https://m2.mtmt.hu/ hun 2026-09-22 08:50 JournalArticle 31523931 VALIDATED true 0 false 2026-05-20T05:19:18.098+0000 2023-12-12T10:07:40.067+0000 2020-08-31T14:40:21.958+0000 true 10010446 Homolya László /api/author/10010446 Author Homolya László (Molekuláris sejtbiológia) true 10010446 2023-12-12T10:07:40.466+0000 2023-12-12T10:07:40.466+0000 2020-10-14T11:26:35.796+0000 true 10062250 Molnár-Taga Márta /api/admin/10062250 Admin Molnár-Taga Márta (SE 4-es admin) true 10062250 2020-12-05T07:45:32.751+0000 true 565 WoS import /api/admin/565 Admin WoS import (admin) true true false true 24 24 /api/publicationtype/24 PublicationType Folyóiratcikk 1 true 24 JournalArticle true 1134514 Survey paper true 24 24 /api/publicationtype/24 PublicationType Folyóiratcikk 1 true 24 JournalArticle /api/subtype/1134514 Összefoglaló cikk SubType Összefoglaló cikk (Folyóiratcikk) 102 true 1134514 true 1 /api/category/1 Category Tudományos true 1 Tátrai, P. true true /api/journal/10022148 REVIEWED PHARMACEUTICS 1999-4923 true false 10022148 false 10022148 true 1999-4923 Journal FOREIGN 12 8 755 755 16 2020 Bilirubin, the end product of heme catabolism, is produced continuously in the body and may reach toxic levels if accumulates in the serum and tissues; therefore, a highly efficient mechanism evolved for its disposition. Normally, unconjugated bilirubin enters hepatocytes through the uptake transporters organic anion transporting polypeptide (OATP) 1B1 and 1B3, undergoes glucuronidation by the Phase II enzyme UDP glucuronosyltransferase 1A1 (UGT1A1), and conjugated forms are excreted into the bile by the canalicular export pump multidrug resistance protein 2 (MRP2). Any remaining conjugated bilirubin is transported back to the blood by MRP3 and passed on for uptake and excretion by downstream hepatocytes or the kidney. The bile salt export pump BSEP as the main motor of bile flow is indirectly involved in bilirubin disposition. Genetic mutations and xenobiotics that interfere with this machinery may impede bilirubin disposition and cause hyperbilirubinemia. Several pharmaceutical compounds are known to cause hyperbilirubinemia via inhibition of OATP1Bs, UGT1A1, or BSEP. Herein we briefly review the in vitro prediction methods that serve to identify drugs with a potential to induce hyperbilirubinemia. In vitro assays can be deployed early in drug development and may help to minimize late-stage attrition. Based on current evidence, drugs that behave as mono-or multispecific inhibitors of OATP1B1, UGT1A1, and BSEP in vitro are at risk of causing clinically significant hyperbilirubinemia. By integrating inhibition data from in vitro assays, drug serum concentrations, and clinical reports of hyperbilirubinemia, predictor cut-off values have been established and are provisionally suggested in this review. Further validation of in vitro readouts to clinical outcomes is expected to enhance the predictive power of these assays. © 2020 by the authors. Licensee MDPI, Basel, Switzerland. true 2020 true true true false true false GOLD 2026-05-20 true https://doi.org/10.3390/pharmaceutics12080755 23 0 23 22 2 23 21 21 19 23 23 22 22 22 1 0 23 22 23 22 0 4 4 Folyóiratcikk Journal Article 24 23 Könyvrészlet Chapter in Book 25 0 Könyv Book 23 0 Egyéb konferenciaközlemény Conference paper 31 0 Egyéb konferenciakötet Conference proceedings 32 0 Oltalmi formák Protection forms 26 0 Disszertáció Thesis 28 0 Egyéb Miscellaneous 29 0 Alkotás Achievement 22 0 Kutatási adat Research data 33 0 Folyóiratcikk Journal Article 24 0 0 0 Könyvrészlet Chapter in Book 25 0 0 0 Könyv Book 23 0 0 0 Egyéb konferenciaközlemény Conference paper 31 0 0 0 Egyéb konferenciakötet Conference proceedings 32 0 0 0 Oltalmi formák Protection forms 26 0 0 0 Disszertáció Thesis 