SuperGen’s SGI-1776 was identified as an orally available, potent and selective inhibitor of the PIM kinases. SGI-1776 was found to induce 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 is expected to serve as a useful in vivo biomarker for future clinical trials. SGI-1776 induced significant tumor regression in MOLM-13 and MV-4-11 acute myologenous leukemia (AML) xenograft models.
James Manuso, president and CEO of SuperGen, said: “Our PIM kinase inhibitor, SGI-1776, has the potential to be an effective treatment for AML and other malignancies that over-express PIM kinase. We plan to initiate phase I clinical trials with SGI-1776 in solid tumors and leukemias later this year.”