Chidamide (Tucidinostat, HBI8000, CS 055)

Description: Chidamide (CS-055, Tucidinostat, HBI-8000; trade name: Epidaza), is a potent and orally bioavailable benzamide-type histone deacetylase (HDAC) inhibitor with IC50s of 95, 160, 67 and 78 nM for HDAC1, HDAC2, HDAC3 and HDAC10, respectively. Chidamide is approved by the Chinese FDA for relapsed or refractory peripheral T-cell lymphoma (PTCL), and has orphan drug status in Japan. As of April 2015 it is only approved in China. Chidamide selectively binds to and inhibits HDAC leading to an increase of acetylation levels of histone protein H3. It also inhibits the expression of signaling kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis, which may inhibit tumor cell proliferation in susceptible tumor cells. Chidamide is being investigated as a treatment for pancreatic cancer. However, it is not US FDA approved for the treatment of pancreatic cancer.

References: Cancer Chemother Pharmacol. 2012 Apr; 69(4):901-9; Oncol Rep. 2015 Jan; 33(1):304-10.

Related CAS#: 743420-02-2 (chidamide impurity); 1616493-44-7 (or 743438-44-0) (Chidamide, Tucidinostat, HBI-8000; CS 055)