Monte Rosa Therapeutics Announces First Subjects Dosed in Phase 1 Study of MRT-8102, a NEK7-Directed Molecular Glue Degrader for the Treatment of Multiple Inflammatory Diseases
Monte Rosa Therapeutics (Nasdaq: GLUE) has initiated dosing in a Phase 1 study of MRT-8102, their novel NEK7-directed molecular glue degrader (MGD) for inflammatory diseases. The study includes single and multiple ascending dose cohorts in healthy volunteers, with initial results expected in H1 2026.
The randomized, double-blind, placebo-controlled trial will evaluate safety, pharmacokinetics, NEK7 protein degradation, and pharmacodynamic markers. Notably, the study includes a special cohort focusing on subjects with high cardiovascular disease risk and elevated CRP, potentially providing early proof of concept for cardio-immunology indications like pericarditis and atherosclerotic cardiovascular disease.
Monte Rosa Therapeutics (Nasdaq: GLUE) ha iniziato la somministrazione di dosi in uno studio di Fase 1 su MRT-8102, il loro nuovo degradatore molecolare a colla (MGD) diretto contro NEK7 per le malattie infiammatorie. Lo studio prevede coorti con dosi singole e multiple crescenti in volontari sani, con i primi risultati attesi nella prima metà del 2026.
Lo studio, randomizzato, in doppio cieco e controllato con placebo, valuterà la sicurezza, la farmacocinetica, la degradazione della proteina NEK7 e i marcatori farmacodinamici. Di particolare rilievo, include una coorte speciale dedicata a soggetti con alto rischio cardiovascolare e livelli elevati di PCR, offrendo potenzialmente una prima conferma del concetto per indicazioni cardio-immunologiche come la pericardite e le malattie cardiovascolari aterosclerotiche.
Monte Rosa Therapeutics (Nasdaq: GLUE) ha comenzado la administración de dosis en un estudio de Fase 1 de MRT-8102, su nuevo degradador molecular tipo pegamento (MGD) dirigido a NEK7 para enfermedades inflamatorias. El estudio incluye cohortes de dosis ascendentes únicas y múltiples en voluntarios sanos, con resultados iniciales esperados para la primera mitad de 2026.
El ensayo aleatorizado, doble ciego y controlado con placebo evaluará la seguridad, farmacocinética, degradación de la proteína NEK7 y marcadores farmacodinámicos. Destaca la inclusión de una cohorte especial centrada en sujetos con alto riesgo cardiovascular y PCR elevada, lo que podría proporcionar una prueba temprana del concepto para indicaciones cardio-inmunológicas como la pericarditis y la enfermedad cardiovascular aterosclerótica.
Monte Rosa Therapeutics (나스닥: GLUE)가 염증성 질환 치료를 위한 새로운 NEK7 표적 분자 글루 분해제(MGD)인 MRT-8102의 1상 임상시험에서 투약을 시작했습니다. 이 연구는 건강한 지원자를 대상으로 단회 및 다회 용량 상승 코호트를 포함하며, 초기 결과는 2026년 상반기에 발표될 예정입니다.
무작위 배정, 이중 맹검, 위약 대조 시험으로서 안전성, 약동학, NEK7 단백질 분해 및 약력학적 지표를 평가합니다. 특히, 심혈관 질환 고위험군 및 C-반응성 단백질(CRP) 상승자를 대상으로 하는 특별 코호트를 포함하여 심낭염 및 죽상동맥경화성 심혈관 질환과 같은 심장-면역학 적응증에 대한 초기 개념 증명을 제공할 가능성이 있습니다.
Monte Rosa Therapeutics (Nasdaq : GLUE) a débuté l’administration de doses dans une étude de phase 1 sur MRT-8102, leur nouveau dégradeur moléculaire à colle (MGD) ciblant NEK7 pour les maladies inflammatoires. L’étude comprend des cohortes à doses uniques et multiples ascendantes chez des volontaires sains, avec des premiers résultats attendus au premier semestre 2026.
L’essai randomisé, en double aveugle et contrôlé par placebo évaluera la sécurité, la pharmacocinétique, la dégradation de la protéine NEK7 et les marqueurs pharmacodynamiques. Notamment, l’étude inclut une cohorte spéciale portant sur des sujets présentant un risque cardiovasculaire élevé et une CRP élevée, offrant potentiellement une preuve de concept précoce pour des indications cardio-immunologiques telles que la péricardite et les maladies cardiovasculaires athérosclérotiques.
Monte Rosa Therapeutics (Nasdaq: GLUE) hat mit der Dosierung in einer Phase-1-Studie von MRT-8102 begonnen, ihrem neuartigen NEK7-gerichteten molekularen Klebstoff-Degrader (MGD) für entzündliche Erkrankungen. Die Studie umfasst einzelne und multiple aufsteigende Dosisgruppen bei gesunden Freiwilligen, mit ersten Ergebnissen, die für das erste Halbjahr 2026 erwartet werden.
Die randomisierte, doppelblinde, placebokontrollierte Studie wird Sicherheit, Pharmakokinetik, NEK7-Proteinabbau und pharmakodynamische Marker bewerten. Besonders hervorzuheben ist eine spezielle Kohorte mit Probanden mit hohem kardiovaskulärem Risiko und erhöhtem CRP, die möglicherweise einen frühen Wirksamkeitsnachweis für kardiologische Immunindikationen wie Perikarditis und atherosklerotische Herz-Kreislauf-Erkrankungen liefert.
