"目录号: HY-14798
Palifosfamide是一种新的DNA烷化剂和异环磷酰胺的活性代谢物， 具有抗癌活性。
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生物活性
Description
Palifosfamide is a novel DNA alkylator and the active metabolite of ifosfamide, with antitumor activity.
In Vitro
Palifosfamide lysine (ZIO-201) is a stable form of palifosfamide. Palifosfamide lysine has broad activity in sarcoma linesin vitro. TheIC50ranges from 2.25 ro 6.75 μM for most cell lines except OS222 (IC50=31.5 μM)[1].
In Vivo
Tumor growth inhibition is seen in both OS31 and OS33 xenografts and the RMS xenograft resulting in a significant difference in event-free survival between the control and the treated groups. Differential gene expression of ALDH3A1 but not ALDH1A1 is noted in the OS31 xenograft[1]. Stabilized palifosfamide administered to mice suppresses MX-1 tumor growth by greater than 80% with 17% complete antitumor responses. Oral bioavailability in rats is 48-73% of parenteral administration, and antitumor activity in mice is equivalent by both routes. Treatment with palifosfamide-tris combined with docetaxelor doxorubicin at optimal regimens results in complete tumor regression in 62-75% of mice[2].
Clinical Trial
University of Maryland-United States Air Force
Traumatic Brain Injury
October 2016
Vical
Influenza
August 2007
Phase 1
Vical
Influenza
August 2007
Phase 1
Ziopharm
Advanced Solid Tumors
June 2011
Phase 1
Indiana University School of Medicine-Ziopharm-Indiana University
Adult Central Nervous System Germ Cell Tumor-Adult Teratoma-Malignant Extragonadal Germ Cell Tumor-Malignant Extragonadal Non-Seminomatous Germ Cell Tumor-Extragonadal Seminoma-Recurrent Malignant Testicular Germ Cell Tumor-Recurrent Ovarian Germ Cell Tumor-Stage IV Extragonadal Non-Seminomatous Germ Cell Tumor-Stage IV Extragonadal Seminoma-Stage IV Ovarian Germ Cell Tumor
February 2013
Phase 2
Ziopharm
Soft Tissue Sarcoma
August 2008
Phase 2
Ziopharm
Malignancy-Cancer-Non Small Cell Lung Cancer-Small Cell Lung Cancer-Testicular Cancer-Thymoma-Ovarian Cancer-Osteosarcoma
November 2010
Phase 1
Ziopharm
Soft Tissue Sarcoma
July 2010
Phase 3
Ziopharm
Advanced Cancer
March 2008
Phase 1
Ziopharm
Extensive-Stage Small Cell Lung Cancer
May 2012
Phase 3
Ziopharm
Breast Cancer Nos Metastatic Recurrent
March 2013
Phase 2
Ziopharm
Advanced Cancer
January 2008
Phase 1
Ziopharm
Advanced Sarcoma
February 2006
Phase 1-Phase 2
Ziopharm
Advanced Cancer
February 2006
Phase 1
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