Monte Rosa Therapeutics has dosed the first participants in the Phase I trial of the NEK7-directed molecular glue degrader (MGD), MRT-8102, aimed at treating inflammatory conditions that are driven by NLRP3 inflammasome, IL-1β, and IL-6.
The double-blind, randomised, placebo-controlled trial aims to assess the tolerability, safety, pharmacokinetics (PK), and pharmacodynamics (PD), as well as NEK7 degradation and ex vivo responses to inflammasome stimulation.
Go deeper with GlobalData
Discover B2B Marketing That Performs
Combine business intelligence and editorial excellence to reach engaged professionals across 36 leading media platforms.
It includes single ascending dose (SAD) and multiple ascending dose (MAD) cohorts, involving healthy volunteers.
Part three of the trial will involve patients at higher risk of cardiovascular disease (CVD) due to obesity and elevated C-reactive protein (CRP) levels.
This segment of the trial aims to assess the tolerability and safety of MRT-8102, as well as its impact on CRP levels, PK and other inflammatory markers.
Initial outcomes from the trial are anticipated in the first half of 2026.
US Tariffs are shifting - will you react or anticipate?
Don’t let policy changes catch you off guard. Stay proactive with real-time data and expert analysis.
By GlobalDataMonte Rosa Therapeutics CEO Markus Warmuth said: “MRT-8102 is the only clinical-stage MGD that selectively targets NEK7, a protein central to NLRP3 inflammasome activation and the downstream dysregulation of IL-1β and IL-6 that underlie multiple inflammatory diseases.
“We believe MRT-8102 could offer a differentiated approach to treating these diseases based on the exciting potency, selectivity, and durable pharmacodynamics seen in our preclinical studies.
“Importantly, one cohort of the ongoing Phase I study will evaluate changes in CRP and other key inflammatory markers in subjects with high CVD risk. We believe this cohort could provide early proof of concept for cardio-immunology indications such as pericarditis and atherosclerotic cardiovascular disease and help guide future development activities.”
The company develops MGD medicines for people with serious conditions, in the autoimmune, oncology and inflammatory disease areas.
It has a worldwide licence deal with Novartis for progressing VAV1-directed MGDs and a partnership with Roche for discovering MGDs targeting cancer and neurological conditions.
