ACUMAPIMOD

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H19N5O2
Molecular Weight	385.4186
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=CC=C(C=C1N2N=CC(C(=O)C3=CC=CC(=C3)C#N)=C2N)C(=O)NC4CC4

InChI

InChIKey=VGUSQKZDZHAAEE-UHFFFAOYSA-N

InChI=1S/C22H19N5O2/c1-13-5-6-16(22(29)26-17-7-8-17)10-19(13)27-21(24)18(12-25-27)20(28)15-4-2-3-14(9-15)11-23/h2-6,9-10,12,17H,7-8,24H2,1H3,(H,26,29)

HIDE SMILES / InChI

Description
Sources: https://adisinsight.springer.com/drugs/800034065 | https://www.ncbi.nlm.nih.gov/pubmed/25599809 | https://www.ncbi.nlm.nih.gov/pubmed/29354676

Acumapimod (BCT-197) is an oral p38 MAP kinase inhibitor and an anti-inflammatory agent developed by Mereo BioPharma that has completed Phase 2 development as first-line therapy for severe acute exacerbations of chronic obstructive pulmonary disease. Another study on acute kidney injury in patients undergoing cardiac surgery had been discontinued. Acumapimod is an inhibitor of p38a with an IC50 value < 1 uM. Previous studies undertaken by Novartis, showed the drug has the capacity to reduce the inflammatory marker TNFα and to increase FEV1.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
LPS‐induced TNFα secretion 1 Target ID: LPS‐induced TNFα secretion Sources: https://www.ncbi.nlm.nih.gov/pubmed/26904383	Inhibitor 8504		115.0 nM [IC50]
MAP kinase p38 alpha 34 Target ID: CHEMBL260 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26904383	Inhibitor 8504		12.0 nM [IC50]

PubMed

Title	Date	PubMed
The COPD Pipeline XXXVI.	2017-10-06	29354676
Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease.	2015-03	25599809

Patents

Sample Use Guides

In Vivo Use Guide

The effects of single doses of 20 and 75 mg acumapimod ± prednisone, were investigated in COPD patients

Route of Administration: Oral

In Vitro Use Guide

Acumapimod is an inhibitor of p38a with an IC50 value < 1 uM.

Name

Type

Language

ACUMAPIMOD

Official Name

English

acumapimod [INN]

Preferred Name

English

BENZAMIDE, 3-(5-AMINO-4-(3-CYANOBENZOYL)-1H-PYRAZOL-1-YL)-N-CYCLOPROPYL-4-METHYL-

Systematic Name

English

Acumapimod [WHO-DD]

Common Name

English

3-(5-AMINO-4-(3-CYANOBENZOYL)PYRAZOL-1-YL)-N-CYCLOPROPYL-4-METHYLBENZAMIDE

Systematic Name

English

Code System Code Type Description

PUBCHEM

11338127