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3D model (JSmol)
ECHA InfoCard 100.171.075
Molar mass 424.44 g·mol−1
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Zibotentan (INN; development code ZD4054) is an experimental anti-cancer drug candidate in development by AstraZeneca.[1] It is an endothelin receptor antagonist.[2]

Zibotentan was granted fast track status for the treatment of prostate cancer by the FDA.

It failed a phase III clinical trial for prostate cancer,[3] but other trials are planned.[4] Tolerability of zibotentan plus docetaxel has been evaluated.[5]

Zibotentan has also been studied in clinical trials for treatment of breast cancer, colorectal cancer, non-small cell lung cancer, ovarian cancer, scleroderma-related renal disease,[6] bone metastasis, and heart failure.[7]


  1. ^ James and Growcott (2009). "Drugs of the Future".
  2. ^ Tomkinson H, Kemp J, Oliver S, Swaisland H, Taboada M, Morris T (2011). "Pharmacokinetics and tolerability of zibotentan (ZD4054) in subjects with hepatic or renal impairment: two open-label comparative studies". BMC Clin Pharmacol. 11: 3. doi:10.1186/1472-6904-11-3. PMC 3070638. PMID 21414193.
  3. ^ "AZ's zibotentan flunks late-stage prostate cancer trial - FierceBiotech". www.fiercebiotech.com. Retrieved 16 April 2018.
  4. ^ "Pfizer, AstraZeneca, and Actelion Separately Report Phase III Trial Failures - GEN". GEN. Retrieved 16 April 2018.
  5. ^ Trump DL, Payne H, Miller K, et al. (September 2011). "Preliminary study of the specific endothelin a receptor antagonist zibotentan in combination with docetaxel in patients with metastatic castration-resistant prostate cancer". Prostate. 71 (12): 1264–75. doi:10.1002/pros.21342. PMID 21271613.
  6. ^ "A Phase II, Single Centre, Randomised, Placebo-controlled, 3-part Trial to Assess the Safety, Tolerability and Efficacy of Zibotentan in Patients With Renal Disease Secondary to Scleroderma - AdisInsight". adisinsight.springer.com. Retrieved 16 April 2018.
  7. ^ "Zibotentan - AdisInsight". adisinsight.springer.com. Retrieved 16 April 2018.

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