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A novel small molecule (SMS077) for resistant tumor treatment

THE INNOVATION SMS077 is a novel small molecule that has cytotoxicity against a broad range of tumor cells types and tumor organoids from patient derived samples. SMS077 inhibits tubulin polymerization in cancer cells and acts as a vascular disrupting agent, targeting new and established vasculature networks in vitro. Cells that develop multidrug-resistance to other therapies remain sensitive to SMS077 treatment.
MARKET OPPORTUNITY Increase in cancer prevalence and unmet medical needs of cancer patients drive the global tubulin inhibitor market. Tubulin targeting agents are a type of chemotherapy used in a variety of cancers with a high level of patient response and survival. However, with time patients acquire drug resistance, which leads to discontinuation of the treatment. Since SMS077 has high efficiency in cells, that acquire resistance to other chemotherapies, it represents a better alternative to treat these patients.
TECHNOLOGY Novel microtubule targeting small molecule, with high efficiency in cells that acquire resistant to chemotherapeutic treatments through P-glycoprotein or MRP over-expression.

SMS077 affects tubulin polymerization in tumor cells. Green: Tubulin; Blue: Hoescht

DEVELOPMENT STATUS. SMS077:
✓ Binds to colchicine binding site, and inhibits microtubule polymerization.
✓ Induces cell cycle arrest and apoptosis of cancer cells (low nM
concentration).
✓ Not a substrate for multidrug resistance proteins.
✓ Demonstrated activity against taxane, vinca alkaloid, etoposide, doxorubicin, dexamethasone, melphalan, cisplatin and carboplatin resistant cancer cells.
✓ Has anti-cancer activity against a broad variety of tumor cells types.
✓ Reduces tumor burden in in vivo xenograft model (see below).
PRINCIPAL INVESTIGATORS Dr. Gabriela Rozic is a Senior Scientific, Head of Translational Oncology Unit at the Institute for Personalized and Translational Medicine in Ariel University. She works in collaboration with Dr. Igor Koman, Prof. Merav Leiba and Irit Shapira to identify and validate SMS077 as an effective anti-cancer molecule.