TEFINOSTAT

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C28H37N3O5
Molecular Weight	495.6105
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=GLNWREBYRLDPQP-MHZLTWQESA-N

InChI=1S/C28H37N3O5/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/h3-5,10-11,16-19,24,27,29,35H,1-2,6-9,12-15,20H2,(H,30,32)(H,31,33)/t27-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C28H37N3O5
Molecular Weight	495.6105
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://clinicaltrials.gov/ct2/show/NCT00820508 | https://clinicaltrials.gov/ct2/show/NCT02759601 | https://www.ncbi.nlm.nih.gov/pubmed/26934551 | https://www.walescancerresearchcentre.org/partner-news/first-patient-recruited-for-chronic-myelomonocytic-leukaemia-trial/

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.

Originator

Approval Year

PubMed

Title	Date	PubMed
The targeted histone deacetylase inhibitor tefinostat (CHR-2845) shows selective in vitro efficacy in monocytoid-lineage leukaemias.	2016-03-29	26934551

Sample Use Guides

In Vivo Use Guide

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

Substance Class	Chemical Created by `admin` on `Mon Mar 31 20:13:09 GMT 2025` Edited by `admin` on `Mon Mar 31 20:13:09 GMT 2025`
Record UNII	ZAU91150SB
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TEFINOSTAT

Official Name

English

BENZENEACETIC ACID, .ALPHA.-(((4-((8-(HYDROXYAMINO)-1,8-DIOXOOCTYL)AMINO)PHENYL)METHYL)AMINO)-, CYCLOPENTYL ESTER, (.ALPHA.S)-

Preferred Name

English

tefinostat [INN]

Common Name

English

CHR2845

Code

English

Tefinostat [WHO-DD]

Common Name

English

CHR-2845

Code

English

CYCLOPENTYL (2S)-2-(((4-(8-(HYDROXYAMINO)-8-OXOOCTANAMIDO)PHENYL)METHYL)AMINO)-2-PHENYLACETATE

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1946