Simvastatin and lovastatin, but not pravastatin, interact with MDR1

T. Sakaeda, K. Takara, M. Kakumoto, N. Ohmoto, T. Nakamura, K. Iwaki, Y. Tanigawara, K. Okumura

研究成果: Article査読

44 被引用数 (Scopus)


The 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, pravastatin, was compared with simvastatin and lovastatin from the viewpoint of susceptibility to interaction with or via the multidrug transporter, MDR1 (P-glycoprotein). This was carried out using the MDR1-overexpressing cell line LLC-GA5-COL150, established by transfection of MDR1 cDNA into porcine kidney epithelial LLC-PK1 cells, and [3H]digoxin, which is a well-documented substrate for MDR1. Pravastatin, at 25-100 μM, had no effect on the transcellular transport of [3H]digoxin whereas simvastatin and lovastatin suppressed the basal-to-apical transport of [3H]digoxin and increased the apical-to-basal transport. It was suggested that recognition by MDR1 was due to the hydrophobicity. In conclusion, simvastatin and lovastatin are susceptible to interaction with or via MDR1, but pravastatin is not. This is important information when selecting the HMG-CoA reductase inhibitors for patients taking drugs that are MDR1 substrates.

ジャーナルJournal of Pharmacy and Pharmacology
出版ステータスPublished - 2002

ASJC Scopus subject areas

  • 薬理学
  • 薬科学


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