Drug intelligence / Profile preview

murepavadin + anti-pseudomonal antibiotic

Development stage
Unknown
Lead developer
Polyphor
Modality
Peptides, Small Molecules
Administration
Intravenous, Inhalation
01

Overview

Murepavadin + anti-pseudomonal antibiotic is a combination approach involving murepavadin, a synthetic cyclic beta-hairpin peptidomimetic antibiotic targeting Pseudomonas aeruginosa, and another antibiotic with recognized anti-pseudomonal activity (such as piperacillin-tazobactam, ceftazidime, cefepime, meropenem, imipenem, or colistin—specific anti-pseudomonal agent not specified in the query). Murepavadin acts by binding to the bacterial outer membrane protein LptD, thereby inhibiting lipopolysaccharide transport and causing outer membrane disruption, which results in bactericidal activity that is highly selective for Pseudomonas aeruginosa and shows potent in vitro and in vivo efficacy, even against multidrug-resistant isolates. Additionally, murepavadin modulates immune responses by activating human mast cells via the MRGPRX2 receptor, potentially contributing to both direct antibacterial action and immune-mediated clearance. Anti-pseudomonal antibiotics work via various mechanisms (e.g., inhibition of cell wall synthesis, interference with protein synthesis, or disruption of cell membrane integrity) depending on the specific agent included in the combination, with the shared property of being active against Pseudomonas aeruginosa[1][2][3][5].

02

Targets

MRGPRX2 (Mas-related G-protein Coupled Receptor X2)LptD

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