Drug intelligence / Profile preview

FR117016

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
01

Overview

FR117016 is an experimental small molecule drug belonging to the benzimidazole class. It acts as a highly potent non-nucleoside inhibitor of adenosine deaminase (ADA), with a reported inhibition constant (Ki) of 7.7 nM. The compound was discovered through structure-based drug design and intentional lead hybridization strategies. Its mechanism involves binding to ADA and stabilizing it in an open conformation that inhibits its enzymatic activity. The primary developer is Fujisawa Pharmaceutical Co., Ltd., Japan[8][10][5]. There are no approved indications or clinical trials beyond preclinical research.

Other names
2-(4-{5-[(1H-1,3-benzodiazol-2-ylamino)methyl]thiophen-2-yl}-1,3-thiazol-2-yl)guanidineN''-(4-(5-((1H-BENZIMIDAZOL-2-YLAMINO)METHYL)-2-THIENYL)-1,3-thiazol-2-YL)GUANIDINE1ndv
02

Targets

ADA (Adenosine deaminase)

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