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

MRT-8102, a highly selective NEK7-directed molecular glue degrader (MGD) developed to treat inflammatory conditions linked to NLRP3, IL-1β, and IL-6 dysregulation, expands Monte Rosa’s clinical I&I portfolio Potency, selectivity, and long-lasting pharmacodynamics of MRT-8102 observed in preclinical studies create potential for clinical differentiation from competitive approaches for inflammatory diseases MRT-8102 Phase 1 clinical results, including data on safety, pharmacokinetics, NEK7 protein degradation, and key downstream pharmacodynamic markers, expected in H1 2026 BOSTON, June 10, 2025 (GLOBE NEWSWIRE) -- Monte Rosa Therapeutics, Inc. (Nasdaq: GLUE), a clinical-stage biotechnology company developing novel molecular glue degrader (MGD)-based medicines, today 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. “The IND clearance of MRT-8102 is another important milestone in our quest to broadly establish MGDs as a modality in immunology and inflammatory (I&I) indications. MRT-8102, following on the heels of our VAV1-directed MGD MRT-6160, is our second IND specifically for I&I indications, and represents the only clinical-stage MGD that selectively targets NEK7, with potential to address multiple inflammatory diseases, including cardio-immunology, rheumatology, and respiratory indications,” said Markus Warmuth, M.D., Chief Executive Officer of Monte Rosa Therapeutics. “We believe MRT-8102 could provide a highly differentiated clinical profile compared to IL-1 antibodies and NLRP3 inhibitors in development based on its potency, selectivity, and long-lasting pharmacodynamics. We look forward to initiating a Phase 1 healthy volunteer study in the coming weeks, with clinical results expected in H1 2026, including data on safety, pharmacokinetics, NEK7 protein degradation, and downstream pharmacodynamic markers. As part of the Phase 1 study, we plan to establish initial proof-of-concept (POC) for cardio-immunology indications by evaluating changes in C-reactive protein (CRP) and other key inflammatory markers in a cohort of subjects with high CRP levels.” Monte Rosa believes its preclinical studies support MRT-8102’s potential to address multiple inflammatory diseases driven by the NLRP3 inflammasome, IL-1β and IL-6. MRT-8102 has demonstrated nanomolar-level degradation of NEK7 in vitro with no off-target activity observed, including related NEK family proteins. In non-human primates (NHPs), oral administration of MRT-8102 resulted in near-complete inhibition of downstream inflammatory markers in ex vivo stimulation assays, as well as improvements in pathological measures in inflammatory disease models. Furthermore, in a rabbit gout model, daily oral dosing of MRT-8102 was observed to reduce pathogenic effects, including a reduction in joint swelling and histopathology scores. Preclinical GLP toxicology studies suggest a considerable safety margin for MRT-8102, with a greater than 200-fold exposure margin over the projected human efficacious dose in both rats and NHPs. In addition to MRT-8102, Monte Rosa is also working to advance a second-generation NEK7 program with enhanced CNS penetration with an IND submission expected in 2026. Monte Rosa retains full worldwide rights to MRT-8102 and its second-generation CNS-optimized NEK7 MGDs. About MRT-8102MRT-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 RosaMonte 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. Forward-Looking Statements This communication includes express and implied “forward-looking statements,” including forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995. Forward-looking statements include all statements that are not historical facts and in some cases, can be identified by terms such as “may,” “might,” “will,” “could,” “would,” “should,” “expect,” “intend,” “plan,” “objective,” “anticipate,” “believe,” “estimate,” “predict,” “potential,” “continue,” “ongoing,” or the negative of these terms, or other comparable terminology intended to identify statements about the future. Forward-looking statements contained herein include, but are not limited to, statements about our ability to grow our product pipeline, our ability to successfully complete research and further development and commercialization of our drug candidates in current or future indications, including the timing and results of our clinical trials and our ability to conduct and complete clinical trials, statements regarding our progress and speed of development of only-in-class and first-in-class molecular glue degrader therapeutics, statements around the Company’s QuEEN™ discovery engine and the Company’s view of its potential to rationally design MGDs with unprecedented selectivity, statements about the advancement and timeline of our preclinical and clinical programs, pipeline and the various products therein, including the ongoing development and progress of our NEK7-directed MGD, referred to as MRT-8102, our plans to initiate a Phase 1 study of MRT-8102 in the coming weeks and our expectations for the design and advancement of such Phase 1 study, including updates related to status, safety data, pharmacokinetics, NEK7 protein degradation, and key downstream pharmacodynamic markers and timing of data read-outs, including the planned readout in the first half of 2026, the Company’s statements around the potential of MRT-8102 to address multiple inflammatory diseases driven by the NLRP3 inflammasome, IL-1β and IL-6, including cardio-immunology, rheumatology, and respiratory indications and the Company’s belief that MRT-8102 could provide a highly differentiated clinical profile compared to IL-1 antibodies and NLRP3 inhibitors in development based on its potency, selectivity, and long-lasting pharmacodynamics, statements relating to MRT-8102’s safety margin, as well as statements around the advancement and timeline of a second-generation NEK7 program and expectations to submit an IND to the FDA in 2026, the expected potential clinical benefit of any of our candidates, advancement and application of our platform, statements around our ability to capitalize on and potential benefits resulting from our research and translational insights, including announcements related to preclinical programs, statements regarding regulatory filings for our development programs, including the planned timing of such regulatory filings, such as IND applications, and potential review by regulatory authorities, as well as our expectations of success for our programs, among others. By their nature, these statements are subject to numerous risks and uncertainties, including those risks and uncertainties set forth in our most recent Annual Report on Form 10-K for the year ended December 31, 2024, filed with the U.S. Securities and Exchange Commission on March 20, 2025, and any subsequent filings, that could cause actual results, performance or achievement to differ materially and adversely from those anticipated or implied in the statements. You should not rely upon forward-looking statements as predictions of future events. Although our management believes that the expectations reflected in our statements are reasonable, we cannot guarantee that the future results, performance, or events and circumstances described in the forward-looking statements will be achieved or occur. Recipients are cautioned not to place undue reliance on these forward-looking statements, which speak only as of the date such statements are made and should not be construed as statements of fact. We undertake no obligation to publicly update any forward-looking statements, whether as a result of new information, any future presentations, or otherwise, except as required by applicable law. Certain information contained in these materials and any statements made orally during any presentation of these materials that relate to the materials or are based on studies, publications, surveys and other data obtained from third-party sources and our own internal estimates and research. While we believe these third-party studies, publications, surveys and other data to be reliable as of the date of these materials, we have not independently verified, and make no representations as to the adequacy, fairness, accuracy or completeness of, any information obtained from third-party sources. In addition, no independent source has evaluated the reasonableness or accuracy of our internal estimates or research and no reliance should be made on any information or statements made in these materials relating to or based on such internal estimates and research. InvestorsAndrew Funderburkir@monterosatx.com MediaCory Tromblee, Scient PRmedia@monterosatx.com

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

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