Clazosentan Explained

Tradename:Pivlaz
Atc Prefix:C04
Atc Suffix:AX33
Legal Status:Rx-only
Cas Number:180384-56-9
Pubchem:6433095
Drugbank:DB06677
Chemspiderid:4938283
Unii:3DRR0X4728
Kegg:D11664
Chembl:109648
Iupac Name:5-methyl-pyridin-2-sulfonic acidamide
C:25
H:23
N:9
O:6
S:1
Smiles: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
Stdinchi: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)
Stdinchikey:LFWCJABOXHSRGC-UHFFFAOYSA-N

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

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]

Notes and References

  1. Idorsia receives Japanese PMDA approval of Pivlaz . Idorsia . GlobalNewsWire . 2022-01-20 . 2022-01-22.
  2. Stephan A. Mayer . Macdonald RL, Higashida RT, Keller E, Mayer SA, Molyneux A, Raabe A, Vajkoczy P, Wanke I, Bach D, Frey A, Nowbakht P, Roux S, Kassell N . Randomized trial of clazosentan in patients with aneurysmal subarachnoid hemorrhage undergoing endovascular coiling . Stroke . 43 . 6 . 1463–1469 . June 2012 . 22403047 . 10.1161/STROKEAHA.111.648980 . 3113695 . free .