ZD6126
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| 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".]] |
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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- ↑ ZD6126, National Cancer Institute summary
- ↑ 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.
- ↑ 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.
- ↑ astrazenecaclinicaltrials.com
- ↑ ZD6126, National Institutes of Health summary
- ↑ Lippert John W. III (2007). "Vascular disrupting agents". Bioorganic & Medicinal Chemistry 15 (2): 605-615. [1]
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