Ertapenem is a new carbapenem developed to address the pharmacokinetic shortcomings (short half-life) of imipenem and meropenem. Ertapenem shares similar structural features with meropenem, including its stability to dehydropeptidase-1, allowing it to be administered without a dehydropeptidase-1 inhibitor. Ertapenem, like imipenem and meropenem, demonstrates broad-spectrum antimicrobial activity against many Gram-positive and -negative aerobes and anaerobes and is resistant to nearly all β-lactamases, including extended-spectrum β-lactamases and AmpCs. The extensive protein binding of ertapenem extends the half-life and allows for once-daily dosing. Ertapenem binds to penicillin binding proteins (PBPs) located on the bacterial cell wall, in particular PBPs 2 and 3, thereby inhibiting the final transpeptidation step in the synthesis of peptidoglycan, an essential component of the bacterial cell wall. Inhibition of peptidoglycan synthesis results in weakening and lysis of the cell wall and cell death.
Ertapenem is a parenteral carbapenem which is currently approved in the United States for use in the treatment of intraabdominal infections, complicated skin and soft-tissue infections, community-acquired pneumonia, and complicated urinary tract infections. Ertapenem is unique for its long elimination half-life, which allows for once-daily dosing. Because of its broad spectrum of activity, it is often used for the treatment of infections requiring prolonged parenteral therapy.
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