Zibotentan

Product Description

Zibotentan, ZD4054, is a potent antagonist of Endothelin A (ETA, IC50 = 13nM) with no effect at the ETB receptor nor at a broad panel of other targets. In a range of tumour cell lines including osteoblast, vascular myoepithelial, prostate, breast, and ovarian, ZD4054 inhibits pro-oncologic behavior such as inhibition of apoptosis and cellular proliferation. In murine tumor xenograft models of prostate, ovarian, breast, and other cancers, ZD4054 inhibited tumour cell proliferation and mortality when dosed at concentrations of 10mg/kg/day, ip or 50mg/kg/day, po. ZD4054 also inhibited blood vessel growth into the above tumour explants at concentrations of 25 and 50mg/kg/day, po. (Sourced from: https://openinnovation.astrazeneca.com/preclinical-research/preclinical-molecules/zibotentan.html)

Mechanisms of Action: ETa Antagonist

Novel Mechanism: No

Modality: Small Molecule

Route of Administration: Oral

FDA Designation: None *

Approval Status: Not Approved

Approved Countries: None

Approved Indications: None

Known Adverse Events: None

Company: AstraZeneca
Company Location: CAMBRIDGE X0 CB2 0AA
Company CEO: Pascal Soriot
Additonal Commercial Interests: None