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Activity of AFN-1252, a novel FabI inhibitor, againstStaphylococcus aureusin anin vitropharmacodynamic model simulating human pharmacokinetics

Year: 2013

Type: article

Abstract: AFN-1252, a potent enoyl-ACP reductase (FabI) inhibitor, is under development for the treatment of Staphylococcus aureus infections. The activity of AFN-1252 against two isolates of S. aureus, MSSA 26213 and MRSA S186, was studied in an in vitro pharmacodynamic model simulating AFN-1252 pharmacokinetics in man. Reductions in bacterial viable count over the first 6 hours were generally 1-2 logs and maximal reductions in viable count were generally achieved at fAUC/MIC ratios of 100-200. Maximum reductions in viable count against MSSA 29213 and MRSA S186 were approximately 4 logs, achieved by 450 mg q12h (fAUC/MIC = 1875) dosing at 28 hours. Staphylococcal resistance to AFN-1252 did not develop throughout the 48-hour experiments. As multidrug resistance continues to increase, these studies support the continued investigation of AFN-1252 as a targeted therapeutic for staphylococcal infections.

Source: Journal of Chemotherapy

DOI: 10.1179/1973947812y.0000000060

Authors: Brian T Tsuji, Yoriko Harigaya, Alan J Lesse, Alan Forrest, Dung Ngo

Institutions: University at Buffalo, State University of New York, United States Food and Drug Administration, Center for Drug Evaluation and Research, State University of New York

Language: English

Topic: Antimicrobial Resistance in Staphylococcus

Subfield: Infectious Diseases

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: hybrid

OpenAlex ID: W2072232626

FWCI: 1.359

Cites: 7

Cited by: 10

Related to: 10