U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C28H37N3O5.C4H6O6
Molecular Weight 645.6973
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Tefinostat tartrate

SMILES

O[C@H]([C@@H](O)C(O)=O)C(O)=O.ONC(=O)CCCCCCC(=O)NC1=CC=C(CN[C@H](C(=O)OC2CCCC2)C3=CC=CC=C3)C=C1

InChI

InChIKey=HRYGRYINGGVIDB-USLHTNTQSA-N
InChI=1S/C28H37N3O5.C4H6O6/c32-25(14-6-1-2-7-15-26(33)31-35)30-23-18-16-21(17-19-23)20-29-27(22-10-4-3-5-11-22)28(34)36-24-12-8-9-13-24;5-1(3(7)8)2(6)4(9)10/h3-5,10-11,16-19,24,27,29,35H,1-2,6-9,12-15,20H2,(H,30,32)(H,31,33);1-2,5-6H,(H,7,8)(H,9,10)/t27-;1-,2-/m01/s1

HIDE SMILES / InChI
Tefinostat (also known as CHR-2845) was developed as an innovative oral HDAC (histone deacetylase) inhibitor that selectively targets macrophages and monocytes – central cells of the innate immune system. Chroma Therapeutics develops tefinostat for the treatment of hematological and lymphoid malignancies. In addition, the drug is under investigation in clinical trial phase I/II for cancer-associated inflammation in hepatocellular carcinoma. The aim of this study is to find the best dose of the drug without causing side effects. Besides, Phase II of clinical trial ‘MONOCLE’ study for the treatment of chronic myelomonocytic leukemia (CMML) has been initiated and the first patient has been recruited.

Approval Year

PubMed

PubMed

TitleDatePubMed
The targeted histone deacetylase inhibitor tefinostat (CHR-2845) shows selective in vitro efficacy in monocytoid-lineage leukaemias.
2016-03-29

Sample Use Guides

Up to 5 cohorts of 3-6 patients (number is dependent on DLT occurrence) will be treated for 28 days once or twice daily (360, 480mg once daily, then 240, 360, 480mg twice daily) to determine safety and tolerability of Tefinostat and to identify the recommended dose for Phase II.
Route of Administration: Oral
Name Type Language
Tefinostat tartrate
Preferred Name English
Code System Code Type Description
FDA UNII
4Z5LF92QAJ
Created by admin on Wed Apr 02 19:40:33 GMT 2025 , Edited by admin on Wed Apr 02 19:40:33 GMT 2025
PRIMARY