BOSTON, MA, USA I November 01, 2022 IMonte Rosa Therapeutics, Inc. (NASDAQ: GLUE), a biotechnology company developing novel molecular glue degrader (MGD)-based medicines, today announced the company has dosed the first patient in its Phase 1/2 clinical trial evaluating MRT-2359 for the treatment of MYC-driven solid tumors, including lung cancer. MRT-2359 is a potent, selective and orally bioavailable GSPT1-directed MGD, designed to disrupt protein synthesis in MYC-driven tumors, and lead to anti-tumor activity.
“MYC transcription factors are well-defined drivers of human cancers, and disrupting protein translation has emerged as a promising path to address this highly prevalent disease pathway. Dosing the first patient is a significant milestone in developing MRT-2359 as a therapeutic option for MYC-driven cancers,” said Filip Janku, M.D., Ph.D., Chief Medical Officer of Monte Rosa. “We have designed our Phase 1 trial to move efficiently through dose escalation and, by focusing on tumor types where MYC expression is prevalent, to improve our chances of seeing early signals of clinical activity. We are encouraged by the strong preclinical data and hope that MRT-2359 will make a meaningful difference in the lives of patients.”
The Phase 1/2, open-label, multicenter study will primarily assess the safety, tolerability, pharmacokinetic (PK), pharmacodynamic (PD) and preliminary clinical activity of MRT-2359 in patients with previously treated selected solid tumors, including non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), high-grade neuroendocrine cancer of any primary site, diffuse large B-cell lymphoma (DLBCL) and solid tumors with L-MYC or N-MYC amplification. In the Phase 1 portion of the study, patients will receive escalating doses of MRT-2359 to determine the maximum tolerated dose (MTD) and recommended Phase 2 dose (RP2D). Once the RP2D is determined, the anti-tumor activity of MRT-2359 will be assessed as part of the Phase 2 portion of the study, which includes molecular biomarkers for stratification and selection.
To learn more about the MRT-2359 clinical trial, visit clinicaltrials.gov (Identifier: NCT05546268).
About MRT-2359
MRT-2359 is a potent, selective and orally bioavailable molecular glue degrader (MGD) that induces the interaction between the E3 ubiquitin ligase component cereblon (CRBN) and the translation termination factor GSPT1, leading to the targeted degradation of GSPT1 protein. The MYC transcription factors (c‑MYC, L-MYC and N-MYC) are well-established drivers of human cancers that maintain high levels of protein translation, which is critical for uncontrolled cell proliferation and tumor growth. Our preclinical studies have shown that this addiction to MYC-induced protein translation creates a dependency on GSPT1. MRT-2359 exploits this vulnerability by inducing degradation of GSPT1, disrupting protein synthesis preferentially in MYC-driven cell lines and leading to anti-tumor activity in MYC-driven tumor models. Our ongoing Phase 1/2 clinical study aims to evaluate the safety, tolerability and anti-tumor activity of MRT-2359.
About Monte Rosa
Monte Rosa Therapeutics is a biotechnology company developing a portfolio of novel molecular glue degrader (MGD) medicines. These medicines are designed to employ the body’s natural mechanisms to selectively eliminate therapeutically relevant proteins. The company has developed a proprietary protein degradation platform, called QuEEN™ (Quantitative and Engineered Elimination of Neosubstrates), that enables it to rapidly identify protein targets and MGD product candidates that are designed to eliminate therapeutically relevant proteins in a highly selective manner. The company’s drug discovery platform combines diverse and proprietary chemical libraries of small molecule protein degraders with in-house proteomics, structural biology, AI/machine learning-based target selection, and computational chemistry capabilities to predict and obtain protein degradation profiles. For more information, visit www.monterosatx.com.
SOURCE: Monte Rosa Therapeutics
Post Views: 122
BOSTON, MA, USA I November 01, 2022 IMonte Rosa Therapeutics, Inc. (NASDAQ: GLUE), a biotechnology company developing novel molecular glue degrader (MGD)-based medicines, today announced the company has dosed the first patient in its Phase 1/2 clinical trial evaluating MRT-2359 for the treatment of MYC-driven solid tumors, including lung cancer. MRT-2359 is a potent, selective and orally bioavailable GSPT1-directed MGD, designed to disrupt protein synthesis in MYC-driven tumors, and lead to anti-tumor activity.
“MYC transcription factors are well-defined drivers of human cancers, and disrupting protein translation has emerged as a promising path to address this highly prevalent disease pathway. Dosing the first patient is a significant milestone in developing MRT-2359 as a therapeutic option for MYC-driven cancers,” said Filip Janku, M.D., Ph.D., Chief Medical Officer of Monte Rosa. “We have designed our Phase 1 trial to move efficiently through dose escalation and, by focusing on tumor types where MYC expression is prevalent, to improve our chances of seeing early signals of clinical activity. We are encouraged by the strong preclinical data and hope that MRT-2359 will make a meaningful difference in the lives of patients.”
The Phase 1/2, open-label, multicenter study will primarily assess the safety, tolerability, pharmacokinetic (PK), pharmacodynamic (PD) and preliminary clinical activity of MRT-2359 in patients with previously treated selected solid tumors, including non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), high-grade neuroendocrine cancer of any primary site, diffuse large B-cell lymphoma (DLBCL) and solid tumors with L-MYC or N-MYC amplification. In the Phase 1 portion of the study, patients will receive escalating doses of MRT-2359 to determine the maximum tolerated dose (MTD) and recommended Phase 2 dose (RP2D). Once the RP2D is determined, the anti-tumor activity of MRT-2359 will be assessed as part of the Phase 2 portion of the study, which includes molecular biomarkers for stratification and selection.
To learn more about the MRT-2359 clinical trial, visit clinicaltrials.gov (Identifier: NCT05546268).
About MRT-2359
MRT-2359 is a potent, selective and orally bioavailable molecular glue degrader (MGD) that induces the interaction between the E3 ubiquitin ligase component cereblon (CRBN) and the translation termination factor GSPT1, leading to the targeted degradation of GSPT1 protein. The MYC transcription factors (c‑MYC, L-MYC and N-MYC) are well-established drivers of human cancers that maintain high levels of protein translation, which is critical for uncontrolled cell proliferation and tumor growth. Our preclinical studies have shown that this addiction to MYC-induced protein translation creates a dependency on GSPT1. MRT-2359 exploits this vulnerability by inducing degradation of GSPT1, disrupting protein synthesis preferentially in MYC-driven cell lines and leading to anti-tumor activity in MYC-driven tumor models. Our ongoing Phase 1/2 clinical study aims to evaluate the safety, tolerability and anti-tumor activity of MRT-2359.
About Monte Rosa
Monte Rosa Therapeutics is a biotechnology company developing a portfolio of novel molecular glue degrader (MGD) medicines. These medicines are designed to employ the body’s natural mechanisms to selectively eliminate therapeutically relevant proteins. The company has developed a proprietary protein degradation platform, called QuEEN™ (Quantitative and Engineered Elimination of Neosubstrates), that enables it to rapidly identify protein targets and MGD product candidates that are designed to eliminate therapeutically relevant proteins in a highly selective manner. The company’s drug discovery platform combines diverse and proprietary chemical libraries of small molecule protein degraders with in-house proteomics, structural biology, AI/machine learning-based target selection, and computational chemistry capabilities to predict and obtain protein degradation profiles. For more information, visit www.monterosatx.com.
SOURCE: Monte Rosa Therapeutics
Post Views: 122
