On March 3 , 2017 Lin BioScience reported it has licensed the intellectual property portfolio for a novel inhibitor of CDC7 kinase (Press release, Lin Bioscience, MAR 3, 2017, View Source [SID1234520603]). Under this worldwide exclusive licensing agreement with Columbia University and Memorial Sloan Kettering Cancer Center, Lin BioScience plans to develop this potent CDC7 inhibitor (LBS-007) against a wide range of cancers.

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CDC7 is one of two heterodimeric kinases involved in the cell cycle regulation of eukaryotic DNA replication. Activated at the G1/S phase transition, CDC7 activates the helicase that unwinds DNA in preparation for cellular DNA replication. CDC7 is overexpressed in cancer cells, and its inhibition leads to irreparable DNA damage and apoptosis. In normal cells, however, CDC7 inhibition harmlessly stalls the cell cycle, which restarts when levels normalize. This selectivity has made CDC7 a sought-after target for drug makers.

For Mark Frattini, M.D, Ph.D., Associate Professor of Medicine and Experimental Therapeutics at Columbia University Medical Center (CUMC) and Director of Research for the medical center’s Hematologic Malignancies, the licensing of LBS-007, which he developed in collaboration with researchers at Memorial Sloan Kettering Cancer Center, is the culmination of almost a decade of work developing a unique CDC7 inhibitor that is less prone to off-target effects and shows preclinical effectiveness against nearly 80 malignancies, ranging from leukemia and non-small cell lung cancer to melanoma and ovarian cancer.

"CDC7 inhibitors are a new class of anti-cancer therapy, and Lin BioScience is proud to be working with Dr. Mark Frattini and his team at Columbia University, who are leading experts and among the first to develop this novel drug treatment. LBS-007 has shown its potential as a potent agent to treat a variety of cancer indications, and we look forward to initiating a first-in-human Phase 1 trial in 2017," said Dr. Tom Lin, CEO of Lin Bioscience.

Frattini and his collaborators initially focused on hematologic cancers, and have shown strong results of tests on primary patient samples and animal models of multiple hematologic cancers. The first-in-human Phase 1 trial will begin this year in patients with relapsed or refractory acute myeloid leukemia, acute lymphoid leukemia, chronic myeloid leukemia in blast crisis and resistant to oral tyrosine kinase inhibitors, and myelodysplastic syndrome.