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

Research output: Contribution to journalArticlepeer-review

44 Citations (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.

Original languageEnglish
Pages (from-to)419-423
Number of pages5
JournalJournal of Pharmacy and Pharmacology
Issue number3
Publication statusPublished - 2002
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science


Dive into the research topics of 'Simvastatin and lovastatin, but not pravastatin, interact with MDR1'. Together they form a unique fingerprint.

Cite this