Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug Disposition
The ATP-binding cassette (ABC) transporters play a key role in drug pharmacokinetics. These membrane transporters expressed within physiological barriers can be a source of pharmacokinetic variability. Changes in ABC transporter expression and functionality may consequently affect the disposition of...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-09-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/10/1544 |
| _version_ | 1797513418956079104 |
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| author | Sonia Saib Xavier Delavenne |
| author_facet | Sonia Saib Xavier Delavenne |
| author_sort | Sonia Saib |
| collection | DOAJ |
| description | The ATP-binding cassette (ABC) transporters play a key role in drug pharmacokinetics. These membrane transporters expressed within physiological barriers can be a source of pharmacokinetic variability. Changes in ABC transporter expression and functionality may consequently affect the disposition of substrate drugs, resulting in different drug exposure. Inflammation, present in several acute and chronic diseases, has been identified as a source of modulation in drug transporter expression leading to variability in drug response. Its regulation may be particularly dangerous for drugs with a narrow therapeutic index. In this context, numerous in vitro and in vivo models have shown up- or downregulation in the expression and functionality of ABC transporters under inflammatory conditions. Nevertheless, the existence of contradictory data and the lack of standardization for the models used have led to a less conclusive interpretation of these data. |
| first_indexed | 2024-03-10T06:17:18Z |
| format | Article |
| id | doaj.art-7f071edf2b0540fa9cb81595b4b9ccc6 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T06:17:18Z |
| publishDate | 2021-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-7f071edf2b0540fa9cb81595b4b9ccc62023-11-22T19:37:16ZengMDPI AGPharmaceutics1999-49232021-09-011310154410.3390/pharmaceutics13101544Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug DispositionSonia Saib0Xavier Delavenne1INSERM U1059, Dysfonction Vasculaire et de l’Hémostase, 42270 Saint-Priest-En-Jarez, FranceINSERM U1059, Dysfonction Vasculaire et de l’Hémostase, 42270 Saint-Priest-En-Jarez, FranceThe ATP-binding cassette (ABC) transporters play a key role in drug pharmacokinetics. These membrane transporters expressed within physiological barriers can be a source of pharmacokinetic variability. Changes in ABC transporter expression and functionality may consequently affect the disposition of substrate drugs, resulting in different drug exposure. Inflammation, present in several acute and chronic diseases, has been identified as a source of modulation in drug transporter expression leading to variability in drug response. Its regulation may be particularly dangerous for drugs with a narrow therapeutic index. In this context, numerous in vitro and in vivo models have shown up- or downregulation in the expression and functionality of ABC transporters under inflammatory conditions. Nevertheless, the existence of contradictory data and the lack of standardization for the models used have led to a less conclusive interpretation of these data.https://www.mdpi.com/1999-4923/13/10/1544inflammationABC transporterspharmacokinetic variabilitydrug transport |
| spellingShingle | Sonia Saib Xavier Delavenne Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug Disposition Pharmaceutics inflammation ABC transporters pharmacokinetic variability drug transport |
| title | Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug Disposition |
| title_full | Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug Disposition |
| title_fullStr | Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug Disposition |
| title_full_unstemmed | Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug Disposition |
| title_short | Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug Disposition |
| title_sort | inflammation induces changes in the functional expression of p gp bcrp and mrp2 an overview of different models and consequences for drug disposition |
| topic | inflammation ABC transporters pharmacokinetic variability drug transport |
| url | https://www.mdpi.com/1999-4923/13/10/1544 |
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