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1. (WO2017151775) USE OF TRANS-[TETRACHLOROBIS(1H-INDAZOLE)RUTHENATE (III)] FOR THE TREATMENT OF CANCER

Pub. No.:    WO/2017/151775    International Application No.:    PCT/US2017/020209
Publication Date: Sat Sep 09 01:59:59 CEST 2017 International Filing Date: Thu Mar 02 00:59:59 CET 2017
IPC: A61K 31/416
A61K 51/04
A61K 33/14
A61K 39/395
A61K 38/20
A61K 38/21
C07K 16/28
A61P 35/00
Applicants: INTEZYNE TECHNOLOGIES
Inventors: BAKEWELL, Suzanne
SETHURAMAN, Jyothi
Title: USE OF TRANS-[TETRACHLOROBIS(1H-INDAZOLE)RUTHENATE (III)] FOR THE TREATMENT OF CANCER
Abstract:
IT-139, sodium trans-[tetrachlorobis(1H-indazole)ruthenate(III)], is an intravenously administered small molecule compound. In preclinical anti-tumor and mechanism of action studies, IT-139 showed activity against a broad range of tumor types, including those which are resistant to standard anti-cancer agents (e.g., platinums, vinca alkaloids, taxanes, anthracyclines). This activity is believed to arise from IT-139's novel mechanism of action that targets the GRP78 pathway. It was found that up-regulation of GRP78 is a key cancer cell survival pathway. Downregulation of GRP78 using IT-139 removes this resistance pathway allowing for chemotherapy and immuno-oncology agents to be more effective in treating cancer.