On December 30, 2010, Jenken submitted protocol amendment to FDA. The study design will be a two-stage adaptive group sequential design with one planned interim analysis. This two-stage trial design combines a small scale of dose selection study and a phase 2b confirmatory study. At the first stage, a total of 60 subjects (i.e., 15 subjects per arm) will be enrolled. Additional 44 subjects per arm will be recruited at the second stage depending upon the review of interim data at the end of the first stage. A total of 148 subjects will be required to account for a possible 20% dropout. All subjects will be randomly assigned to each of the 4 treatment groups (5, 15 and 35 mg of JKB-122 and placebo).

JKB-122 is a weak and competitive antagonist to TLR4 (toll-like receptor 4), a type 1 transmembrane protein that is a key mediator of the release of proinflammatory cytokines and inflammatory responses and a member of TLRs which are mainstays of the innate immune system and best known for their role in host defenses against infections. Lipopolysaccharide (LPS), an endotoxin, is a specific agonist for TLR4 and patients infected with chronic HCV infection display more than a 10-fold-increase in serum levels of endotoxins and an increased expression of TLR4. In addition, TLR4 is expressed in two key liver cell types involved in hepatic fibrosis: hepatic stellate cells and Kupffer cells. JKB-122 has been shown to exhibit antifibrotic activity in bile-duct ligated rats which further supports that a TLR4 antagonist is of potential in treating liver fibrosis.

A recent clinical study report that a 62% SVR (sustained viral response) was achieved for HCV-IDU (injectable drug users) patients who received JKB-122 implants during the interferon and ribavirin treatment suggests that the use of JKB-122 is safe in HCV patients and the improvement outcome in immunodeficient IDU patients can be attributed to the immunoneutralizing effects of JKB-122.

Altogether, these results suggest that Jenken's proprietary TLR4 antagonist technology may be useful in the treatment of chronic liver disease or as a hepatoprotective (anti-inflammatory and antifibrotic) drug in normalizing liver enzymes by preventing, treating, and/or stopping the progression of liver damage in HCV-infected patients with elevated liver enzymes who did not respond or intolerable previously to, or relapsed from the current combination therapy option. This technology offers the potential to fulfill the unmet medical need of treating chronic liver disease.

"Jenken's proprietary technology of TLR4 antagonists for neutralizing cytokine overproduction, a specific therapy for chronic inflammation, differs from most, if not all, of the anti-inflammatory drugs available today," said Founder, and Chief Scientific Officer Dr. Edwin Wu. "It offers the potential to fulfill the unmet medical need of restoring normal liver function, regardless of the cause of the liver damage (inflammation or fibrosis) or disease. And we expect it will have broader application for inflammation-associated diseases of the kidney and lung as well."