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PZ-601 is a carbapenem antibiotic currently being tested as having a broad spectrum of activity including strains resistant to other carbapenems. Despite early Phase II promise, Novartis (who acquired PZ-601 in a merger deal with Protez Pharmaceuticals) recently dropped PZ-601, citing a high rate of adverse events in testing.
Meropenem, sold under the brand name Merrem among others, is an intravenous carbapenem antibiotic used to treat a variety of bacterial infections. [3] Some of these include meningitis, intra-abdominal infection, pneumonia, sepsis, and anthrax.
One mechanism of resistance is mutation in or loss of outer membrane porins, preventing antibiotics from entering the cells. [21] Changes within the porin protein gene cause a frameshift, altering the porin structure and function. [21] Changes in the porin protein hinder the diffusion of carbapenem and other antibiotics into the periplasm. [22]
Like all carbapenem antibiotics, ertapenem has a broader spectrum of activity than other beta-lactams like penicillins and cephalosporins. Similar to doripenem , meropenem and biapenem , ertapenem has slightly better activity against many Gram-negative bacteria than other carbapenems such as imipenem .
Thienamycin was the first among the naturally occurring class of carbapenem antibiotics to be discovered and isolated. [3] Carbapenems are similar in structure to their antibiotic “cousins” the penicillins. Like penicillins, carbapenems contain a β-lactam ring (cyclic amide) fused to a five-membered ring. Carbapenems differ in structure ...
β-Lactam antibiotics are indicated for the prevention and treatment of bacterial infections caused by susceptible organisms. At first, β-lactam antibiotics were mainly active only against gram-positive bacteria, yet the recent development of broad-spectrum β-lactam antibiotics active against various gram-negative organisms has increased their usefulness.
Nacubactam is an investigational β-lactamase inhibitor being developed for the treatment of infections caused by carbapenem-resistant Enterobacteriaceae (CRE). It belongs to the diazabicyclooctane (DBO) class of compounds and exhibits a dual mechanism of action.
However, the bla NDM-1 gene produces NDM-1, which is a carbapenemase beta-lactamase - an enzyme that hydrolyzes and inactivates these carbapenem antibiotics. [citation needed] Carbapenemases are particularly dangerous resistance mechanisms, since they can inactivate a wide range of different antibiotics. [10]