Drug intelligence / Profile preview

cefazolin

Development stage
Approved
Lead developer
GSK
Modality
Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

Cefazolin is a first-generation cephalosporin antibiotic used to treat a wide range of bacterial infections. It is commonly administered by intravenous or intramuscular injection and is effective against many Gram-positive bacteria and some Gram-negative bacteria. Its primary indications include treatment of skin and soft tissue infections (such as cellulitis), urinary tract infections (UTIs), pneumonia, infective endocarditis caused by susceptible organisms like Staphylococcus aureus and Streptococcus species; bone and joint infections; biliary tract infections; genital infections; septicemia; and perioperative prophylaxis to prevent surgical site infection. Mechanistically it acts by binding to penicillin-binding proteins (PBPs) in the bacterial cell wall—specifically inhibiting the final transpeptidation step in peptidoglycan synthesis—leading to cell lysis via autolytic enzymes. This bactericidal action makes it effective for both treatment and prevention of serious bacterial diseases[1][2][3][4][5]. Cefazolin was originally developed by GlaxoSmithKline under the brand name Nostof[2]. It is now widely manufactured as a generic drug.

Brand names
AncefKefzolCefacidalCefamezinCefrinaElzogramFaxilenGramaxinKefolKefzolanKezolinNovaporinNostofReflinZinolZolicef
Other names
头孢唑啉 (Chinese)头孢唑林 (Chinese)cephazolin
02

Targets

PBP (Penicillin-binding protein family)

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