Drug intelligence / Profile preview

cefotaxime + imipenem + cilastatin + piperacillin + tazobactam

Development stage
Unknown
Lead developer
Hoechst
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[4][5][7]. 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)[2][3][4].

02

Targets

β-lactamaseDPEP1 (Dehydropeptidase 1)PBP (Penicillin-binding protein family)

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