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Zibotentan

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Zibotentan
Names
Preferred IUPAC name N-(3-Methoxy-5-methylpyrazin-2-yl)-2-pyridine-3-sulfonamide
Other names ZD4054
Identifiers
CAS Number
3D model (JSmol)
ChEBI
ChemSpider
ECHA InfoCard 100.171.075 Edit this at Wikidata
IUPHAR/BPS
PubChem CID
UNII
CompTox Dashboard (EPA)
InChI
  • 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)Key: FJHHZXWJVIEFGJ-UHFFFAOYSA-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
SMILES
  • O=S(=O)(Nc1ncc(nc1OC)C)c4cccnc4c3ccc(c2nnco2)cc3
Properties
Chemical formula C19H16N6O4S
Molar mass 424.44 g·mol
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). ☒N verify (what is  ?) Infobox references
Chemical compound

Zibotentan (INN; development code ZD4054) is an experimental anti-cancer drug candidate in development by AstraZeneca. It is an endothelin receptor antagonist.

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, but other trials are planned. Tolerability of zibotentan plus docetaxel has been evaluated.

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, bone metastasis, and heart failure.

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. 28 September 2010. 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. S2CID 29707062.
  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.

External links

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