Drug intelligence / Profile preview

bezafibrate + diflunisal

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

Overview

Bezafibrate + diflunisal is an investigational fixed-dose combination of two small molecule drugs: bezafibrate, a fibrate-class lipid-lowering agent, and diflunisal, a nonsteroidal anti-inflammatory drug (NSAID). The combination was developed under the code name CRx-401 as a novel insulin sensitizer for the treatment of type 2 diabetes. Bezafibrate acts primarily as an agonist of peroxisome proliferator-activated receptor alpha (PPAR-alpha), reducing cholesterol and triglyceride levels while increasing HDL cholesterol. Diflunisal inhibits prostaglandin synthesis by blocking cyclooxygenase enzymes (prostaglandin G/H synthase 1 and 2), providing analgesic and anti-inflammatory effects. In this combination, low-dose diflunisal is used to synergistically enhance the anti-diabetic effects of bezafibrate through disease-targeted mechanisms that improve glycemic control without promoting weight gain. The product was developed by Zalicus (formerly CombinatoRx) for type 2 diabetes but does not appear to have reached regulatory approval[3][4][5].

Other names
bezafibrate + diflunisalCRx 401CRx401CRx-401
02

Targets

PPARD (Peroxisome proliferator–activated receptor delta)PPARG (Peroxisome proliferator-activated receptor gamma)PGHS-1 (Prostaglandin G/H Synthase 1)HMGB1 (High mobility group protein B1)PPARA (Peroxisome proliferator-activated receptor alpha)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)CXCL12 (C-X-C motif chemokine ligand 12)

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