMAGING. Hepatic uptake of the magnetic resonance imaging contrast agent Gd-EOB-DTPA: role of human organic anion transporters. Leonhardt M, Keiser M, Oswald S, Kühn J, Jia J, Grube M, Kroemer HK, Siegmund W, Weitschies W. PubMed

Clin Pharmacol Ther. 2010;87:663-7. Pharmacokinetic and pharmacodynamic interactions between the immunosuppressant sirolimus and the lipid-lowering drug ezetimibe in healthy volunteers. Oswald S, Nassif A, Modess C, Keiser M, Hanke U, Engel A, Lütjohann D, Weitschies W, Siegmund W. PubMed

J Pharm Sci. 2010;99:422-9. Synergistic influence of Abcb1 and Abcc2 on disposition and sterol lowering effects of ezetimibe in rats. Oswald S, May K, Rosin J, Lütjohann D, Siegmund W. PubMed

J Biol Chem. 2010;285:11336-47. Rapid modulation of the organic anion transporting polypeptide 2B1 (OATP2B1, SLCO2B1) function by protein kinase C-mediated internalization. Köck K, Koenen A, Giese B, Fraunholz M, May K, Siegmund W, Hammer E, Völker U, Jedlitschky G, Kroemer HK, Grube M. PubMed

AJR Am J Roentgenol. 2009;193:1318-23. IMAGING. Normal dynamic MRI enhancement patterns of the upper abdominal organs: gadoxetic acid compared with gadobutrol. Kühn JP, Hegenscheid K, Siegmund W, Froehlich CP, Hosten N, Puls R. PubMed

Pharmacogenet Genomics. 2008;18:559-68. Disposition of ezetimibe is influenced by polymorphisms of the hepatic uptake carrier OATP1B1. Oswald S, König J, Lütjohann D, Giessmann T, Kroemer HK, Rimmbach C, Rosskopf D, Fromm MF, Siegmund W. PubMed

Xenobiotica. 2007;37:1171-95. Transporter-mediated uptake into cellular compartments. Oswald S, Grube M, Siegmund W, Kroemer HK. PubMed

J Pharm Sci. 2007;96:3478-84. Disposition of the cholesterol absorption inhibitor ezetimibe in mdr1a/b (-/-) mice. Oswald S, Koll C, Siegmund W. PubMed

Clin Pharmacol Ther. 2006;80:477-85. Disposition and sterol-lowering effect of ezetimibe are influenced by single-dose coadministration of rifampin, an inhibitor of multidrug transport proteins. Oswald S, Giessmann T, Luetjohann D, Wegner D, Rosskopf D, Weitschies W, Siegmund W. PubMed

J Pharmacol Exp Ther. 2006;318:1293-9. Disposition and sterol-lowering effect of ezetimibe in multidrug resistance-associated protein 2-deficient rats. Oswald S, Westrup S, Grube M, Kroemer HK, Weitschies W, Siegmund W. PubMed

Clin Pharmacol Ther. 2006;79:206-17.  Intestinal expression of P-glycoprotein (ABCB1), multidrug resistance associated protein 2 (ABCC2), and uridine diphosphate-glucuronosyltransferase 1A1 predicts the disposition and modulates the effects of the cholesterol absorption inhibitor ezetimibe in humans. Oswald S, Haenisch S, Fricke C, Sudhop T, Remmler C, Giessmann T, Jedlitschky G, Adam U, Dazert E, Warzok R, Wacke W, Cascorbi I, Kroemer HK, Weitschies W, von Bergmann K, Siegmund W. PubMed

J Chromatogr B Analyt Technol Biomed Life Sci. 2006;830:143-50. A LC-MS/MS method to quantify the novel cholesterol lowering drug ezetimibe in human serum, urine and feces in healthy subjects genotyped for SLCO1B1. Oswald S, Scheuch E, Cascorbi I, Siegmund W. PubMed