TOP1288 / Topivert - LARVOL DELTA

THE PHARMACOLOGICAL PROFILE OF TOP1288, A NARROW SPECTRUM KINASE INHIBITOR (NSKI) IN CLINICAL DEVELOPMENT AS AN ANTI-INFLAMMATORY TREATMENT FOR ULCERATIVE COLITIS (DDW 2017) - "...The activity of TOP1288, an NSKI in clinical development, has been compared to selective kinase inhibitors (BIRB-796, dasatinib and BAY-61-3606) in a range of innate and adaptive inflammatory cell assays...TOP1288 inhibited spontaneous IL-1β, IL-6 and IL-8 release from inflamed colonic biopsies with efficacy similar to or greater than prednisolone...Targeted, multi-kinase inhibition using the NSKI TOP1288 leads to an efficacious and broad inhibitory profile in UC tissues and across a range of cell types including epithelial cells, innate and adaptive immune cells. TOP1288, which is in clinical development, may provide significant advantages over existing selective kinase approaches thus offering a much improved therapeutic benefit in IBD."

Clinical • Biosimilar • Immunology • Inflammatory Bowel Disease • Rheumatoid Arthritis

TOP2: Phase 2a Study to Evaluate the Safety/Tolerability and Efficacy of TOP1288 200 mg Rectal Solution Once Daily for 4 Weeks in Ulcerative Colitis (clinicaltrials.gov) - P2a; N=77; Completed; Sponsor: Topivert Pharma Ltd; Recruiting ➔ Completed; N=60 ➔ 77

Enrollment change • Trial completion • Biosimilar • Immunology • Inflammation • Inflammatory Bowel Disease

Study for Safety and Tolerability of TOP1288 Administered Rectally in Healthy and Ulcerative Colitis Subjects (clinicaltrials.gov) - P1; N=70; Recruiting; Sponsor: Topivert Pharma Ltd; Trial primary completion date: Jan 2016 ➔ Jul 2016

Trial primary completion date • Biosimilar • Immunology • Inflammatory Bowel Disease

TopiVert Pharma Limited: positive results from TOP1288 phase 1 study (GlobeNewswire) - P1, N= NA; NCT03071081; Sponsor: TopiVert Pharma Ltd; "The results demonstrated that TOP1288 was being delivered to the colon with drug detected in tissue biopsies up to 36 hours after last dose. In addition, dose-dependent positive effects on markers of target engagement and biomarker responses were seen...indicating that the measured concentrations were pharmacologically relevant. TOP1288 was also found to be safe and well tolerated when administered orally with minimal systemic absorption being noted, confirming results from prior studies."

P1 data