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
Clinical data
Trade namesEpidaza, Hiyasta
Other namesChidamide, HBI-8000
ATC code
  • None
Identifiers
  • N-(2-Amino-4-fluorophenyl)-4-[[[(E)-3-pyridin-3-ylprop-2-enoyl]amino]methyl]benzamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC22H19FN4O2
Molar mass390.418 g·mol−1
3D model (JSmol)
  • C1=CC(=CN=C1)/C=C/C(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N
  • 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 is approved by the Chinese FDA for relapsed or refractory peripheral T-cell lymphoma (PTCL) and has orphan drug status in Japan.[2][better source needed] 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

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  1. ^ Lowe D (April 2015). "China's First Homegrown Pharma". Seeking Alpha.
  2. ^ a b "Chipscreen Biosciences Announces CFDA Approval of Chidamide (Epidaza) for PTCLs in China" (Press release). 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).
  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.
  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.