Delving into the Latest Updates on BM-221 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

C5AR1

Action

stimulants

Mechanism

C5AR1 stimulants(C5a anaphylatoxin chemotactic receptor stimulants)

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal Diseases

Active Indication

Solid tumorBreast Cancer

Inactive Indication-

Originator Organization

Suzhou Baimai Biopharmaceutical Co. Ltd.

Active Organization

The University of Queensland

Suzhou Baimai Biopharmaceutical Co. Ltd.

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

The anaphylatoxin C5a is a complement peptide associated with immune-related disorders. C5a binds with equal potency to two GPCRs, C5aR1 and C5aR2. Multiple C5a peptide agonists have been developed to interrogate the C5a receptor function but none show selectivity for C5aR1. To address these limitations, we developed potent and stable peptide C5aR1 agonists that display no C5aR2 activity and over 1000-fold selectivity for C5aR1 over C3aR. This includes BM213, which induces C5aR1-mediated calcium mobilization and pERK1/2 signaling but not β-arrestin recruitment, and BM221, which exhibits no signaling bias. Both ligands are functionally similar to C5a in human macrophage cytokine release assays and in a murine in vivo neutrophil mobilization assay. BM213 showed antitumor activity in a mouse model of mammary carcinoma. We anticipate that these C5aR1-selective agonists will be useful research tools to investigate C5aR1 function.

100 Deals associated with BM-221

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Solid tumor	Preclinical	China	Suzhou Baimai Biopharmaceutical Co. Ltd.	02 Aug 2022
Breast Cancer	Preclinical	Australia	The University of Queensland	11 Nov 2021