Monte Rosa Therapeutics Begins Dosing in MRT-6160 Study
Monte Rosa Therapeutics Begins Dosing in MRT-6160 Study
MRT-6160 is a powerful and selectively designed VAV1-directed molecular glue degrader, presenting a novel therapeutic strategy for addressing both systemic and neurological autoimmune and inflammatory disorders.
Initial results from the Phase 1 clinical trial, including biomarker data demonstrating pharmacodynamic effects, are anticipated to be available in early 2025.
BOSTON, Monte Rosa Therapeutics, Inc. (NASDAQ: GLUE), a clinical-stage biotechnology enterprise focused on the development of groundbreaking molecular glue degrader (MGD)-based therapies, has announced that the first participants have been dosed in its Phase 1 clinical trial, which employs single and multiple ascending dose (SAD/MAD) methodologies involving healthy volunteers. This study evaluates MRT-6160, a VAV1-directed MGD, being specifically developed to treat systemic and neurological autoimmune disorders. Preliminary findings from this Phase 1 study are expected in early 2025.
“We are excited to commence our Phase 1 clinical evaluation of MRT-6160, a potent, highly selective, and orally bioavailable VAV1-directed MGD,” expressed Markus Warmuth, M.D., Chief Executive Officer of Monte Rosa Therapeutics. “We believe that MRT-6160 is the first rationally designed MGD being explored clinically for indications beyond oncology. Our approach with MGDs effectively targets proteins that have historically been difficult to address through traditional treatment options. By targeting VAV1, a crucial regulator linked to T- and B-cell receptor function, MRT-6160 presents a novel opportunity to manage a variety of autoimmune and inflammatory conditions. This Phase 1 trial is structured to deliver essential insights into safety, pharmacokinetics, degradation of VAV1 protein, and critical downstream pharmacodynamic markers such as CD69, IL-2, IL-6, and IL-17, which will further guide our clinical strategy. We eagerly anticipate sharing initial clinical findings from this study in early 2025, followed by potential proof-of-concept trials for conditions including ulcerative colitis and rheumatoid arthritis, among others.”
The development of MRT-6160 is underpinned by promising preclinical evidence across multiple models simulating autoimmune or inflammatory conditions. Additionally, preclinical GLP toxicology data suggest that MRT-6160 could present a unique therapeutic profile for addressing T-cell, T/B-cell, and Th17-mediated systemic and neurological autoimmune diseases. The compound has demonstrated an ability to effectively degrade VAV1 in vitro within human T and B cells, and has shown positive outcomes in various preclinical models related to autoimmune disorders, including those simulating inflammatory bowel conditions, rheumatoid arthritis, and multiple sclerosis.
About MRT-6160
MRT-6160 is an investigational molecular glue degrader targeting VAV1, noted for its potency, high selectivity, and oral bioavailability. Preclinical investigations have confirmed significant degradation of VAV1 with no observed undesired effects on alternative proteins. VAV1, belonging to the Rho-family of guanine nucleotide exchange factors, plays a vital role in the signaling mechanisms downstream of T- and B-cell receptors. The expression of VAV1 is confined to blood and immune cells, including T and B cells. Findings from preclinical studies indicate that strategically targeting VAV1 via MGD results in the modulation of T- and B-cell receptor-related activities, observable both in vitro and in vivo. This modulation is marked by a notable reduction in cytokine secretion, essential proteins involved in the maintenance of autoimmune responses. Furthermore, VAV1-targeted MGDs have yielded encouraging results in preclinical models addressing autoimmune conditions, indicating their potential therapeutic applications across a spectrum of systemic and neurological autoimmune disorders, such as inflammatory bowel disease, rheumatoid arthritis, and other dermatological conditions.
About Monte Rosa
Monte Rosa Therapeutics is committed to advancing innovative molecular glue degrader (MGD) treatments aimed at assisting patients affected by severe diseases in oncology, autoimmune, and inflammatory domains. MGDs are small-molecule protein degraders that hold the potential to address a myriad of illnesses that other modalities have struggled to effectively treat. The company's proprietary QuEEN™ (Quantitative and Engineered Elimination of Neosubstrates) discovery platform harnesses AI-driven chemistry, varied chemical libraries, structural biology, and proteomics to pinpoint degradable protein targets and systematically design MGDs with unmatched selectivity. Through the QuEEN discovery model, Monte Rosa accesses a broad and diverse range of validated biology across several therapeutic areas. Additionally, Monte Rosa boasts the industry's foremost MGD development pipeline, encompassing oncology, autoimmune disorders, and more, alongside a strategic partnership with Roche to identify and develop MGDs for previously undruggable cancer and neurological disease targets. For additional information, you can find resources at www.monterosatx.com.
Contact Information
Investors:
Andrew Funderburk
ir@monterosatx.com
Media:
Cory Tromblee, Scient PR
media@monterosatx.com
Frequently Asked Questions
1. What is MRT-6160 designed to target?
MRT-6160 is engineered to target VAV1, a key regulator involved in T- and B-cell receptor activity, which is relevant for various autoimmune disorders.
2. When are initial results from the MRT-6160 Phase 1 study expected?
The initial Phase 1 clinical results, along with biomarker data, are anticipated to be disclosed in early 2025.
3. What conditions could benefit from MRT-6160?
MRT-6160 may be beneficial for autoimmune diseases such as ulcerative colitis, rheumatoid arthritis, inflammatory bowel disease, and multiple sclerosis.
4. How is MRT-6160 different from traditional treatments?
MRT-6160 utilizes a molecular glue degrader approach, potentially overcoming limitations faced by conventional treatments in targeting difficult-to-drug proteins.
5. Where can I find more information about Monte Rosa Therapeutics?
More information about Monte Rosa Therapeutics and its innovative therapies can be found at its official website: www.monterosatx.com.
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