"目錄號(hào): HY-14798

Cell Cycle/DNA Damage-

Palifosfamide是一種新的DNA烷化劑和異環(huán)磷酰胺的活性代謝物湃番， 具有抗癌活性吠撮。

DNA Alkylator/Crosslinker

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Mitomycin C-Oxaliplatin-Temozolomide-Streptozocin-Carboplatin-Cyclophosphamide-Calicheamicin-Melphalan-Busulfan-Carmustine-RITA-SJG-136-Fotemustine-Lomustine-Satraplatin-

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

NCT02911675

University of Maryland-United States Air Force

Traumatic Brain Injury

October 2016

NCT00694213

Vical

Influenza

August 2007

Phase 1

NCT00709800

Vical

Influenza

August 2007

Phase 1

NCT01340547

Ziopharm

Advanced Solid Tumors

June 2011

Phase 1

NCT01808534

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

NCT00718484

Ziopharm

Soft Tissue Sarcoma

August 2008

Phase 2

NCT01242072

Ziopharm

Malignancy-Cancer-Non Small Cell Lung Cancer-Small Cell Lung Cancer-Testicular Cancer-Thymoma-Ovarian Cancer-Osteosarcoma

November 2010

Phase 1

NCT01168791

Ziopharm

Soft Tissue Sarcoma

July 2010

Phase 3

NCT00607711

Ziopharm

Advanced Cancer

March 2008

Phase 1

NCT01555710

Ziopharm

Extensive-Stage Small Cell Lung Cancer

May 2012

Phase 3

NCT01703754

Ziopharm

Breast Cancer Nos Metastatic Recurrent

March 2013

Phase 2

NCT00608803

Ziopharm

Advanced Cancer

January 2008

Phase 1

NCT00439686

Ziopharm

Advanced Sarcoma

February 2006

Phase 1-Phase 2

NCT00421135

Ziopharm

Advanced Cancer

February 2006

Phase 1

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References

[1].Hingorani P, et al. Preclinical activity of palifosfamide lysine (ZIO-201) in pediatric sarcomas including oxazaphosphorine-resistant osteosarcoma. Cancer Chemother Pharmacol. 2009 Sep;64(4):733-40.

[2].Jones B, et al. Anticancer activity of stabilized palifosfamide in vivo: schedule effects, oral bioavailability, and enhanced activity with docetaxel and doxorubicin. Anticancer Drugs. 2012 Feb;23(2):173-84.