RESMINOSTAT

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H19N3O4S
Molecular Weight	349.405
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN(C)CC1=CC=C(C=C1)S(=O)(=O)N2C=CC(\C=C\C(=O)NO)=C2

InChI

InChIKey=FECGNJPYVFEKOD-VMPITWQZSA-N

InChI=1S/C16H19N3O4S/c1-18(2)11-13-3-6-15(7-4-13)24(22,23)19-10-9-14(12-19)5-8-16(20)17-21/h3-10,12,21H,11H2,1-2H3,(H,17,20)/b8-5+

HIDE SMILES / InChI

Molecular Formula	C16H19N3O4S
Molecular Weight	349.405
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26952006 | https://www.ncbi.nlm.nih.gov/pubmed/29299154 | https://clinicaltrials.gov/ct2/show/NCT01037478 | https://clinicaltrials.gov/ct2/show/NCT00943449 | https://clinicaltrials.gov/ct2/show/NCT01277406

Resminostat (4SC-201) is a hydroxamate HDAC inhibitor (a novel class I, IIb, and IV histone deacetylase inhibitor). Resminostat inhibits proliferation of a large variety of rodent and human cancer cell lines, likely via the Akt signalling pathway. Phase I and II clinical trials have evaluated the efficacy and safety of resminostat in the treatment of relapsed or refractory Hodgkin's Lymphoma, hepatocellular carcinoma, advanced colorectal carcinoma, and in patients with advanced stage mycosis fungoides or Sezary syndrome (an aggressive form of blood cancer). Results in patients with hepatocellular carcinoma showed that resminostat (combined with sorafenib) was safe, well-tolerated and displayed early signs of efficacy.

Approval Year

Targets

Primary Target	Pharmacology	Potency
Histone deacetylase 1 51 Target ID: Q13547 Gene ID: 3065.0 Gene Symbol: HDAC1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/20201941	Inhibitor 8297	42.5 nM [IC50]
Histone deacetylase 3 35 Target ID: O15379 Gene ID: 8841.0 Gene Symbol: HDAC3 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/20201941	Inhibitor 8297	50.1 nM [IC50]
Histone deacetylase 6 27 Target ID: Q9UBN7 Gene ID: 10013.0 Gene Symbol: HDAC6 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/20201941	Inhibitor 8297	71.8 nM [IC50]
Histone deacetylase 23 Target ID: CHEMBL2093865 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20201941	Inhibitor 8297

PubMed

Title	Date	PubMed
First-in-human, pharmacokinetic and pharmacodynamic phase I study of Resminostat, an oral histone deacetylase inhibitor, in patients with advanced solid tumors.	2013 Oct 1	24065624

Substance Class	Chemical Created by `admin` on `Fri Dec 15 16:42:18 GMT 2023` Edited by `admin` on `Fri Dec 15 16:42:18 GMT 2023`
Record UNII	1578EUB98L
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

RESMINOSTAT

Official Name

English

Resminostat [WHO-DD]

Common Name

English

RAS2410

Code

English

BYK-408740

Code

English

(2E)-3-(1-((4-((DIMETHYLAMINO)METHYL)PHENYL)SULFONYL)-1H-PYRROL-3-YL)-N-HYDROXYPROP-2-ENAMIDE

Systematic Name

English

RAS-2410

Code

English

4SC-201

Code

English

BYK408740

Code

English

resminostat [INN]

Common Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

345511