Abstract
Overexpression of drug efflux pumps is one of the main reasons for the development of multi-drug resistant tumours and bacterial and fungal infections. Inhibition of these pumps gives rise to a restoration of drug sensitivity and thus represents a versatile approach for overcoming multi-drug resistance. Although clinical trials were not as encouraging as expected, several compounds are currently undergoing Phase III clinical studies. This review gives an overview on the patent literature (from the year 2000 to mid 2003) on the field of inhibitors of drug efflux pumps.