Novel anti cancer drug for the treatment of Brain
The researchers at Tel Aviv University and Perrigo Pharmaceuticals have developed a platform technology (the Rotem Platform) enabling the development of potent anti cancer drugs based on the chemical modifications of known psychotropics.The leading molecule - Rotem201 – is an NCE derivative of the antidepressant Sertralin. Rotem201 has demonstrated strong anti proliferative and pro-apoptotic effects in vitro in a range of cell lines, including multi drug resistant (MDR) cells. Moreover, Rotem201 demonstrated remarkable anti cancer activity in various xenograft models including human glioma tumors xenografted orthotopically in nude mice. Rotem201 was well tolerated in initial toxicology studies.
Rotem201 may thus serve as a potential drug candidate for the treatment of brain tumors and resistant states of cancer.
The Need Brain tumors are the leading cause of death from childhood cancers among persons up to 19 years and the second leading cause of cancer-related deaths in males ages 20-39. High-grade gliomas, are among the most lethal of all cancers, and cerebral metastases are a common complication among patients with different type of cancer. Treatment includes mainly surgery, when possible, and radiation therapy. Chemotherapy is generally not a very effective treatment for most malignant primary brain tumors or metastatic tumors. Multi drug resistant tumors are related to poor prognosis and outcome. Thus, novel drugs that escape resistance and are able to cross the BBB and effectively kill tumor cells are desperately needed. Potential Applications Cancer treatment Rotem201: treatment of brain cancer (Glioma, Neuroblastoma) and MDR tumors. The Rotem Platform: development of additional derivatives, for the potential treatment of solid tumors such as prostate and colorectal tumors. Potential treatment for non malignant proliferative diseases such as Meningiomas, polyposis, myomas, etc.
Advantages A unique, BBB crossing, anti tumor agent. Rotem201 can be administered per os. Rotem201 is well tolerated in initial toxicology studies. The Rotem platform may enable the formation of additional, NCE's, with potent anti cancer activity for the treatment of solid tumors.
Stage Rotem201 demonstrated potent antiproliferative activity on various cancer cells (lymphoma,leukemia, colon, glioma, epidermal), including MDR cells. Rotem201 reduced tumor burden in nude mice model of human colon cancer, and in a model of orthotopically xenografted human glioma mice. Rotem201 anticancer activity is comparable to other common chemotherapeutic agents (5FU) and shows additive effect in combination with chemotherapeutic agents (Doxorubicine). BBB penetration was demonstrated both in the orthotopically xenografted human glioma and in behavioral models. Rotem201 can be administered orally (behavioral models). Rotem201 is well tolerated in initial toxicology studies. Rotem201 was shown to preserve the antidepressant activity of Sertraline as demonstrated in various behavioral models and receptor binding evaluation.
Inventor(s): Avraham Weizman, Irit Gil-Ad, Moshe Portnoy
Type of Offer: Licensing
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