Sarafloxacin (DB11491): A Comprehensive Pharmacological and Regulatory Monograph

1.0 Executive Summary

Sarafloxacin is a second-generation fluoroquinolone antibiotic developed by Abbott Laboratories exclusively for veterinary applications.[1] Characterized as a synthetic organic small molecule, its primary intended use was the control of colibacillosis, a significant bacterial disease caused by

Escherichia coli, in poultry, specifically broiler chickens and turkeys.[3] Its mechanism of action is characteristic of its class, involving the potent inhibition of essential bacterial enzymes—DNA gyrase and topoisomerase IV—thereby disrupting DNA replication and leading to a rapid bactericidal effect.[5]

In vitro studies demonstrated that Sarafloxacin possessed a broad spectrum of activity and high potency against a range of Gram-negative and Gram-positive pathogens, with efficacy comparable to established fluoroquinolones like ciprofloxacin.[4]

Despite its promising antimicrobial profile, the clinical and regulatory trajectory of Sarafloxacin was complex and ultimately short-lived. Pharmacokinetic studies revealed significant variability across species, a factor that profoundly influenced its safety assessment. While demonstrating adequate absorption and distribution in target avian species, its oral bioavailability was found to be markedly low in humans.[8] This specific characteristic led international regulatory bodies, such as the Joint FAO/WHO Expert Committee on Food Additives (JECFA), to adopt a forward-thinking approach to its human safety evaluation. The Acceptable Daily Intake (ADI) was established not on traditional toxicological endpoints, but on the potential microbiological impact of unabsorbed drug residues on human gut flora, a decision that set a significant precedent in the assessment of veterinary antimicrobials.[9]