Zibotentan

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Zibotentan
Names
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 Edit this at Wikidata
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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Zibotentan (INN) (earlier code name ZD4054) is an anti-cancer candidate.[1] It is an endothelin receptor antagonist.[2]

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]

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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  3. ^ http://www.fiercebiotech.com/story/azs-zibotentan-flunks-late-stage-prostate-cancer-trial/2010-09-27
  4. ^ http://www.genengnews.com/gen-news-highlights/pfizer-astrazeneca-and-actelion-separately-report-phase-iii-trial-failures/81243985/
  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.

External links

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