Tucidinostat

Tucidinostat
Clinical data
Trade names	Epidaza, Hiyasta
Other names	Chidamide, HBI-8000
Identifiers
	IUPAC name N-(2-Amino-4-fluorophenyl)-4-[[[(E)-3-pyridin-3-ylprop-2-enoyl]amino]methyl]benzamide;
CAS Number	1616493-44-7 ;
PubChem CID	12136798;
DrugBank	06334;
ChemSpider	7976319;
UNII	87CIC980Y0;
KEGG	D10993;
ChEMBL	ChEMBL3621988;
Chemical and physical data
Formula	C22H19FN4O2
Molar mass	390.418 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=CC(=CN=C1)/C=C/C(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N;
	InChI InChI=1S/C22H19FN4O2/c23-18-8-9-20(19(24)12-18)27-22(29)17-6-3-16(4-7-17)14-26-21(28)10-5-15-2-1-11-25-13-15/h1-13H,14,24H2,(H,26,28)(H,27,29)/b10-5+; Key:SZMJVTADHFNAIS-BJMVGYQFSA-N;

Tucidinostat (INN, also known as chidamide and sold under the brand names Epidaza and Hiyasta) is a histone deacetylase inhibitor (HDI) developed in China.[1] It was also known as HBI-8000.[2] It is a benzamide HDI and inhibits Class I HDAC1, HDAC2, HDAC3, as well as Class IIb HDAC10.[3]

Tucidinostat is approved by the Chinese FDA for relapsed or refractory peripheral T-cell lymphoma (PTCL) and has orphan drug status in Japan.[2] In Japan, it was approved for relapsed or refractory adult T-cell leukemia-lymphoma (ATLL) treatment in June 2021.[4]

Tucidinostat is being researched as a treatment for pancreatic cancer.[5][6][7] However, it is not US FDA approved for the treatment of pancreatic cancer.

References

Lowe D (April 2015). "China's First Homegrown Pharma". Seeking Alpha.
"Chipscreen Biosciences Announces CFDA Approval of Chidamide (Epidaza) for PTCLs in China". PR Newswire Association LLC.
"HUYA Bioscience International Grants An Exclusive License For HBI-8000 In Japan And Other Asian Countries To Eisai". PR Newswire Association LLC. February 2016.
"Marketing Approval of HBI-8000 (Tucidinostat) for Relapsed or Refractory ATLL Treatment in Japan" (PDF).
Qiao Z, Ren S, Li W, Wang X, He M, Guo Y, et al. (April 2013). "Chidamide, a novel histone deacetylase inhibitor, synergistically enhances gemcitabine cytotoxicity in pancreatic cancer cells". Biochemical and Biophysical Research Communications. 434 (1): 95–101. doi:10.1016/j.bbrc.2013.03.059. PMID 23541946.
Guha M (April 2015). "HDAC inhibitors still need a home run, despite recent approval". Nature Reviews. Drug Discovery. 14 (4): 225–6. doi:10.1038/nrd4583. PMID 25829268. S2CID 36758974.
Wang SS (2015-04-02). "A New Cancer Drug, Made in China". The Wall Street Journal. Retrieved 13 April 2015.

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[SA2015-1] Lowe D (April 2015). "China's First Homegrown Pharma". Seeking Alpha.

[FBT2016-2] "Chipscreen Biosciences Announces CFDA Approval of Chidamide (Epidaza) for PTCLs in China". PR Newswire Association LLC.

[3] "HUYA Bioscience International Grants An Exclusive License For HBI-8000 In Japan And Other Asian Countries To Eisai". PR Newswire Association LLC. February 2016.

[4] "Marketing Approval of HBI-8000 (Tucidinostat) for Relapsed or Refractory ATLL Treatment in Japan" (PDF).

[Qiao2013-5] Qiao Z, Ren S, Li W, Wang X, He M, Guo Y, et al. (April 2013). "Chidamide, a novel histone deacetylase inhibitor, synergistically enhances gemcitabine cytotoxicity in pancreatic cancer cells". Biochemical and Biophysical Research Communications. 434 (1): 95–101. doi:10.1016/j.bbrc.2013.03.059. PMID 23541946.

[Guha2015-6] Guha M (April 2015). "HDAC inhibitors still need a home run, despite recent approval". Nature Reviews. Drug Discovery. 14 (4): 225–6. doi:10.1038/nrd4583. PMID 25829268. S2CID 36758974.

[7] Wang SS (2015-04-02). "A New Cancer Drug, Made in China". The Wall Street Journal. Retrieved 13 April 2015.