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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Guardian Therapeutics
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Lexington, MA 02421
+1 (781) 918-6580

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