Feb 13, 2020 Innovation Pharmaceuticals Phase 1 Trial of Brilacidin for Ulcerative Colitis Meets Primary Endpoints; Positive Topline Results of Oral Brilacidin
· Targeted colonic delivery shown
· Drug well-tolerated
WAKEFIELD, MA – February 13, 2020 (GLOBE NEWSWIRE) Innovation Pharmaceuticals (OTCQB:IPIX) (“the Company”), a clinical stage pharmaceutical company, is pleased to announce that preliminary top-line data from its Phase 1 trial (NCT03234465) studying the use of delayed-release tablets of Brilacidin showed the trial met its primary endpoints. In the study, the timed-release OralogiK™ formulation of Brilacidin was radiolabeled (with complexed technetium-99m) and evaluated for safety and colonic delivery in 9 healthy volunteers (6 with Brilacidin and 3 placebo) as part of the Company’s larger clinical development program in Inflammatory Bowel Disease (IBD).
Study results show that Brilacidin delayed-release tablets were well tolerated across all treatment cohorts with no serious adverse events reported. Of the 9 subjects treated, 2 subjects on Brilacidin and 2 subjects on placebo experienced at least one adverse event. The adverse events were of mild intensity and none were deemed to be related to study treatment.
Gamma scintigraphic imaging was used to visualize in vivo performance of the enteric coated delayed release tablets designed to target delivery of Brilacidin (50mg, 100mg, and 200mg) to the colon. For Brilacidin treatments, radiolabel release was observed in the ascending colon for four out of the six subjects and in the terminal ileum and ileocecal junction for the remaining two. Following release, dispersion of the radiolabel was then observed throughout the colon.
A series of images from one Brilacidin study subject are provided below which illustrate the radiolabeled study oral tablet being successfully dispersed into the colon.
Serial blood samples were collected through 24 hours post-dose to assess absorption of oral Brilacidin from the colon. Blood level analysis, using a sensitive limit of quantitation in plasma of 1 ng/mL, demonstrated no quantifiable Brilacidin concentrations at any timepoint across treatment cohorts and shows containment of Brilacidin within the target location. (Confirmatory repeat plasma concentration analyses are ongoing to verify this finding).
Given Brilacidin has shown clinical efficacy with limited absorption in other clinical trials, in Ulcerative Proctitis/Ulcerative Proctosigmoiditis and Oral Mucositis, these results suggest oral Brilacidin for IBD might be safely dosed at even higher levels of drug via targeted release tablet.
Professor Howard Stevens, Principal Investigator for the study and Chairman of BDD Pharma, commented:
“BDD are delighted to have successfully completed the first oral dosing study of Brilacidin, which has demonstrated the capability of its OralogiK™ Technology to deliver a Brilacidin formulation to the colon. The treatments were well-tolerated with no treatment related adverse events. Although absorption of Brilacidin was not observed from analysis of plasma concentrations, this was not unexpected and may indeed be a desirable attribute for a drug that acts by virtue of its local effect on inflamed mucosal surfaces within the lower GI tract. We look forward to further collaboration with Innovation Pharma as this exciting drug progresses through development.”
Nine subjects were enrolled in the single-center, randomized, single-blinded, placebo-controlled, single dose-escalation Phase 1 trial, three subjects per cohort. In each cohort, two subjects received Brilacidin (cohort 1: 50mg; cohort 2: 100mg; and cohort 3: 200mg) and one subject placebo.
About Brilacidin for IBD
Inflammatory Bowel Disease (IBD) is a hard-to-treat, chronic, autoimmune condition that affects approximately 10 million people worldwide, including 3 million people in the U.S., with 70,000 newly diagnosed cases each year. The overall GI market sector is estimated to grow from $35.7 billion in 2015 to $48.4 billion by 2022. Brilacidin is being developed as a novel, non-corticosteroid, non-biologic treatment, with formulation plans including oral tablets for Ulcerative Colitis and Crohn’s Disease, and enema, foam and/or gel for mild-to-moderate Ulcerative Proctitis/Ulcerative Proctosigmoiditis (UP/UPS), two types of IBD. As released previously, a majority of patients treated with Brilacidin administered via retention enema achieved Clinical Remission (Modified Mayo scoring) in a Phase 2, open-label, Proof-of-Concept (PoC) clinical trial evaluating Brilacidin for UP/UPS. In addition, mucosal healing was evidenced by endoscopic review, an increasingly important measure toward establishing a drug’s efficacy. In late 2018, the Company presented a scientific poster—Brilacidin for Inflammatory Bowel Disease (available for download here, pdf)—at the inaugural “IBD Innovate 2018” conference, hosted by the Crohn’s & Colitis Foundation. Brilacidin may be particularly beneficial in treating IBD due to: 1) its ability to inhibit Phosphodiesterase 4 (PDE4), which is being pursued as a novel therapeutic avenue in IBD; and 2) its potential to compensate for defensin deficiencies that are implicated in the pathogenesis of IBD.