Delving into the Latest Updates on RX-111 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

L-sel

Mechanism

L-sel inhibitors(Leukocyte adhesion molecule-1 inhibitors)

Therapeutic Areas

Digestive System DisordersOther Diseases

Active Indication-

Inactive Indication

InflammationInflammatory Bowel Diseases

Originator Organization

Rimonyx Pharmaceuticals Ltd.

Active Organization-

Inactive Organization

BioLineRx Ltd.

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

OBJECTIVE AND DESIGNElucidate the mechanism of action of the small molecule inhibitor of protein binding to glycosaminoglycans, RX-111 and assay its anti-inflammatory activity in animal models of inflammatory disease.MATERIALSThe glycosaminoglycan, heparin, was used in the mechanism of action study of RX-111. Human T lymphocytes and umbilical vein endothelial cells were used to assay the in vitro activity of RX-111. Mouse and rat models of disease were used to assay the anti-inflammatory activity of RX-111 in vivo.METHODSCircular dichroism and UV/Vis absorption spectroscopy were used to study the binding of RX-111 to the glycosaminoglycan, heparin. T lymphocyte rolling on endothelial cells under shear flow was used to assay RX-111 activity in vitro. Delayed-type hypersensitivity (DTH) and tri-nitrobenzene sulfonic acid (TNBS)-induced colitis in mice and experimental autoimmune encephalomyelitis (EAE) in rats were used to assay anti-inflammatory activity of RX-111 in vivo.RESULTSRX-111 was shown to bind directly to heparin. It inhibited leukocyte rolling on endothelial cells under shear flow and reduced inflammation in the mouse model of DTH. RX-111 was efficacious in the mouse model of inflammatory bowel disease, TNBS-induced colitis and the rat model of multiple sclerosis, EAE.CONCLUSIONSRX-111 exercises its broad spectrum anti-inflammatory activity by a singular mechanism of action, inhibition of protein binding to the cell surface GAG, heparan sulfate. RX-111 and related thieno[2,3-c]pyridine derivatives are potential therapeutics for the treatment of inflammatory and autoimmune diseases.

100 Deals associated with RX-111

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