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Irinotecan

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Km (μM) Cell System Reference
ABCC2 MRP2, cMOAT 48.9 bile canalicular membrane vesicles Chu, 1998
ABCB1 MDR1, P-gp 45.5 MDCK II-MDR1 Luo, 2002
ABCC2 MRP2, cMOAT 90.8 MDCK II-MRP2 Luo, 2002
ABCB1 MDR1, P-gp 116.1 Caco-2 Luo, 2002

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In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
SLC22A2 OCT2 Irinotecan 15.6 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT2 Sandoval, 2018
SLC22A1 OCT1 Irinotecan 20.8 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
SLC22A3 OCT3 Irinotecan 74.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
SLC22A2 OCT2 Irinotecan 2.7 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT2 Wittwer, 2013
SLC47A1 MATE1 Irinotecan 7.9 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE1 Wittwer, 2013
SLC47A2 MATE2K Irinotecan 7.9 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE2K Wittwer, 2013
SLC47A2 MATE2K Irinotecan 78.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE2K Wittwer, 2013
SLC22A2 OCT2 Irinotecan 1.7 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) CHO-OCT2 Sandoval, 2018
SLC22A5 OCTN2 Irinotecan 219 L-carnitine MDCKII-hOCTN2 Diao, 2010
SLC47A1 MATE1 Irinotecan 2.1 Metformin HEK293-MATE1 Wittwer, 2013
SLC47A1 MATE1 Irinotecan 4.3 Metformin MDCK2- MATE1 Wittwer, 2013
SLC22A2 OCT2 Irinotecan 3.3 Metformin CHO-OCT2 Sandoval, 2018
SLC22A1 OCT1 Irinotecan 1.5 Morphine HEK293-OCT1 Tzvetkov, 2013
SLC22A1 OCT1 Irinotecan 1.4 Morphine HEK293-OCT1 Zhu, 2018
SLC22A2 OCT2 Irinotecan 3.2 NBD-MTMA CHO-OCT2 Sandoval, 2018
SLC22A2 OCT2 Irinotecan 4.5 Tetraethylammonium CHO-OCT2 Sandoval, 2018

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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