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Description

Alafosfalin is a phosphonodipeptide with significant activity as an antibacterial agent and as a potentiator of beta-lactam antibiotics. Alafosfalin shows good activity both in vitro and in vivo, particularly against Enterobacteriaceae. The compound acts by interfering with bacterial cell wall biosynthesis and also potentiates the activity of beta-lactam antibiotics. Alafosfalin was found to be highly active against Escherichia coli and moderately active against Serratia, Klebsiella, Enterobacter, and Citrobacter, but less active against gram-positive organisms than were beta-lactams such as cephazolin or ampicillin and inactive against indole-positive Proteus, Pseudomonas, and Acinetobacter.

Originator

Approval Year

PubMed

Sample Use Guides

In Vivo Use Guide
Studies in humans showed that oral doses of 50 to 2,500 mg were well absorbed, but some metabolic hydrolysis occurred before the drug reached the general circulation. Oral bioavailability was approximately 50% and was largely independent of dose.
Route of Administration: Oral
In Vitro Use Guide
E.coli were the most susceptible to alafosfalin among all species, among 144 isolates, 93 and 86% of the strains were inhibited by 12.5 and 1.56 ug/ml, respectively, whereas the MIC50 was 0.39 ug/ml.
Substance Class Mixture
Record UNII
XMK47YQG9R
Record Status Validated (UNII)
Record Version
All of the following components must be present:
Definition References
(2)