Enmetazobactam

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A beta-lactamase inhibitor used in combination with antibiotics


Chemical structure of Enmetazobactam

Enmetazobactam is a novel beta-lactamase inhibitor that is used in combination with beta-lactam antibiotics to enhance their efficacy against resistant bacterial strains. It is particularly effective against bacteria that produce extended-spectrum beta-lactamases (ESBLs), which are enzymes that confer resistance to many beta-lactam antibiotics.

Mechanism of Action

Enmetazobactam works by inhibiting the activity of beta-lactamase enzymes. These enzymes are produced by certain bacteria and can break down beta-lactam antibiotics, rendering them ineffective. By inhibiting these enzymes, enmetazobactam protects the antibiotic from degradation, allowing it to exert its antibacterial effect.

Clinical Use

Enmetazobactam is primarily used in combination with cefepime, a fourth-generation cephalosporin antibiotic. This combination is effective against a wide range of Gram-negative bacteria, including those that produce ESBLs. The combination is used to treat complicated urinary tract infections (cUTIs) and other serious infections caused by resistant bacteria.

Pharmacokinetics

Enmetazobactam is administered intravenously and has a pharmacokinetic profile that complements that of cefepime. It is rapidly distributed in the body and is primarily excreted unchanged in the urine. This pharmacokinetic property makes it particularly suitable for treating urinary tract infections.

Development and Approval

Enmetazobactam was developed to address the growing problem of antibiotic resistance, particularly resistance mediated by beta-lactamase enzymes. It has undergone clinical trials to assess its safety and efficacy in combination with cefepime. The combination has shown promising results in treating infections caused by resistant bacteria.

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Contributors: Prab R. Tumpati, MD