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Monte Rosa Therapeutics Announces Initiation of IND Enabling Studies for MRT-8102, A First-in-Class NEK7 Directed Molecular Glue Degrader and NLRP3/IL-1β Pathway Inhibitor
MRT-8102 nominated as first NEK7-directed development candidate, targeting inflammatory diseases driven by IL-1β and the NLRP3 inflammasome MRT-8102 and other
About this update from Monte Rosa Therapeutics, Inc.
[{"type":"text","content":"MRT-8102 nominated as first NEK7-directed development candidate, targeting inflammatory diseases driven by IL-1β and the NLRP3 inflammasome MRT-8102 and other NEK7 program MGDs are potentially applicable across a range of inflammatory disorders, metabolic disorders, as well as ocular and neurological diseases IND-enabling studies ongoing; IND submission anticipated in Q1 2025 BOSTON, March 11, 2024 (GLOBE NEWSWIRE) -- Monte Rosa Therapeutics, Inc. (Nasdaq: GLUE), a clinical-stage biotechnology company developing novel molecular glue degrader (MGD)-based medicines, today announced a novel development candidate, MRT-8102, a potent, highly selective and orally bioavailable NIMA related kinase 7 (NEK7)-directed MGD. MRT-8102 is expected to be developed for the treatment of inflammatory diseases driven by interleukin-1β (IL-1β) and the NLRP3 inflammasome, which are critical elements of the inflammatory process. This is the first development candidate to be declared from the Company’s NEK7 development program. “NEK7 is an essential component of the NLRP3 inflammasome pathway that has been implicated in many serious diseases, and we are excited to advance MRT-8102 toward clinical development,” said Markus Warmuth, M.D., Chief Executive Officer of Monte Rosa Therapeutics. “In preclinical non-human primate studies, MRT-8102 has demonstrated potent and selective degradation of NEK7, reducing downstream IL-1β. We believe MRT-8102 has the potential to be developed in multiple inflammatory diseases, including gout, pericarditis and other cardiovascular diseases. We are also evaluating opportunities for the program in CNS disorders such as Parkinson’s disease as well as in obesity and other metabolic disorders in light of the ability of our NEK7-directed MGDs to penetrate the blood brain barrier. IND-enabling studies are underway, and we plan to file our first IND for the program in the first quarter of 2025. The advancement of MRT-8102, along with our VAV1-directed MGD MRT-6160, which is progressing toward an IND filing in the first half of this year, demonstrates the continued growth of our immunology and inflammation portfolio and the power and versatility of our QuEEN™ discovery engine.” The NLRP3 inflammasome is a multiprotein complex that regulates the innate immune system and inflammatory signaling. Aberrant NLRP3 inflammasome activati...