precision delivery
for patient-tailored therapies

The combination of gut restriction and local bioactivation represents one of the best strategies to improve the therapeutic index of a pharmacologic treatment. giiant first used this approach with PDE4 inhibitor prodrugs to treat IBD.

The lead candidate, GT-2108, meets all the criteria of our Precision Delivery platform.

GT-2108

  • target not engaged until the parent drug is released from prodrug bioactivation at the site of inflammation
  • low permeability in the upper GI tract
  • no premature prodrug bioactivation in the upper GI tract
  • quantitative, enzyme-mediated parent release in the colonic area

gut restricted approach

Following oral administration, giiant’s prodrug candidates are first inactive, poorly absorbed and remain restricted to the gut. This prevents systemic exposure of their active form allowing for safer therapies. Once activated by the gut microbiota at desired location, high concentration of the active drug is achieved locally at the site of inflammation in the GI tract.

PDE4 target

giiant’s Precision Delivery Platform uses the phosphodiesterase-4 (PDE4) enzyme as its first therapeutic target. PDE4 is highly expressed in immune and proinflammatory cells. The inhibition of PDE4 prevents transcription factors, such as NF-κB, from inducing the expression of various proinflammatory mediators involved in IBD, such as TNF-α and various interleukins.

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