The lead candidate, GT-2108, meets all the criteria of our Precision Delivery platform.
- target not engaged until parent 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
- and 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 remained restricted to the gut. This prevents systemic exposure of their active form, for safer therapies. Once activated by the gut microbiota at desired location, it achieves high concentration of active drug, locally at the inflammation site into the GI tract.
giiant’s Precision Delivery Platform uses the phosphodiesterase-4 (PDE4) enzyme as 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, like TNF-alpha and various interleukins.