Zibotentan

Source: Wikipedia, the free encyclopedia.
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 Edit this at Wikidata
IUPHAR/BPS
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).
☒N verify (what is checkY☒N ?)

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

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. 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. 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