Enzo reports publication of study on breast cancer therapeutic candidate

Enzo Biochem reported the publication of a study in the Journal of Lipid Research by researchers at a collaborating institution that shows SK1-I, the company’s proprietary Sphingosine Kinase 1 inhibitor drug candidate, was effective in reversing resistance to the breast cancer drug tamoxifen in a tamoxifen-resistant human breast cancer cell line. As pointed out in the publication, endocrine therapy, such as tamoxifen, is a first line treatment for estrogen receptor-positive breast cancer patients. However, more than 50% of patients who initially respond to tamoxifen ultimately fail therapy due to the development of resistance. These results suggest that SK1-I may have potential in the treatment of tamoxifen-resistant breast cancers. Sphingosine Kinase 1 is a key enzyme in the Sphingosine pathway that has been implicated in tumor cell growth and pathological inflammation. The enzyme acts by phosphorylating the cellular lipid Sphingosine to Sphingosine 1-Phosphate, an important biological mediator of tumor cell proliferation and drug resistance in various cancers, and of immune function. SK1-I is a small molecule that specifically inhibits Sphingosine Kinase 1 and has shown anti-cancer activity in various models of hematological cancers, such as Acute Lymphoblastic Leukemia, and solid tumors, such as glioblastoma. As a result of Enzo’s research, a novel solid tumor indication for SK1-I has also recently been validated in multiple in vitro human tumor cell line models and is undergoing further development. In further support of this program, Enzo has established in-house GMP manufacturing of SK1-I and is planning to initiate in vivo tumor xenograft studies for the lead solid tumor indication using the GMP-manufactured compound in the near term. The company is also exploring various partnership approaches for the continued development of the compound. Apart from oncology, in the immunoregulation area, another of Enzo’s research collaborators has shown that SK1-I prevents the induction of Interferon Gamma, a major inflammatory biomarker, in a well-established Concanavalin A induced animal model of autoimmune hepatitis. The compound SK1-I and related compounds, as well as their use in oncology and other therapeutic areas, are covered by a family of issued U.S. patents co-owned by Enzo and Virginia Commonwealth University and exclusively licensed by VCU to Enzo. Foreign patent family members have also issued or been allowed. The basic patent terms of the U.S. patents in this patent family continue into 2029, before possible extensions. On May 22, 2018, the latest patent in this family, U.S. Patent No. 9,974,758, which is directed to methods for treating cancer using SK1-I, was issued.
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