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Erlotinib

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.


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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
SLC22A1 OCT1 Erlotinib 86 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
SLC22A1 OCT1 Erlotinib 16.24 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
SLCO2B1 OATP2B1, OATP-B Erlotinib 0.07 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
SLCO1B1 OATP1B1, OATP-C, OATP2, LST-1 Erlotinib 21 21 Estradiol-17beta-glucuronide HEK-OATP1B1 Karlgren, 2012
SLCO1B3 OATP1B3, OATP8 Erlotinib 44 41 Estradiol-17beta-glucuronide HEK293-OATP1B3 Karlgren, 2012
ABCG2 BCRP, MXR Erlotinib 0.13 0.15 Estrone sulfate BCRP-expressing K562 vesicles Noguchi, 2009
SLC22A1 OCT1 Erlotinib 0.356 Metformin HEK293-OCT1 Minematsu, 2011
SLC47A1 MATE1 Erlotinib 8 Metformin HEK293-MATE1 Minematsu, 2011
SLC47A2 MATE2K Erlotinib 3.45 Metformin HEK293-MATE2K Minematsu, 2011
ABCB1 MDR1, P-gp Erlotinib 2 Vincristine MDR1-expressing K562 vesicles Noguchi, 2009

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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