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11/20/09 Intravenous and Oral Microdose Pharmacokinetics of Three Novel Inhibitors of FabI in Healthy Subjects
Date Posted: |
23 Nov 2009 |
Summary: |
Poster presented at AAPS Annual Conference, LA, California, November 2009. With Affinium Pharmaceuticals and Quotient Clinical. Intravenous and Oral Microdose Pharmacokinetics of Three Novel Inhibitors of FabI in Healthy Subjects |
Download: |
 Affinium Nov 09_AAPS Poster.pdf Download |
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AFN-1492, AFN1534 and AFN 1672 are three FabI compounds selected as potential candidates for novel, oral therapeutics for gram
negative bacterial infections. These compounds were selected based on excellent in vitro potency against a wide range of organisms, potent whole cell Minimal Inhibitory Concentrations (MICs) and desirable pharmacokinetic properties in the mouse, rat and dog. Each molecule has demonstrated oral efficacy in the mouse infection models.
Preclinical pharmacokinetic studies in rat and dog have shown inconsistent species differences in bioavailability and half-life.
In conclusion: Oral and intravenous microdosing of the three candidate FabL inhibitors has provided quantitative data on their bioavailability and pharmacokinetics. This information, together with in vitro MIC and physicochemical considerations will be invaluable in assisting in the selection of one or more of these molecules as potential clinical development candidates.
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