Clazosentan

Clazosentan (INN, trade name Pivlaz[1]) is a drug belonging to the class of endothelin receptor antagonists.

Clazosentan
Clazosentan molecule
Identifiers
  • 5-methyl-pyridin-2-sulfonic acid{6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-[2-(1H-tetrazol-5-yl)-pyridin-4-yl]-pyrimidin-4-yl}amide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC25H23N9O6S
Molar mass577.58 g·mol−1
3D model (JSmol)
  • CC1=CN=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=CC(=NC=C3)C4=NNN=N4)OCCO)OC5=CC=CC=C5OC
  • InChI=1S/C25H23N9O6S/c1-15-7-8-20(27-14-15)41(36,37)32-24-21(40-19-6-4-3-5-18(19)38-2)25(39-12-11-35)29-22(28-24)16-9-10-26-17(13-16)23-30-33-34-31-23/h3-10,13-14,35H,11-12H2,1-2H3,(H,28,29,32)(H,30,31,33,34)
  • Key:LFWCJABOXHSRGC-UHFFFAOYSA-N

Mechanism

The endothelin 1 receptor is one of the strongest known vasoconstrictors. After subarachnoidal bleedings, irritation of the blood vessels can lead to a vasospasm and thus to an ischaemia, an insufficient blood supply to brain tissue. One possible effect of this is, in turn, an ischaemic stroke.

Trials

In a randomized trial with patients who had aneurysmal subarachnoid bleeding and were being treated with endovascular coiling, 15 mg/h clazosentan significantly reduced vasospasm-related morbidity and all-cause mortality. Clazosentan, however, did not improve the neurological outcome as measured by the extended Glascow Outcome Scale.[2]

References
  1. "Idorsia receives Japanese PMDA approval of PIVLAZ" (Press release). GlobalNewsWire. 2022-01-20. Retrieved 2022-01-22.
  2. Macdonald RL, Higashida RT, Keller E, Mayer SA, Molyneux A, Raabe A, et al. (June 2012). "Randomized trial of clazosentan in patients with aneurysmal subarachnoid hemorrhage undergoing endovascular coiling". Stroke. 43 (6): 1463–1469. doi:10.1161/STROKEAHA.111.648980. PMID 22403047. S2CID 3113695.
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