ZD6126

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ZD6126
File:ZD6126.png
Systematic (IUPAC) name
Phosphoric acid mono-(5-acetylamino-9,10,11-trimethoxy-6,7-dihydro-5H-dibenzo[a,c]cyclohepten-3-yl) ester
Identifiers
CAS Number 219923-05-4
Synonyms ANG 453; AZD 6126; N-Acetylcolchicinol dihydrogenphosphate
Chemical data
Formula C20H24NO8P
Molar mass 437.38 g/mol[[Script error: No such module "String".]]
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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 cancer tumors in mice.[2]

A phase I clinical trial identified gastrointestinal and cardiac effects as limiting dosing.[3] Two phase II clinical trials were started investigating ZD6126 in metastatic renal cell carcinoma and metastatic colorectal cancer.[4] [5]


ZD6126 was being investigated by AstraZeneca as a VDA (vascular disrupting agent). However, the trials were halted, after it became apparent that ZD6126 was too cardiotoxic at the required doses.[6]



References

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  1. Jump up ↑ ZD6126, National Cancer Institute summary
  2. Jump up ↑ Hisatsugu Goto, Seiji Yano, Helong Zhang, Yuka Matsumori, Hirohisa Ogawa, David C. Blakey and Saburo Sone (1 July 2002). "Activity of a New Vascular Targeting Agent, ZD6126, in Pulmonary Metastases by Human Lung Adenocarcinoma in Nude Mice". Cancer Research. 62 (13): 3711–3715. PMID 12097279. 
  3. Jump up ↑ LoRusso Patricia M; Gadgeel Shirish M; Wozniak Antoinette; Barge Alan J; Jones Helen K; DelProposto Zachary S; DeLuca Pamela A; Evelhoch Jeffrey L; Boerner Scott A; Wheeler Catherine (2008). "Phase I clinical evaluation of ZD6126, a novel vascular-targeting agent, in patients with solid tumors". Investigational new drugs. 26 (2): 159–67. doi:10.1007/s10637-008-9112-9. PMID 18219445. 
  4. Jump up ↑ astrazenecaclinicaltrials.com
  5. Jump up ↑ ZD6126, National Institutes of Health summary
  6. Jump up ↑ Lippert John W. III (2007). "Vascular disrupting agents". Bioorganic & Medicinal Chemistry 15 (2): 605-615. [1]
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