Date: 2016-05-09
Type of information: Presentation of results at a congress
phase: 1
Announcement: presentation of results at the Digestive Disease Week (DDW) 2016 in San Diego
Company: Topivert Pharma (UK)
Product: TOP1288
Action
mechanism: kinase inhibitor. TOP1288 is a Narrow Spectrum Kinase Inhibitor (NSKI). NSKIs are a novel class of small molecules targeting key kinases which play pivotal roles as signalling molecules in multiple inflammatory pathways. Inhibition of this combination of kinases leads to potent and broad anti-inflammatory effects in both innate and adaptive immune responses. The compounds are specifically designed to prevent absorption into the circulation, thereby avoiding any propensity for systemic side effects.
Disease: ulcerative colitis
Therapeutic area: Autoimmune diseases - Inflammatory diseases - Digestive diseases
Country: UK
Trial
details: This phase 1 study evaluates the safety and tolerability of TOP1288 rectal single and multiple ascending doses in healthy subjects and multiple doses in subjects with ulcerative colitis. (NCT02463045)
Latest
news: * On May 9, 2016, TopiVert Pharma, a clinical-stage biotechnology company developing Narrow Spectrum Kinase Inhibitors (NSKIs) as novel, locally-acting medicines for the treatment of chronic inflammatory diseases of the gastrointestinal tract and eye, announced that it will present posters on the Phase I study data results and pre-clinical pharmacology for TOP1288, its lead compound for the treatment of ulcerative colitis, a form of inflammatory
bowel disease, at the Digestive Disease Week (DDW) 2016 in San Diego, California, from 21-24 May.
The poster to be presented is "A first-in-human randomized double-blind placebo-controlled clinical trial of a novel narrow spectrum kinase inhibitor". Rowley et al.
* On March 17, 2016, TopiVert Pharma announced positive Phase I study results for TOP1288, its lead compound for the treatment of ulcerative colitis. TopiVert will present the Phase I study data at the 11th Congress of ECCO in Amsterdam on Friday 18 March 2016. The Phase I study results demonstrate that a rectal formulation of TOP1288, a potent inhibitor of key kinases involved in inflammation, has an excellent safety and tolerability profile in healthy volunteers when administered once or twice daily for five days at a dose of up to 200mg. Furthermore, TOP1288 was detected in tissue biopsies taken from the colon 24 hours after dosing, positive signals of target engagement and biomarker response were observed and only minimal drug was found in the systemic circulation. These results support the concept that NSKIs have the potential to produce sustained effects in mucosal tissues after local administration, but without the undesirable side effects often seen in ulcerative colitis patients treated with current systemically available therapies.
TopiVert plans to start a Phase II proof of concept study with a rectal formulation of TOP1288 in ulcerative colitis patients in mid-2016, with results anticipated by mid-2017. This study is designed to demonstrate whether TOP1288 provides a clinical benefit in ulcerative colitis patients with active disease while avoiding significant exposure to healthy tissues outside the gastrointestinal tract.
TopiVert is also planning to start a Phase I study of an oral formulation of TOP1288 in the second half of this year which will similarly report in mid-2017. An oral product offers greater patient acceptability and convenience over a rectal formulation.
* On May 14, 2015, TopiVert Pharma, a clinical-stage biotech focused on the local treatment of serious inflammatory diseases, announced the start of a Phase I study with its lead compound, TOP1288, in ulcerative colitis. TOP1288 is being tested initially in a Phase I study, including volunteers and ulcerative colitis patients, to examine safety and tolerability of a rectal formulation as well as to explore predictive biomarkers for use in later studies. The trial, conducted at a specialist centre in London, is the first part of a programme to deliver a novel oral and rectal anti-inflammatory treatment for patients with ulcerative colitis. The trial will report in 2016.
