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ABCG2 C421A polymorphisms affect exposure of the epidermal growth factor receptor inhibitor gefitinib.

Investigational new drugs - 1 Dec 2020

Sakamoto Sho, Sato Kazuhiro, Takita Yuri, Izumiya Yuka, Kumagai Naho, Sudo Kazuhisa, Hasegawa Yukiyasu, Yokota Hayato, Akamine Yumiko, Okuda Yuji, Asano Mariko, Takeda Masahide, Sano Masaaki, Miura Masatomo, Nakayama Katsutoshi

Abstract excerpt

ATP-binding castle protein G2 (ABCG2) is thought to inhibit the activities of certain gefitinib transporters, thereby affecting drug pharmacokinetics. The C421A polymorphism affects the function and expression of ABCG2 on the cell membrane. Previous studies have shown that proton-pump inhibitors (PPIs) inhibit gefitinib absorption, as well as the function of ABCG2. We evaluated the plasma concentrations of...

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PMID: 32436059
DOI: 10.1007/s10637-020-00946-x

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