Monte Rosa Therapeutics Updates on MRT-2359 and MRT-6160 Development Progress

Monte Rosa Therapeutics, Inc., a clinical-stage biotechnology company listed on Nasdaq under the ticker GLUE, has announced significant progress in its two lead programs, MRT-2359 and MRT-6160. The company specializes in developing innovative molecular glue degrader (MGD)-based medicines aimed at tackling serious diseases, including those in oncology and autoimmune conditions.

MRT-2359 is undergoing a Phase 1/2 clinical trial targeting MYC-driven solid tumors. The trial has successfully completed the 0.5 mg dosing group using a 21 days on, 7 days off regimen, demonstrating a favorable safety and pharmacodynamic profile. Based on these positive results, Monte Rosa considers this dosing strategy as a potential recommended Phase 2 dose. The company is also evaluating a higher 0.75 mg dose with the same dosing schedule. By the second half of 2024, Monte Rosa expects to determine the final recommended Phase 2 dose and provide updated clinical results, moving forward with the Phase 2 expansion cohorts.

MRT-2359 is a highly selective, orally bioavailable investigational drug designed to degrade the GSPT1 protein by facilitating its interaction with the cereblon E3 ubiquitin ligase. This targeted degradation disrupts protein synthesis mechanisms critical for tumor growth in MYC-driven cancers, which rely heavily on continuous protein production for unchecked cell proliferation.

Simultaneously, Monte Rosa has made strides with MRT-6160, aimed at treating systemic and neurological autoimmune diseases. The company has achieved IND submission to the U.S. FDA, paving the way for clinical trials. MRT-6160 targets the VAV1 protein, a signaling molecule in T and B cells, which plays a pivotal role in autoimmune diseases. Preclinical studies have shown that MRT-6160 can selectively degrade VAV1, reducing cytokine secretion and potentially offering therapeutic benefits for conditions like rheumatoid arthritis, multiple sclerosis, and inflammatory bowel disease.

Monte Rosa plans to initiate a Phase 1 single ascending dose/multiple ascending dose (SAD/MAD) study for MRT-6160 later this summer, with initial clinical data expected in the first quarter of 2025. Following the Phase 1 trial, the company intends to proceed with proof-of-concept studies in various autoimmune and inflammatory diseases, exploring applications in dermatology, rheumatology, and neurology.

Monte Rosa's unique approach leverages its proprietary QuEEN™ (Quantitative and Engineered Elimination of Neosubstrates) discovery engine. This platform combines AI-guided chemistry, extensive chemical libraries, structural biology, and proteomics to identify and design MGDs with unprecedented selectivity. QuEEN™ enables the company to target a wide array of well-validated biological pathways across multiple therapeutic areas, offering potential solutions for diseases previously considered untreatable.

The company's promising pipeline of MGDs extends across oncology and autoimmune diseases, supported by a strategic collaboration with Roche to develop treatments for cancer and neurological diseases. Monte Rosa's advancements reinforce its leading position in the MGD space, aiming to provide transformative therapies for patients with severe illnesses.

Monte Rosa Therapeutics continues to make headway in clinical development, emphasizing the potential of MGDs in providing new treatment options for challenging diseases. With ongoing trials and future clinical milestones on the horizon, the company is well-positioned to advance its innovative therapies towards broader clinical application.