Delving into the Latest Updates on NR11/1943 (Norgine) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

NR11/1943, chemokine receptor 9 antagonist (Norgine)

Target

CCR9

Action

antagonists

Mechanism

CCR9 antagonists(C-C chemokine receptor type 9 antagonists)

Therapeutic Areas

Immune System DiseasesDigestive System Disorders

Active Indication

Inflammatory Bowel Diseases

Inactive Indication-

Originator Organization

Norgine Ltd.

Active Organization

Norgine Ltd.

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Chemokine receptor 9 (CCR9), a cell surface chemokine receptor which belongs to the G protein-coupled receptor, 7-trans-membrane superfamily, is expressed on lymphocytes in the circulation and is the key chemokine receptor that enables these cells to target the intestine. It has been proposed that CCR9 antagonism represents a means to prevent the aberrant immune response of inflammatory bowel disease in a localized and disease specific manner and one which is accessible to small molecule approaches. One possible reason why clinical studies with vercirnon, a prototype CCR9 antagonist, were not successful may be due to a relatively poor pharmacokinetic (PK) profile for the molecule. We wish to describe work aimed at producing new, orally active CCR9 antagonists based on the 1,3-dioxoisoindoline skeleton. This study led to a number of compounds that were potent in the nanomolar range and which, on optimization, resulted in several possible preclinical development candidates with excellent PK properties.

100 Deals associated with NR11/1943 (Norgine)

Login to view more data