Zibotentan

Structural formula
General
Non-proprietary name	Zibotentan
other names	N - (3-methoxy-5-methylpyrazin-2-yl) -2- [4- (1,3,4-oxadiazol-2-yl) phenyl] pyridine-3-sulfonamide ( IUPAC ) ; ZD4054;
Molecular formula	C 19 H 16 N 6 O 4 S
External identifiers / databases
EC number	643-052-5
ECHA InfoCard	100.171.075
PubChem	9910224
ChemSpider	8085875
DrugBank	DB06629
Wikidata	Q198371
Drug information
Drug class	Cytostatic
Mechanism of action	Endothelin A receptor - antagonist
properties
Molar mass	424.433 g · mol -1
safety instructions
H and P phrases	H: 360-373-411
	P: 301 + 312 + 330
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Zibotentan is a potential orally administered cytostatic agent for the treatment of hormone-resistant prostate cancer . It is currently in phase 3 clinical trials .

Zibotentan is being developed by the British pharmaceutical company AstraZeneca . The ethanolamine salt is used medicinally .

Mechanism of action

Zibotentan is a selective endothelin A receptor antagonist . Its plasma half-life is 8 hours and the plasma protein binding is 73.8%.

literature

AstraZeneca, ZD4054 information to support Pre-clinical Studies: AstraZeneca, 7pp., 2005

CD.Morris, A.Rose, J.Curwen, AM.Hughes, DJ.Wilson, DJ.Webb. Specific inhibition of the endothelin A receptor with ZD4054: clinical and pre-clinical evidence. Br J Cancer .92,2005

WR.Schelman, G.Liu, G.Wilding, T.Morris, D.Phung, R. Dreicer. Investigational New Drugs , A phase I study of zibotentan (ZD4054) in patients with metastatic, castrate-resistant prostate cancer. DOI , 10.1007 / s10637-009-9318-5.2009

Individual evidence

↑ Template: CL Inventory / not harmonized There is not yet a harmonized classification for this substance . A labeling of N- (3-methoxy-5-methyl-2-pyrazinyl) -2- [4- (1,3,4-oxadiazol-2-yl) phenyl] -3- is shown, which is derived from a self-classification by the distributor pyridinesulfonamide in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on February 10, 2020.

↑ Zibotentan data sheet from Sigma-Aldrich , accessed on February 10, 2020 ( PDF ).

[1] Template: CL Inventory / not harmonized There is not yet a harmonized classification for this substance . A labeling of N- (3-methoxy-5-methyl-2-pyrazinyl) -2- [4- (1,3,4-oxadiazol-2-yl) phenyl] -3- is shown, which is derived from a self-classification by the distributor pyridinesulfonamide in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on February 10, 2020.

[Sigma-2] Zibotentan data sheet from Sigma-Aldrich , accessed on February 10, 2020 ( PDF ).