Science2 – Giiant Pharma

Targeting

The Site of Inflammation

the science

Orally-Delivered | Gut-Restricted

GiiAnt, the Gastrointestinal-induced Anti-inflammatory technology, is a unique targeted delivery strategy that capitalize on the bacterial activity of the gut microbiota to bioactivate and specifically release the active principle in the lower bowel of the GI tract. This validated and proven strategy still represents the best way to improve the therapeutic index of a pharmacologic treatment. Although orally-delivered, Giiant’s drug candidates are not systemically absorbed while still achieving high drug concentration in the colonic area.

giiant technology

Potent anti-inflammatory agents have been engineered as prodrugs to target only the colonic area

Current efforts of Giiant Pharma in the field of IBD are targeting the moderate-to-severe ulcerative colitis segment of patient population. With the main objective of minimizing treatment-associated side effects, we have identified a novel and potent oral anti-inflammatory agent that gets delivered only to the large intestine (local action). Why delivering a drug to your brain, heart, liver, skin, muscle and others when only your colon is affected? Is it possible to benefit from an anti-inflammatory treatment without suffering from the strong immunosuppression from prednisone, azathioprine or injectable biologics? Our gut-specific delivery platform addresses these two questions with a prodrug technology that confines the anti-inflammatory agent to the sick organ without systemically compromising patient’s immune system.

Orally-Delivered

The prodrug is conveniently orally-dosed but poorly absorbed in the upper GIT. Furthermore, the low bacterial activity found in the small intestine, prevents the premature release of the parent active principle. This allows most of the dose to reach the lower bowel while minimizing systemic exposure.

Gut Bacterial Activation

The sharp gradient of bacterial activity between the upper GIT and the lower bowel is used as a very specific trigger to bioactivate the prodrug in the colonic area.

Active Principle Release

The enzymatic breakdown of the covalent bound linking the parent anti-inflammatory agent and the promoiety releases the active principle. This local delivery represents the best strategy to avoid systemic immunosuppression while maximizing the drug concentration at the site of inflammation.

Dynamic Release System

The ultimate level of precision for drug delivery

The concept of Dynamic Release System (disease-inducible bioactivation) is illustrated below. Even though the prodrug is bioactivated in the non-inflamed area (A), some of it keep progressing to the active site of inflammation (B) where the presence of blood, from colon mucosa ulceration, activates the prodrug. This results in a significant increase in the rate of enzymatic break down and therefore, a higher local concentration of the parent anti-inflammatory agent.