Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction.

  title={Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction.},
  author={Robert S. Foti and Dan A. Rock and Josh T. Pearson and Jan L Wahlstrom and Larry C. Wienkers},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  volume={39 7},
Mibefradil (Posicor) was developed as a calcium channel blocker for the treatment of chronic hypertension. The compound was withdrawn from the market in 1998 because of the potential for rhabdomyolysis, renal failure, or bradycardia when it was coadministered with other drugs. Mibefradil has previously been shown to be a potent reversible (IC(50) = 0.3-2 μM) and mechanism-based (K(i) = 2.3 μM; k(inact) = 0.4 min(-1)) inhibitor of CYP3A4-catalyzed statin metabolism. At present, the mechanism of… CONTINUE READING

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Bioactivation, in: Drug Metabolizing Enzymes: Cytochrome P450 and Other Enzymes in Drug Discovery and Development (Lee JS, Obach

  • J Uetrecht
  • R.S., and Fisher, M.B. ed),
  • 2003
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