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2020•PubMedRequires access

Effects of cyclosporin A on the pharmacokinetics and toxicities of irinotecan mediated by UGT1A1 in vitro and in vivo.

Yanjie Qin, Nanxi Wang, Fen Chen, Xuemei Han, Ying Zhu, Ying Rang, Xuejia Zhai, Yongning Lu

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Abstract

of CsA for UGT1A1 enzyme was 9.4 μM. Furthermore, the UGT1A1 mRNA and protein expression levels were significantly reduced. The present study indicated that CsA treatment could enhance the systemic exposure and toxicity of SN-38 by inhibiting the UGT1A1 enzyme. The inhibition of UGT1A1 enzyme might be a critical factor in the failure of CsA improving irinotecan's treatment index.

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of CsA for UGT1A1 enzyme was 9.4 μM. Furthermore, the UGT1A1 mRNA and protein expression levels were significantly reduced. The present study indicated that CsA treatment could enhance the systemic exposure and toxicity of SN-38 by inhibiting the UGT1A1 enzyme. The inhibition of UGT1A1 enzyme might be a critical factor in the failure of CsA improving irinotecan's treatment index.

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Available abstract

of CsA for UGT1A1 enzyme was 9.4 μM. Furthermore, the UGT1A1 mRNA and protein expression levels were significantly reduced. The present study indicated that CsA treatment could enhance the systemic exposure and toxicity of SN-38 by inhibiting the UGT1A1 enzyme. The inhibition of UGT1A1 enzyme might be a critical factor in the failure of CsA improving irinotecan's treatment index.

Key concepts: Irinotecan, Pharmacokinetics, In vivo, Pharmacology, In vitro, Medicine, Chemistry, Internal medicine

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Effects of cyclosporin A on the pharmacokinetics and toxicities of irinotecan mediated by UGT1A1 in vitro and in vivo. — Research Paper | ScholarLens