Delving into the Latest Updates on IDOR-11172520 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CCR6

Mechanism

CCR6 antagonists(C-C motif chemokine receptor 6 antagonists)

Therapeutic Areas

Immune System Diseases

Active Indication

Immune System Diseases

Inactive Indication-

Originator Organization

Idorsia Ltd.

Active Organization

Idorsia Ltd.

Inactive Organization-

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

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Structure

Molecular FormulaC25H32N4O3

InChIKeyRLAQKDLLSLGHQO-VWLOTQADSA-N

CAS Registry2737274-49-4

Migration of immune cells to sites of inflammation is a critical step in the body's response to infections but also during autoimmune flares. Chemokine receptors, members of the GPCR receptors, are instrumental in directing specific cell types to their target organs. Herein, we describe a highly potent small molecule antagonist of the chemokine receptor CCR6, which came out of fine-tuned structural elaborations from a proprietary HTS hit. Three main issues in the parent chemical series-cytotoxicity, phototoxicity, and hERG, were successfully solved. Biological characterization demonstrated that compound 45 (IDOR-1117-2520) is a selective and insurmountable antagonist of CCR6. In vivo proof-of-mechanism studies in a mouse lung inflammation model using a representative compound from the chemical class of 45 confirmed that the targeted CCR6⁺ cells were efficiently inhibited from migrating into the bronchoalveoli. Finally, ADMET and physicochemical properties were well balanced and the preclinical package warranted progress in the clinic.

100 Deals associated with IDOR-11172520

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