Research & Development

Background information on β-lactams

β-Lactam antibiotics are a broad class of antibiotics that includes penicillins, cephalosporins , monobactams, and carbapenems. Because of their efficacy and safety, β-lactams are the most commonly used antibiotics in the world. Almost 60% of all antibiotics prescribed in U.S. hospitals are β-lactams1.

β-Lactams work by binding to bacterial proteins called Penicillin Binding Proteins (PBPs). PBPs are a family of essential bacterial enzymes involved in the synthesis of peptidoglycan, the major component of the bacterial cell wall. When β-lactam antibiotics bind to PBPs, they disrupt the integrity of the cell wall, leading to bacterial lysis and death.

Unfortunately, many bacteria produce resistance enzymes, β-lactamases, which inactivate the β-lactam antibiotic, thereby preventing the antibiotic from reaching and binding to the PBPs. In so doing, the bacteria protects itself against the antibiotic. The recent spread of these β-lactamase enzymes amongst gram negative bacteria (in particular, the Enterobacteriaceae family, the principal causative pathogens for urinary tract infections and intra-abdominal infections, among others) is significantly compromising the clinical utility of β-lactam antibiotics.

VenatoRx approaches to innovation in the β-lactam space

VenatoRx focuses on specific approaches to address the issue of β-lactam resistance. Such approaches include:

  • β-Lactamase inhibitors: rescue of β-lactams from inactivation by bacterial β-lactamases
  • Next generation β-lactams: β-lactams with unique bacterial coverage, enhanced affinity for target-mutated Gram positives (e.g., MRSA) and broad Gram negative coverage, including Pseudomonas
  • Next generation PBP inhibitors: novel (non-β-lactam) antibiotics acting on the penicillin binding proteins (PBPs) to disrupt cell wall synthesis