The Discovery of GSK2251052: A First-in-Class Boron ... - Anacor
The Discovery of GSK2251052: A First-in-Class Boron ... - Anacor
The Discovery of GSK2251052: A First-in-Class Boron ... - Anacor
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Phase II Cl<strong>in</strong>ical Studies<br />
LRS114689: Comparative, dose-rang<strong>in</strong>g study <strong>of</strong> <strong>GSK2251052</strong> vs.<br />
meropenem <strong>in</strong> <strong>in</strong> the treatment <strong>of</strong> complicated <strong>in</strong>tra-abdom<strong>in</strong>al <strong>in</strong>fection<br />
LRS114688: Comparative, dose-rang<strong>in</strong>g study <strong>of</strong> <strong>GSK2251052</strong> vs.<br />
imipenem-cilastat<strong>in</strong> <strong>in</strong> complicated lower ur<strong>in</strong>ary tract <strong>in</strong>fection and<br />
pyelonephritis<br />
– Both studies are dose rang<strong>in</strong>g , 750mg:1500mg twice a day: Active Comparator<br />
– 210 subjects per study<br />
– Independent Safety Review Committee<br />
– Decide on the most appropriate and safe dose for Phase III<br />
In PH2 cUTI study 4 <strong>of</strong> 14 patients (20 patients enrolled) saw a rapid<br />
emergence <strong>of</strong> mutants with high <strong>GSK2251052</strong> MIC values<br />
– Mutations were <strong>in</strong> leuS<br />
In PH2 cIAI study no resistance mutants were discovered <strong>in</strong> 15 patients<br />
enrolled<br />
Work is ongo<strong>in</strong>g to determ<strong>in</strong>e future development options for<br />
<strong>GSK2251052</strong><br />
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