28 0 0 0 Egyéb Miscellaneous 29 0 0 0 Alkotás Achievement 22 0 0 0 Kutatási adat Research data 33 0 0 0 2021 0 2 2 2 2 2022 0 5 5 5 5 2023 0 7 6 7 6 2024 0 1 1 1 1 2025 0 6 6 6 6 2026 0 2 2 2 2 Q1 false 10009464 false false false 2020-10-13T11:26:21.321+0000 Morfológiai és Fiziológiai Tanszék (SE / ETK2007) 2 15 1 2 0 true Language 10002 /api/language/10002 Angol Angol English true 2 true PersonAuthorship 93093572 /api/authorship/93093572 Tátrai, P. [Tátrai, Péter (Biológia), szerző] 1 0.5 true false false Author 10021027 /api/author/10021027 Tátrai Péter (Biológia) Tátrai Péter true 10021027 true Tátrai P. true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 93093573 /api/authorship/93093573 Krajcsi, P. ✉ [Krajcsi, Péter (Transzporter essz...), szerző] Morfológiai és Fiziológiai Tanszék (SE / ETK2007) 2 0.5 false true true Author 10009464 /api/author/10009464 Krajcsi Péter (Transzporter esszék, génterápia, apoptózis) Krajcsi Péter true 10009464 true Krajcsi P. true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PublicationIdentifier 17514314 /api/publicationidentifier/17514314 DOI: 10.3390/pharmaceutics12080755 PlainSource 6 /api/publicationsource/6 DOI PublicationSourceType 10001 /api/publicationsourcetype/10001 DOI true true true DOI DOI https://doi.org/@@@ true true 6 true GOLD true IDENTICAL 10.3390/pharmaceutics12080755 https://doi.org/10.3390/pharmaceutics12080755 false true PublicationIdentifier 17754094 /api/publicationidentifier/17754094 WoS: 000564096600001 PlainSource 1 /api/publicationsource/1 WoS PublicationSourceType 10003 /api/publicationsourcetype/10003 Indexelő adatbázis false true true WoS WoS https://www.webofscience.com/wos/woscc/full-record/@@@ true true 1 true IDENTICAL 000564096600001 https://www.webofscience.com/wos/woscc/full-record/000564096600001 false true PublicationIdentifier 17514313 /api/publicationidentifier/17514313 Scopus: 85089370726 PlainSource 3 /api/publicationsource/3 Scopus PublicationSourceType 10003 /api/publicationsourcetype/10003 Indexelő adatbázis false true true Scopus Scopus http://www.scopus.com/record/display.url?origin=inward&eid=2-s2.0-@@@ true true 3 true IDENTICAL 85089370726 http://www.scopus.com/record/display.url?origin=inward&eid=2-s2.0-85089370726 false true PublicationIdentifier 17754095 /api/publicationidentifier/17754095 PubMed: 32796590 PlainSource 17 /api/publicationsource/17 PubMed PublicationSourceType 10003 /api/publicationsourcetype/10003 Indexelő adatbázis false true true PubMed PubMed http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=@@@&dopt=Abstract true true 17 true IDENTICAL 32796590 http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=32796590&dopt=Abstract false true Keyword 4580 /api/keyword/4580 risk assessment true 4580 true Keyword 6585 /api/keyword/6585 In Vitro true 6585 true Keyword 1041699 /api/keyword/1041699 hyperbilirubinemia true 1041699 true Keyword 1567677 /api/keyword/1567677 UGT1A1 true true Keyword 1953761 /api/keyword/1953761 OATP1B1 true true SjrRating 10872106 /api/sjrrating/10872106 sjr:Q1 (2020) Scopus - Pharmaceutical Science PHARMACEUTICS 1999-4923 20 0.24 journal RatingType 10002 /api/ratingtype/10002 sjr sjr true true ClassificationExternal 3003 /api/classificationexternal/3003 Scopus - Pharmaceutical Science true 3003 true Q1 DIRECT true true Reference 2677010 /api/reference/2677010 1. 