- First-in-class NEK7-directed molecular glue degrader entering clinical trials
- Study design includes potential early proof of concept in cardiovascular disease patients
- Unique approach targeting NLRP3 inflammasome activation pathway
- Demonstrated strong preclinical results in potency, selectivity, and durability
- Initial results not expected until H1 2026
- Early-stage clinical trial with no efficacy data yet
Insights
Monte Rosa's novel NEK7 degrader enters Phase 1 with potential differentiation in inflammatory diseases; results expected H1 2026.
Monte Rosa Therapeutics has initiated dosing in a Phase 1 study for MRT-8102, representing a significant clinical milestone for their immunology and inflammation pipeline. This molecular glue degrader (MGD) is particularly noteworthy as it's the only clinical-stage candidate targeting NEK7, a protein central to NLRP3 inflammasome activation that drives multiple inflammatory conditions.
The study design reveals Monte Rosa's strategic approach to early clinical development. Beyond standard single and multiple ascending dose cohorts in healthy volunteers assessing safety and pharmacokinetics, the company has intelligently incorporated pharmacodynamic markers to demonstrate target engagement through NEK7 degradation and downstream effects on inflammasome activation.
Most compelling is the inclusion of a cohort with subjects having elevated cardiovascular disease risk and high CRP levels. This element potentially provides early proof-of-concept data for cardio-immunology indications including pericarditis and atherosclerotic cardiovascular disease. This approach could significantly accelerate development by providing preliminary efficacy signals directly in the Phase 1 study, rather than waiting for separate Phase 2 trials.
The timeline for initial results in H1 2026 sets clear expectations for investors. While this represents a standard development pace, the innovative study design with the high-risk CVD cohort could provide meaningful biological activity data that typically wouldn't emerge until later-stage trials. This may de-risk subsequent development stages and inform prioritization of specific inflammatory indications for Phase 2 studies.
MRT-8102 Phase 1 study includes single and multiple ascending dose cohorts in healthy volunteers and is designed to evaluate safety, pharmacokinetics, NEK7 protein degradation, and other key downstream pharmacodynamic markers; initial results anticipated in H1 2026
Additional Phase 1 cohort designed to evaluate potential early proof of concept in subjects with increased cardiovascular disease (CVD) risk and elevated CRP
BOSTON, Mass., July 21, 2025 (GLOBE NEWSWIRE) -- Monte Rosa Therapeutics, Inc. (Nasdaq: GLUE), a clinical-stage biotechnology company developing novel molecular glue degrader (MGD)-based medicines, today announced that the first subjects have been dosed in a Phase 1 study evaluating MRT-8102, a NEK7-directed MGD being developed for the treatment of inflammatory conditions driven by the NLRP3 inflammasome, IL-1β, and IL-6. Initial results from the Phase 1 study are expected in H1 2026.
“The initiation of the MRT-8102 Phase 1 study represents another exciting step forward for our immunology and inflammation pipeline,” said Markus Warmuth, M.D., Chief Executive Officer of Monte Rosa Therapeutics. “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 1 study will evaluate changes in C-reactive protein (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 MRT-8102 Phase 1 study is a randomized, double-blind, placebo-controlled trial in healthy volunteers that includes both single ascending dose (SAD) and multiple ascending dose (MAD) cohorts. The study is designed to evaluate safety and tolerability, pharmacokinetics (PK), and pharmacodynamics (PD), including NEK7 degradation and ex vivo responses to inflammasome stimulation. Part 3 of the Phase 1 study is a randomized, placebo-controlled trial that will enroll subjects with increased CVD risk due to obesity and elevated CRP, designed to evaluate safety and tolerability, change in CRP levels, pharmacokinetics, and changes in other inflammatory markers.
About MRT-8102
MRT-8102 is a potent, highly selective, and orally bioavailable investigational molecular glue degrader (MGD) that targets NEK7 for the treatment of inflammatory diseases linked to NLRP3, IL-1β, and IL-6 dysregulation. NEK7 has been shown to be required for NLRP3 inflammasome assembly, activation and IL-1β release both in vitro and in vivo. Aberrant NLRP3 inflammasome activation and the subsequent release of active IL-1β and interleukin-18 (IL-18) has been implicated in multiple inflammatory disorders, including cardiovascular disease, gout, osteoarthritis, neurologic disorders including Parkinson’s disease and Alzheimer’s disease, and metabolic disorders. In a non-human primate model, MRT-8102 was shown to potently, selectively, and durably degrade NEK7, and resulted in near-complete reductions of IL-1β and caspase-1 following ex vivo stimulation of whole blood. MRT-8102 has demonstrated a considerable safety margin (>200-fold exposure margin over projected human efficacious dose) in GLP toxicology studies.
About Monte Rosa
Monte Rosa Therapeutics is a clinical-stage biotechnology company developing highly selective molecular glue degrader (MGD) medicines for patients living with serious diseases in the areas of oncology, autoimmune and inflammatory diseases, and more. MGDs are small molecule protein degraders that have the potential to treat many diseases that other modalities, including other degraders, cannot. Monte Rosa’s QuEEN™ (Quantitative and Engineered Elimination of Neosubstrates) discovery engine combines AI-guided chemistry, diverse chemical libraries, structural biology, and proteomics to rationally design MGDs with unprecedented selectivity. Monte Rosa has developed the industry’s leading pipeline of MGDs, which spans autoimmune and inflammatory diseases, oncology, and beyond. Monte Rosa has a global license agreement with Novartis to advance VAV1-directed molecular glue degraders and a strategic collaboration with Roche to discover and develop MGDs against targets in cancer and neurological diseases previously considered impossible to drug. For more information, visit www.monterosatx.com.
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FAQ
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