Monte Rosa Therapeutics initiates IND-enabling studies for MRT-8102

Monte Rosa Therapeutics announced a novel development candidate, MRT-8102, a potent, highly selective and orally bioavailable NIMA related kinase 7-directed MGD. MRT-8102 is expected to be developed for the treatment of inflammatory diseases driven by interleukin-1beta 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. The NLRP3 inflammasome is a multiprotein complex that regulates the innate immune system and inflammatory signaling. Aberrant NLRP3 inflammasome activation and the subsequent release of active IL-1beta and interleukin-18 has been implicated in multiple inflammatory disorders, including gout, cardiovascular disease, neurological disorders including Parkinson’s disease and Alzheimer’s disease, ocular disease, diabetes, obesity, and liver disease. NEK7 has been shown to be required for NLRP3 inflammasome assembly, activation and IL-1beta release both in vitro and in vivo, and Monte Rosa’s own in vitro and in vivo work has shown that NEK7 degradation leads to blockade of the pathway leading to inhibition of the production of IL-1beta.