Gastroenterology
Advantages of an Oral Aptamer
Oral administration of highly stable, non-absorbed inhibitor aptamer will:
Provide a local effect on GI mucosa
With a very patient-friendly dosing regimen…
While avoiding systemic immunosuppression and thrombosis-related risks
Guardian’s Aptamers Remain Intact Even Under Conditions of the GI Tract
Incubated in simulated gastric fluids
Assayed for full-length, intact, aptamer
Virtually 100% preserved for full duration of incubation
Fully 2’OMethyl Aptamer Passes Intact Through Entire Length of GI Tract
Fully 2’OMethyl aptamer assayed in mass balance study
POC with naked VWF aptamer (BT100) and VWF aptamer w/40KDa PEG (BT200)
HPLC-FL method used for full-length, intact aptamer detection with high sensitivity
~20% total naked aptamer dose recovered in feces
Fecal concentration is 50,000-fold higher than plasma Cmax
Fecal recovery is probably underestimated, as the fecal extraction method has not yet been optimized
~40% total PEGylated aptamer dose recovered in feces
Zero detected in plasma
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