Clinical Candidate: Sepin-1 ®
2,2-dimethyl-5-nitro-2H-benzimidazole-1,3-dioxide
Our novel, patent protected Sepin inhibiting compound Sepin-1 selectively eliminates Separase-overexpressing tumor cells while sparing normal cells, and thereby preventing aneuploidy and aneuploidy-associated tumor heterogeneity
Our results indicate that our lead candidate Sepin-1 is not only effective in selectively killing Separase overexpressed tumor cells alone but also exhibits a synergistic effect with existing chemotherapeutic drugs currently used for treating resistant breast cancers.
Sepin-1 well tolerated by the murine and canine models during single- and repeat-dose toxicology studies with no apparent toxicity at pharmacological relevant doses
We have evaluated Sepin-1 in numerous relevant tumor cell lines and xenograft models including, but not limited to BT-474, MCF7, MDA-MB-231 and MDA-MB-231
Q2 2018 DEVELOPMENT STATUS
Chemistry, Manufacturing, and Control (CMC)
Development of an oral formulation
GLP toxicology studies in canines
Animal model testing using oral formulation
IND filing
Intellectual Property
An international PCT “SEPARASE INHIBITORS AND USES THEREOF” (PCT/US2014/061353) was filed on October 20, 2014 and was issued August 21, 2018. The proposal covers the compositions that inhibit Separase activity, including a wide range of envisioned structures including but not limited to Sepin-1. The patent claims over the use of these compounds to treat tumors in various tissues, including but not limited to breast cancer via various administration routes and formulations.
The Baylor Licensing Group disclosure related to this patent is OTA 12-052 “Inhibitors of Cohesin Protease Separase for the Therapy of Aneuploid Human Cancers”.
There are no known encumbrances which will prevent commercial development of the proposed product.
Funding Support
