In the last few years, HDAC inhibitors have become a new focus on target cancer therapy. At NBM, we developed a HDAC8-specific inhibitor which has the following features:
- The cost of the compound is quite low. The precursor of BMX- OS01 is extracted from a very inexpensive herb with a high extraction rate. It takes only 3 steps from precursor to the final compound and each step produces a high yield of the products.
- In in vitro testing, BMX-OS01 is more effective than SAHA (the FDA-approved HDAC inhibitor) against several brain tumor cell lines.
- BMX-OS01 is non-toxic towards normal cells (Human fibroblast Hs68).
- BMX-OS01 does not have mutagenicity (bacterial reverse mutation test) and does not cause chromosome aberration (Mammalian chromosome aberration test).
- In animal studies, BMX-OS01 was found non-toxic at high dose. At the maximal tolerated dose of 1500 mg/kg for 4 days, no toxic effect was found and biopsy did not find any organ abnormality.
- In a subacute toxicity study, BMX-OS01 was taken orally at 500 mg/kg for 28 days and no toxicity was found.
- BMX-OS01 passes the BBB in large quantities.
- In either xenografted or orthotopic models, BMX-OS01 was found to be much more potent than SAHA against brain tumors. In the orthotopic model, complete eradication of brain tumors was seen.
- Patents of BMX-OS01 have been granted in the following regions and others are pending: USA 8318801, Japan 5548893, EU 2236503, China ZL201010145262.9, Australia 2010201322, Korea 10-1208760, Taiwan I365181, Russia 2492163.