Drug intelligence / Profile preview

itraconazole + piperacillin + tazobactam

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral (itraconazole), Intravenous (piperacillin + Tazobactam)
01

Overview

This is a combination regimen consisting of three drugs: - **Itraconazole** is a triazole antifungal agent that inhibits fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase, thereby impairing ergosterol synthesis and disrupting fungal cell membrane formation. It is used to treat various systemic and superficial fungal infections[9]. - **Piperacillin** is an extended-spectrum ureidopenicillin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), leading to bacterial lysis. It has broad-spectrum activity against Gram-positive and Gram-negative bacteria, including *Pseudomonas aeruginosa*[5]. - **Tazobactam** is a β-lactamase inhibitor that protects piperacillin from enzymatic degradation by β-lactamases produced by certain bacteria, thus extending the antibacterial spectrum of piperacillin[2][3][7]. The combination of piperacillin and tazobactam (often known as Zosyn or Tazocin) is widely used for severe bacterial infections such as intra-abdominal infections, pneumonia, skin/soft tissue infections, gynecological infections, and sepsis[1][2][6]. Itraconazole may be co-administered in cases where there are concurrent or suspected invasive fungal infections.

02

Targets

CYP51A1 (Sterol 14α-demethylase)PBP (Penicillin-binding protein family)Class A BL (Class A beta-lactamase)

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