MRT-8102 / Monte Rosa Therap - LARVOL DELTA

Selective Degradation of NIMA-related kinase 7 (NEK7) via a Molecular Glue Degrader Inhibits IL-1 Downstream of NLRP3 Inflammasome Activation: A Novel Therapeutic Approach for Cardiovascular Inflammation (AHA 2025) - "Our studies indicate that MRT-8102 is a potent, selective NEK7 degrader that inhibits NLRP3-driven activity including cytokine release in vivo and in vitro. Therefore, the NEK7-targeting MGD, MRT-8102, holds promise as a novel therapeutic for the treatment of CVD driven by chronic innate immune activation."

Cardiovascular • Inflammation • Obesity • Targeted Protein Degradation • CRBN • IL1B • NLRP3 • TNFA

A First-in-human, 3-part Study of MRT-8102 in Healthy Participants and Participants at Cardiovascular Risk With Elevated CRP (clinicaltrials.gov) - P1 | N=100 | Recruiting | Sponsor: Monte Rosa Therapeutics, Inc

New P1 trial • Cardiovascular

Targeting NLRP3 Inflammasome Activation and Inflammation in Gout with NEK7 Molecular Glue Degraders: A Novel Therapeutic Strategy (EULAR 2025) - "MRT-8102 is a potent and highly selective NEK7 MGD that effectively suppresses NLRP3-driven inflammation. Our findings demonstrate robust inhibition of IL-1β, pyroptosis and ASC speck formation across in vitro models, complete IL-1β suppression in an ex vivo inflammation model in NHPs, and therapeutic efficacy in a functional rabbit model of gout. These results highlight the potential of NEK7-targeting MGDs as a promising therapeutic approach for NLRP3-mediated inflammatory diseases, including gout."

Gout • Inflammation • Inflammatory Arthritis • Musculoskeletal Diseases • Rheumatology • Targeted Protein Degradation • CD14 • CRBN • IL18 • IL1B • NLRP3

Monte Rosa Therapeutics Announces FDA Clearance of IND Application for MRT-8102, a NEK7-Directed Molecular Glue Degrader for the Treatment of Multiple Inflammatory Diseases (The Manila Times) - "Monte Rosa Therapeutics, Inc...announced U.S. Food and Drug Administration (FDA) clearance of an Investigational New Drug (IND) application for MRT-8102, a NEK7-directed MGD being developed for the treatment of inflammatory diseases driven by the NLRP3 inflammasome and IL-1β. The Company plans to initiate a Phase 1 study of MRT-8102 in the coming weeks and anticipates sharing initial results in H1 2026."

IND • New P1 trial • P1 data • Immunology

Monte Rosa Therapeutics Announces Fourth Quarter 2024 Financial Results and Provides Corporate… (GlobeNewswire) - "Submit an IND application for MRT-8102 in H1 2025. Submit an IND application for the second generation NEK7-directed MGD with enhanced CNS penetration in 2026."

IND • Immunology • Inflammation • Oncology

Monte Rosa Therapeutics Announces Second Quarter 2024 Financial Results and Provides Corporate Update (GlobeNewswire) - "ANTICIPATED MILESTONES: Announce the recommended Phase 2 dose for the MRT-2359 Phase 1/2 study and report Phase 1 clinical activity and safety results in H2 2024. The Company also plans to initiate the Phase 2 portion of the study before year-end; Submit an IND application for MRT-8102 in H1 2025. Nominate a development candidate for the CDK2 preclinical program in 2024."

IND • P1 data • Pipeline update • Trial status • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Immunology • Inflammation • Lung Cancer • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor

Monte Rosa Therapeutics Announces Third Quarter 2023 Financial Results and Provides Corporate Update (GlobeNewswire) - "The Company now expects to release the recommended Phase 2 dose for the MRT-2359 Phase 1/2 study in Q2 2024. On track for planned IND submission for MRT-6160 in the first half of 2024. The Company expects to nominate a development candidate for its NEK7 preclinical program in Q1 2024. The Company expects to nominate a development candidate for its CDK2 preclinical program in 2024."

IND • P1/2 data • Pipeline update • Immunology • Oncology • Solid Tumor

Monte Rosa Therapeutics Announces $25 Million Registered Direct Offering, Priced At- the-Market Under Nasdaq Rules (Monte Rosa Therap Press Release) - "Monte Rosa Therapeutics, Inc...today announced that it has raised $25 million at-the-market from a life sciences-dedicated investor....Monte Rosa intends to use the net proceeds from the offering towards its further advancement of its clinical and late preclinical pipeline, including MRT-2359, its orally bioavailable, GSPT1-directed MGD, MRT-6160, its orally bioavailable VAV1-directed MGD, and its NEK7 program, to key value inflection points."

Financing • Immunology • Oncology