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Kotsampasakou, E., Escher, S.E., Ecker, G.F., Linking organic anion transporting polypeptide 1B1 and 1B3 (OATP1B1 and OATP1B3) interaction profiles to hepatotoxicity—The hyperbilirubinemia use case (2017) Eur. J. Pharm. Sci, 100, pp. 9-16. , [CrossRef] [PubMed] 84 false true /api/publication/31523931 Tátrai P. et al. Prediction of drug-induced hyperbilirubinemia by in vitro testing. (2020) PHARMACEUTICS 1999-4923 12 8<div class="JournalArticle Publication long-list"> <div class="authors"> <img title="Forrásközlemény" style="float: left" src="/frontend/resources/grid/publication-core-icon.png"> <img title="Idézőközlemény" style="float: left" src="/frontend/resources/grid/publication-citation-icon.png"> <div class="autype autype0"> <span class="author-name" mtid="10021027"><a href="/gui2/?type=authors&mode=browse&sel=10021027" target="_blank">Tátrai P. (<span class="authorship-author-name">Tátrai Péter</span> <span class="authorAux-mtmt"> Biológia</span>) </a> </span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10009464"><a href="/gui2/?type=authors&mode=browse&sel=10009464" target="_blank">Krajcsi P. ✉ (<span class="authorship-author-name">Krajcsi Péter</span> <span class="authorAux-mtmt"> Transzporter esszék, génterápia, apoptózis</span>) </a> </span> <span class="author-affil"><span title="Semmelweis Egyetem">SE</span>/<span title="Egészségtudományi Kar">ETK2007</span>/Morfológiai és Fiziológiai Tanszék</span> </div> </div> <div class="title"><a href="/gui2/?mode=browse&params=publication;31523931" target="_blank">Prediction of drug-induced hyperbilirubinemia by in vitro testing</a></div> <div> <span class="journal-title">PHARMACEUTICS</span> <span class="journal-issn">( <a target="_blank" href="https://portal.issn.org/resource/ISSN/1999-4923">1999-4923</a>)</span>: <span class="journal-volume">12</span> <span class="journal-issue">8</span> <span class="page"> Paper 755. 16 p. </span> <span class="year">(2020)</span> </div> <div class="pub-footer"> <span class="language" xmlns="http://www.w3.org/1999/html">Nyelv: Angol | </span> <span class="identifiers"> <span class="id identifier oa_GOLD" title=" Gold "> <a style="color:blue" title="10.3390/pharmaceutics12080755" target="_blank" href="https://doi.org/10.3390/pharmaceutics12080755"> DOI </a> </span> <span class="id identifier oa_none" title="none"> <a style="color:blue" title="000564096600001" target="_blank" href="https://www.webofscience.com/wos/woscc/full-record/000564096600001"> WoS </a> </span> <span class="id identifier oa_none" title="none"> <a style="color:blue" title="85089370726" target="_blank" href="http://www.scopus.com/record/display.url?origin=inward&eid=2-s2.0-85089370726"> Scopus </a> </span> <span class="id identifier oa_none" title="none"> <a style="color:blue" title="32796590" target="_blank" href="http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=32796590&dopt=Abstract"> PubMed </a> </span> </span> <OnlyViewableByAuthor><div class="ratings"> <div class="journal-subject">Folyóirat szakterülete: Scopus - Pharmaceutical Science&nbsp;&nbsp;&nbsp;SJR indikátor:&nbsp;Q1</div> </div></OnlyViewableByAuthor> <div class="publication-citation" style="margin-left: 0.5cm;"> <span title="Nyilvános idézőközlemények összesen, említések nélkül" class="citingPub-count">Nyilvános idéző összesen: 23</span> | Független: 22 | Függő: 1 | Nem jelölt: 0 | WoS jelölt: 21 | Scopus jelölt:&nbsp;19 | WoS/Scopus jelölt:&nbsp;23 | DOI jelölt:&nbsp;21 </div> <div class="publication-citation"> <a target="_blank" href="/api/publication?cond=citations.related;eq;31523931&sort=publishedYear,desc&sort=title"> Idézett közlemények száma: 4 </a> </div> <div class="mtid"><span class="long-pub-mtid">Közlemény: 31523931</span> | <span class="status-data status-VALIDATED"> Egyeztetett </span> Forrás Idéző | <span class="type-subtype">Folyóiratcikk ( Összefoglaló cikk ) </span> | <span class="pub-category">Tudományos</span> | <span class="publication-sourceOfData">Scopus</span> </div> <div class="lastModified">Utolsó módosítás: 2023.12.12. 11:07 Horváth Viktória (SE_ETK_Admin5_HV, admin) </div> </div></div>