murepavadin

Murepavadin is a first-in-class, pathogen-specific peptidomimetic antibiotic developed for the treatment of serious infections caused by *Pseudomonas aeruginosa*. It is a synthetic cyclic beta hairpin peptidomimetic that functions through a novel mechanism of action by binding to the lipopolysaccharide transport protein D (LptD), an outer membrane protein involved in lipopolysaccharide biogenesis in Gram-negative bacteria. By inhibiting LptD, murepavadin disrupts lipopolysaccharide transport and assembly in the bacterial outer membrane, leading to cell death. Murepavadin exhibits potent bactericidal activity specifically against *Pseudomonas aeruginosa*, including multidrug-resistant and colistin-resistant strains, with little or no activity against other Gram-negative or Gram-positive bacteria. The drug has shown promising results in preclinical and early clinical studies for hospital-acquired bacterial pneumonia (HABP) and ventilator-associated bacterial pneumonia (VABP) due to *Pseudomonas aeruginosa*. Development was led by Polyphor but phase III trials were suspended for safety review[3][5][6]. Murepavadin is highly specific for *Pseudomonas aeruginosa* and does not exhibit significant cross-resistance with other antibiotics[3]. It also acts as a G protein-biased agonist at MRGPRX2 on mast cells, which may have implications for immune modulation[4][8]. Phase III development was suspended due to safety concerns[5].

Other names

Murepavadin TFA