.Pharmacolibrary.Drugs.C_CardiovascularSystem.C04A_PeripheralVasodilators.C04AX33_Clazosentan.Clazosentan

Information

Clazosentan is a selective endothelin A (ETA) receptor antagonist developed primarily for the prevention and treatment of cerebral vasospasm following aneurysmal subarachnoid hemorrhage (aSAH). It acts to inhibit vasoconstriction mediated by endothelin-1, thereby improving cerebral blood flow. Clazosentan is approved for use in some regions such as Japan, but not widely approved globally.

Pharmacokinetics

Pharmacokinetic parameters derived from healthy adult subjects after intravenous dosing.

References

1. van Giersbergen, PL, et al., & Dingemanse, J (2007). Influence of ethnic origin and sex on the pharmacokinetics of clazosentan. Journal of clinical pharmacology 47(11) 1374–1380. DOI:10.1177/0091270007307337 PUBMED:https://pubmed.ncbi.nlm.nih.gov/17906281

2. Henrich, A, et al., & Krause, A (2021). PK/PD modeling of a clazosentan thorough QT study with hysteresis in concentration-QT and RR-QT. Journal of pharmacokinetics and pharmacodynamics 48(2) 213–224. DOI:10.1007/s10928-020-09728-7 PUBMED:https://pubmed.ncbi.nlm.nih.gov/33389549

3. Volz, AK, et al., & Lehr, T (2019). Target-Mediated Population Pharmacokinetic Modeling of Endothelin Receptor Antagonists. Pharmaceutical research 37(1) 2–None. DOI:10.1007/s11095-019-2723-3 PUBMED:https://pubmed.ncbi.nlm.nih.gov/31823033

Revisions

• 06/2025 initial generated model