Endothelinen: mogelijk een nieuw farmacologisch aangrijpingspunt bij hart- en vaatziekten, nierziekten en oncologische aandoeningen

– Only 10 years ago, the vasoconstricting peptide endothelin was discovered; it is produced by endothelial cells.

– Different isoforms and receptors of endothelin have been identified. The effects of endothelin-1, the most important isoform, are mainly vasoconstriction and proliferation of cells.

– In the last few years endothelin receptor antagonists have become available, which can delineate the clinical importance of the endothelin system.

– Possible indications for endothelin receptor blockers are renal disease (acute and chronic renal failure) and cardiovascular disease (heart failure; restenosis after percutaneous transluminal coronary angioplasty (PTCA); pulmonary hypertension; systemic hypertension).

– There is also a possible role for endothelin receptor blockers in oncology (prostatic carcinoma).

– Currently clinical trials are being carried out to determine the efficacy of these compounds for the above-mentioned indications.