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Developed as an oral anticancer drug to treat estrogen receptor–positive breast cancer, GDC‐0810 was shown to be a potent inhibitor of organic anion‐transporting polypeptide 1B1 and 1B3 (OATP1B1/1B3) from an in vitro assay. A clinical study was conducted to assess the drug‐drug interaction potential between GDC‐0810 and pravastatin, which is a relatively selective and sensitive OATP1B1/1B3 substrate...
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