Pipeline

OBP-801

Outline

OBP-801 is a histone deacetylase (HDAC) inhibitor, having specific and strong activity on HDAC, which is expected to show anticancer effect by promoting an expression of tumor suppressor genes in cancer cell and inducing apoptotic and autophagic cell death.
The results of pre-clinical studies on OBP-801 indicated the most potent HDAC inhibitory activity as compared to other HDAC inhibitors including and Zolinza® and Istodax®, and its efficacy on a wide range of cancers is expected.
Furthermore, Oncolys has been exploring the potential ophthalmic use of OBP-801 in collaboration with Kyoto Prefectural University of Medicine.

OBP-801

Target indication

Lung cancer, lymphoma, kidney cancer, and glaucoma

Current status

We concluded a worldwide exclusive license agreement with Astellas Pharma Inc. on October 2009 to develop, manufacture and commercialize OBP-801.
After completion of preclinical and CMC works, we filed an IND to the US FDA in 2014 and have been conducting phase 1 clinical study for solid tumor.
For the ophthalmic use, we initiated to explore the possibility of using OBP-801 as an alternate drug of mitomycin C in glaucoma operation in collaboration with Kyoto Prefectural University of Medicine.

References

FGFR inhibitor BGJ398 and HDAC inhibitor OBP-801 synergistically inhibit cell growth and induce apoptosis in bladder cancer cells.

Outline:The combination treatment of HDAC inhibitor, OBP-801 with FGFR inhibitor, BGJ398 showed the synergistic inhibition of the growth in bladder cancer cells.

Published online on: December 1,2017
https://doi.org/10.3892/or.2017.6127 Pages: 627-632

https://www.ncbi.nlm.nih.gov/pubmed/29207153

The histone deacetylase inhibitor OBP-801 and eribulin synergistically inhibit the growth of triple-negative breast cancer cells with the suppression of survivin, Bcl-xL, and the MAPK pathway.

Outline:The combination treatment of HDAC inhibitor, OBP-801 with eribulin showed the synergistic inhibition of the growth in TNBC cells.

Breast Cancer Research and Treatment, ISSN: 0167-6806 (Print) 1573-7217 (Online)
https://www.ncbi.nlm.nih.gov/pubmed/29752686

The novel HDAC inhibitor OBP-801/YM753 enhances the effects of 5-fluorouracil with radiation on esophageal squamous carcinoma cells.

Furutani A, Sowa Y, Fujiwara H, Otsuji E, Sakai T.
Oncol Res. 2014;21(5): 281-286. doi:, 2014

A novel HDAC inhibitor OBP-801 and a PI3K inhibitor LY294002 synergistically induce apoptosis via the suppression of survivin and XIAP in renal cell carcinoma.

Yamada T, Horinaka M, Shinnoh M, Yoshioka T, Miki T, Sakai T.
013 Oct;43(4): 1080-1086. doi: 1, 2013

Combination of a novel HDAC inhibitor OBP-801/YM753 and a PI3K inhibitor LY294002 synergistically induces apoptosis in human endometrial carcinoma cells due to increase of Bim with accumulation of ROS.

Yoshioka T, Yogosawa S, Yamada T, Kitawaki J, Sakai T.
2013 May;129(2): 425-32. doi:, 2013

YM753, a novel histone deacetylase inhibitor, exhibits antitumor activity with selective, sustained accumulation of acetylated histones in tumors in the WiDr xenograft model.

Shindoh N, Mori M, Terada Y, Oda K, Amino N, Kita A, Taniguchi M, Sohda KY, Nagai K, Sowa Y, Masuoka Y, Orita M, Sasamata M, Matsushime H, Furuichi K, Sakai T.
2008 Mar;32(3): 545-55, 2008

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