Decreased biotolerability for ivermectin and cyclosporin A in mice exposed to potent P-glycoprotein inhibitors

Int J Cancer. 1995 Oct 9;63(2):263-7. doi: 10.1002/ijc.2910630220.


SDZ PSC 833 or SDZ 280-446 are strong blockers of the function of class I mdr gene-encoded P-glycoprotein molecules, which were developed for the reversal of multi-drug-resistance of tumor cells. When treated with such drugs, normal mice may display hypersensitivity to cyclosporin A and ivermectin. The recorded signs of acute toxicity are compatible with alterations of the murine central nervous system functions and with earlier data suggesting that P-glycoprotein expressed at the murine blood-brain barrier might be involved in the exclusion of cyclosporin A or ivermectin from brain tissue.

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors*
  • Animals
  • Blood-Brain Barrier
  • Cyclosporine / administration & dosage*
  • Cyclosporins / pharmacology*
  • Drug Resistance, Multiple
  • Drug Tolerance
  • Hybridization, Genetic
  • Ivermectin / administration & dosage*
  • Mice
  • Mice, Inbred C57BL
  • Mice, Inbred DBA
  • Peptides, Cyclic / pharmacology*


  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Cyclosporins
  • Peptides, Cyclic
  • SDZ 280 446
  • Ivermectin
  • Cyclosporine
  • valspodar