Chemistry:ZD6126

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Short description: Chemical compound
ZD6126
Skeletal formula
Ball-and-stick model
Clinical data
Other namesANG 453; AZD 6126; N-Acetylcolchicinol dihydrogenphosphate
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC20H24NO8P
Molar mass437.385 g·mol−1
3D model (JSmol)
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ZD6126 is a vascular-targeting agent and a prodrug of N-acetylcolchinol, related to colchicine.[1] It has shown promising results on tumors in mice.[2]

A phase I clinical trial identified gastrointestinal and cardiac effects as limiting dosing.[3] Two phase II clinical trials were suspended investigating ZD6126 in metastatic renal cell carcinoma and metastatic colorectal cancer.[4]

ZD6126 was being investigated by AstraZeneca as a vascular disrupting agent (VDA). However, the trials were halted, after it became apparent that ZD6126 was too cardiotoxic at the required doses.[5]

References

  1. "ZD6126". NCI Drug Dictionary. U.S. National Cancer Institute. http://www.cancer.gov/Templates/drugdictionary.aspx?CdrID=353153. 
  2. "Activity of a new vascular targeting agent, ZD6126, in pulmonary metastases by human lung adenocarcinoma in nude mice". Cancer Research 62 (13): 3711–5. July 2002. PMID 12097279. http://cancerres.aacrjournals.org/cgi/content/abstract/62/13/3711. 
  3. "Phase I clinical evaluation of ZD6126, a novel vascular-targeting agent, in patients with solid tumors". Investigational New Drugs 26 (2): 159–67. April 2008. doi:10.1007/s10637-008-9112-9. PMID 18219445. 
  4. "ZD6126". ClinicalTrialsGov. U.S. National Library of Medicine. http://www.clinicaltrials.gov/ct2/results?term=zd6126. 
  5. "Vascular disrupting agents". Bioorganic & Medicinal Chemistry 15 (2): 605–15. January 2007. doi:10.1016/j.bmc.2006.10.020. PMID 17070061.