Drug intelligence / Profile preview

cefotaxime + imipenem + cilastatin + piperacillin + tazobactam

Development stage
Discontinued
Lead developer
Sanofi
Modality
Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

This is a combination of five antibiotics and antibiotic adjuncts, each with distinct mechanisms of action.

  • Cefotaxime is a third-generation cephalosporin that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), leading to cell lysis and death.
  • Imipenem is a carbapenem antibiotic that also inhibits bacterial cell wall synthesis via PBPs; it has broad-spectrum activity against Gram-positive and Gram-negative bacteria.
  • Cilastatin is not an antibiotic but an inhibitor of renal dehydropeptidase I, used in combination with imipenem to prevent its degradation in the kidneys, thereby increasing imipenem's efficacy.
  • Piperacillin is an extended-spectrum ureidopenicillin that targets PBPs for bactericidal activity, especially against Pseudomonas aeruginosa and other Gram-negative organisms.
  • Tazobactam is a β-lactamase inhibitor combined with piperacillin to protect it from enzymatic breakdown by β-lactamases produced by resistant bacteria.

This combination would theoretically provide extremely broad antibacterial coverage—including many multidrug-resistant organisms—by combining multiple classes of β-lactams (cephalosporin, carbapenem, penicillin) plus two β-lactamase inhibitors (cilastatin as adjunct for imipenem; tazobactam for piperacillin). However, there are no known approved or marketed products containing all five agents together; such combinations are typically used separately or in pairs (e.g., imipenem-cilastatin or piperacillin-tazobactam).

02

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