Drug intelligence / Profile preview

FK-614

Development stage
Phase 2
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

FK‑614 is an orally active, non-thiazolidinedione (non-TZD) small molecule that acts as a selective peroxisome proliferator–activated receptor gamma (PPARγ) agonist. It was originally developed for the treatment of type 2 diabetes mellitus and functions as an insulin sensitizer by improving peripheral glucose utilization and ameliorating insulin resistance in both peripheral tissues and liver. Unlike thiazolidinediones such as pioglitazone or rosiglitazone, FK‑614 is a benzimidazole derivative without a TZD structure. Preclinical studies demonstrated its ability to induce adipocyte differentiation via PPARγ activation, reduce expression of pro-inflammatory cytokines like TNF-alpha in adipose tissue, increase the number of small adipocytes, and enhance insulin sensitivity in muscle. Clinical trials reached up to phase II for diabetes; more recently it has been investigated under the code name ATx08‑001 for neuropathic pain indications[1][2][3][4][5][7][10].

Other names
3-(2,4-dichlorobenzyl)-2-methyl-N-(pentylsulfonyl)-3H-benzimidazole-5-carboxamide193012-35-0UNII-V5Q32BZX79UNII-V-5Q32BZX79UNII-V 5Q32BZX79V5Q32BZX79V-5Q32BZX79V 5Q32BZX791-(2,4-dichlorobenzyl)-2-methyl-N-(pentane-1-sulfonyl)-1H-benzimidazole-6-carboxamide
02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)

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