regression in acute myologenous leukemia (AML) xenograft models
(Abstract No. 4974). In an oral presentation entitled, "A potent
small molecule PIM kinase inhibitor with activity in cell lines from
hematological and solid malignancies," Dr. Steven Warner, SuperGen's
Manager, Discovery Biology, detailed how scientists used the
Company's CLIMB(TM) technology to build a model that allowed for the
creation of small molecule PIM kinase inhibitors. SGI-1776 was
identified as a potent and selective inhibitor of the PIM kinases,
inducing apoptosis and cell cycle arrest, thereby causing a
reduction in phospho-BAD levels and enhancement of mTOR inhibition
in vitro. SGI-1776 induced significant tumor regression in MV-4-11
(AML) and MOLM-13 (AML) xenograft models.
-- MP-470, a clinical-stage multi-targeted tyrosine kinase inhibitor
and Rad51 suppressor, was shown to be bioavailable and safe in
humans (Abstract No. 4083). The presentation entitled, "MP-470, a
potent oral Rad51 suppressor is safe and tolerable in first-in-human
study," summarized the data indicating that MP-470 can be safely
administered in doses of up to 900 mg per day. Additionally, it was
found that Rad51 expression is modulated in a dose-dependent manner.
This is consistent with pre-clinical studies where MP-470 was shown
to sensitize cancer cells to DNA damaging agents and radiation
therapy by suppressing Rad51, a protein responsible for repair of
double strand DNA breaks in cancer cells.
-- MP-470 was shown to effectively sensitize prostate and breast cancer
cells to erlotinib (Abstract No. 671). The presentation entitled,
|SOURCE SuperGen Inc.|
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