Description:
IC50 Value: 0.5-1.5mg/ml [1]
Palifosfamide (Zymafos or ZIO-201) references a novel composition (tris formulation) that is the functional active metabolite of ifosfamide (IFOS), a bi-functional DNA alkylator being investigated as a potential therapy for the treatment of soft tissue sarcoma (STS).
in vitro: Palifosfamide lysine was cytotoxic against all the cell lines tested with the IC(50) ranging from 0.5 to 1.5 microg/ml except for OS222, which had an IC(50) of 7 microg/ml [1].
in vivo:  Dose response, route and schedule of administration, and interaction with docetaxel or doxorubicin were investigated in NCr-nu/nu mice bearing established orthotopic mammary MX-1 tumor xenografts. Oral activity was investigated in P388-1 leukemia in CD2F1 mice. Oral and intraperitoneal bioavailabilities were compared in Sprague-Dawley rats. Stabilized palifosfamide administered by optimized regimens suppressed MX-1 tumor growth (P<0.05) by greater than 80% with 17% complete antitumor responses and up to three-fold increase in time to three tumor doublings over controls. Median survival in the P388-1 (P<0.001) model was increased by 9 days over controls [2]. The IV MTD of palifosfamide lysine in mice was 100 mg/kg per day for three consecutive days. Tumor growth inhibition was 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 [1].
Clinical trial: PICASSO: A Study of Palifosfamide Tris Plus Doxorubicin Versus Doxorubicin in Unresectable or Metastatic Soft-Tissue Sarcoma . Phase2