Abstract
Tebipenem (SPR859) is the microbiologically active form of SPR994 (tebipenem-pivoxil), an orally available carbapenem with activity against extended-spectrum β-lactamase (ESBL)-producing Enterobacteriaceae Measurement of the relative binding of SPR859 to the bacterial cell targets revealed that it is a potent inhibitor of multiple penicillin-binding proteins (PBPs) but primarily a Gram-negative PBP 2 inhibitor, similar to other compounds in this class. These data support further clinical development of SPR994.
Keywords:
PBP; carbapenems; penicillin-binding proteins; tebipenem.
Copyright © 2019 American Society for Microbiology.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Bacterial Agents / pharmacology
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Bacterial Proteins / antagonists & inhibitors*
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Bacterial Proteins / metabolism
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Carbapenems / pharmacology*
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Gram-Negative Bacteria / drug effects*
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Gram-Negative Bacteria / metabolism
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Gram-Positive Bacteria / drug effects*
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Gram-Positive Bacteria / metabolism
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Humans
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Microbial Sensitivity Tests / methods
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Penicillin-Binding Proteins / antagonists & inhibitors*
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Penicillin-Binding Proteins / metabolism
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beta-Lactamases / metabolism
Substances
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Anti-Bacterial Agents
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Bacterial Proteins
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Carbapenems
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Penicillin-Binding Proteins
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beta-Lactamases
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tebipenem