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prodrug increases its in vivo efficacy due to enhanced drug delivery
and stability," highlighted data indicating that S-110 showed robust
anti-tumor activity in prostate and cisplatin-resistant ovarian
carcinoma xenograft models. Additionally, S-110 restored sensitivity
to cisplatin in the ovarian cancer model. Reduced toxicity was
observed along with an increased half-life compared to decitabine.
-- June 2008: The Company had two abstracts accepted for oral and poster
presentation at the 13th Congress of the European Hematology
Association (EHA) that took place June 12-15, 2008 in Copenhagen,
Denmark. Highlights of the presentations are included below:
-- SGI-1776, an oral PIM kinase inhibitor, causes tumor regression in
acute myologenous leukemia (AML) xenograft models (abstract #744).
In a poster presentation entitled "A potent small molecule PIM
kinase inhibitor with in vivo oral availability and activity in cell
lines from hematological malignancies," Dr. Gregory Berk, SuperGen's
Chief Medical Officer, detailed how scientists used the CLIMB
technology to build a model that allowed for the creation of small
molecule PIM kinase inhibitors. SGI-1776 was identified as an
orally available, potent and selective inhibitor of the PIM kinases.
SGI-1776 induces cell cycle arrest, dose dependent apoptosis and a
reduction in phospho-BAD levels in leukemia and lymphoma cell lines.
Phospho-BAD is a direct substrate for PIM, and may serve as a useful
in vivo biomarker for future clinical trials. Most notably,
SGI-1776 induced significant tumor regression in MOLM-13 (AML) and
MV-4-11 (AML) xenograft models.
-- SGI-1252, the Company's JAK2 kinase inhibitor, inhibits tumor cell
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