Zibotentan

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
Names
Preferred IUPAC name
N-(3-Methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide
Other names
ZD4054
Identifiers
3D model (JSmol)
ChemSpider
ECHA InfoCard 100.171.075
UNII
  • InChI=1S/C19H16N6O4S/c1-12-10-21-17(19(23-12)28-2)25-30(26,27)15-4-3-9-20-16(15)13-5-7-14(8-6-13)18-24-22-11-29-18/h3-11H,1-2H3,(H,21,25) ☒N
    Key: FJHHZXWJVIEFGJ-UHFFFAOYSA-N ☒N
  • InChI=1/C19H16N6O4S/c1-12-10-21-17(19(23-12)28-2)25-30(26,27)15-4-3-9-20-16(15)13-5-7-14(8-6-13)18-24-22-11-29-18/h3-11H,1-2H3,(H,21,25)
    Key: FJHHZXWJVIEFGJ-UHFFFAOYAL
  • O=S(=O)(Nc1ncc(nc1OC)C)c4cccnc4c3ccc(c2nnco2)cc3
Properties
C19H16N6O4S
Molar mass 424.44 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references

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]

References
  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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