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

Description

CH5183284/Debio 1347 is selective and orally available fibroblast growth factor receptors: FGFR1, FGFR2, and FGFR3 inhibitor that has a unique chemical scaffold. By interacting with unique residues in the ATP-binding site of FGFR1, FGFR2, or FGFR3, CH5183284/Debio 1347 selectively inhibits there receptors, but does not inhibit kinase insert domain receptor (KDR) or other kinases. CH5183284/Debio 1347 will provide therapeutic opportunities for patients who have FGFR genetic alterations and patients with acquired resistance to existing FGFR selective inhibitors that contain the common methoxy moieties.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
PubMed

PubMed

TitleDatePubMed
The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor.
2014 Nov
ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor.
2015 Dec
Patents

Sample Use Guides

In Vivo Use Guide
Adaptive doses of Debio1347 (CH5183284): (10 mg to 210 mg/day) until the recommended dose is determined.
Route of Administration: Oral
In Vitro Use Guide
MAPK pathway suppression by CH5183284/Debio 1347 in FGFR-altered cancer cell lines was investigated. Cells were treated with 1 μmol/L CH5183284/Debio 1347. It was confirmed that the ERK (GSE15417) and MEK signatures were suppressed by CH5183284/Debio 1347 only in sensitive cell lines harboring FGFR alterations. Consistent with this, suppression of phospho-ERK by a 2-hour treatment with CH5183284/Debio 1347 was observed in seven cancer cell lines harboring FGFR alterations.
Substance Class
Concept
Record UNII
2SMH8D25J8
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DEBIO-1347 (S)-HYDROXYSUCCINATE
Code English
BUTANEDIOIC ACID, 2-HYDROXY-, (2S)-, COMPD. WITH (5-AMINO-1-(2-METHYL-1H-BENZIMIDAZOL-6-YL)-1H-PYRAZOL-4-YL)-1H-INDOL-2-YLMETHANONE (1:1)
Systematic Name English
Classification Tree Code System Code
EU-Orphan Drug EU/3/17/1916
Created by admin on Mon Oct 21 20:53:31 UTC 2019 , Edited by admin on Mon Oct 21 20:53:31 UTC 2019
Code System Code Type Description
EVMPD
SUB192816
Created by admin on Mon Oct 21 20:53:31 UTC 2019 , Edited by admin on Mon Oct 21 20:53:31 UTC 2019
PRIMARY
CAS
1265231-80-8
Created by admin on Mon Oct 21 20:53:31 UTC 2019 , Edited by admin on Mon Oct 21 20:53:31 UTC 2019
PRIMARY
This is a non-substance concept
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY
This is a non-substance concept