Monte Rosa Therapeutics Publicizes First Quarter 2024 Monetary Outcomes and Gives Company Replace – Monte Rosa Therapeutics (NASDAQ:GLUE)

MRT-2359, a molecular glue degrader (MGD) being developed for MYC-driven strong tumors, advancing in ongoing Part 1/2 scientific trial; willpower of beneficial Part 2 dose anticipated in Q2 2024; Part 1 scientific information anticipated in H2 2024

MRT-6160, a VAV1-directed MGD in growth for systemic and neurological autoimmune ailments, on observe towards anticipated IND submission in Q2 2024 and initiation of Part 1 SAD/MAD research mid-year; Part 1 scientific information anticipated in Q1 2025

MRT-8102, a first-in-class NEK7-directed MGD and NLRP3/IL-1β pathway inhibitor, demonstrated environment friendly blood-brain barrier penetration and CNS exercise in non-human primates (NHPs); IND submission on observe for Q1 2025

New discovery program unveiled for CCNE1-directed MGDs; first to instantly drug necessary, beforehand undruggable strong tumor oncology goal

Robust money place anticipated to fund operations into H1 2026, enabling development of MRT-2359, MRT-6160, and MRT-8102 applications via scientific milestones

BOSTON, Might 09, 2024 (GLOBE NEWSWIRE) — Monte Rosa Therapeutics, Inc. GLUE, a clinical-stage biotechnology firm growing novel molecular glue degrader (MGD)-based medicines, right this moment reported enterprise highlights and monetary outcomes for the primary quarter ending March 31, 2024.

“We’re excited by the numerous advances made throughout our total portfolio, together with each our oncology and immunology/irritation applications,” mentioned Markus Warmuth, M.D., Chief Government Officer of Monte Rosa Therapeutics. “Our Part 1/2 scientific trial evaluating MRT-2359 for MYC-driven strong tumors is on observe and we plan to announce the beneficial Part 2 dose later this quarter and to report scientific information from this program within the second half of the yr. We eagerly anticipate the initiation of a Part 1 research of MRT-6160, the primary of our MGD drug candidates for immune-related ailments, in mid-2024, with outcomes from the research anticipated in Q1 2025. Preclinical GLP toxicology information we have introduced right this moment, together with information in a number of illness fashions, counsel the potential for a extremely differentiated profile throughout a number of autoimmune ailments. Moreover, MRT-8102, our NEK7-directed MGD focusing on ailments pushed by IL-1β and the NLRP3 inflammasome, is quickly progressing towards scientific research. We have lately demonstrated robust CNS publicity and NEK7 degradation in non-human primates, supporting the potential growth of MRT-8102 in neurologic indications and weight problems amongst others, along with its potential use in gout, pericarditis, and different peripheral inflammatory circumstances. We’re additionally more than happy to announce our discovery program for CCNE1 (Cyclin E1), a well-validated oncology goal usually thought-about undruggable by typical modalities. We imagine our capability to degrade CCNE1 potently and selectively and to elicit anti-tumor exercise in in vivo fashions gives additional validation for the differentiation of our QuEEN™ discovery engine and the potential of our MGDs in opposition to a broad spectrum of targets.”

Dr. Warmuth concluded, “The fast and environment friendly development of our pipeline clearly illustrates the ability of our AI/ML-driven QuEEN™ discovery engine. By means of our ongoing inside efforts in addition to our analysis collaboration with Roche, we stay up for persevering with this robust progress.”

RECENT HIGHLIGHTS

MRT-2359, GSPT1-directed MGD for MYC-driven strong tumors

• Monte Rosa continues to judge MRT-2359 in a Part 1/2 scientific trial in MYC-driven strong tumors (NCT05546268). Enrollment is ongoing in backfill cohorts at clinically energetic doses utilizing a 5-days-on, 9-days-off drug schedule and in dose escalation cohorts utilizing a 21-days-on, 7-days-off drug schedule. The Firm is on observe to find out the beneficial Part 2 dose (RP2D) in Q2 2024 and report Part 1 research leads to H2 2024. Monte Rosa expects to provoke the Part 2 portion of the research earlier than year-end.
• The Firm presented preclinical information on the American Affiliation for Most cancers Analysis (AACR) Annual Assembly demonstrating that therapy with MRT-2359 resulted in marked tumor regressions within the AR-V7- and c-MYC-expressing 22RV1 xenograft mouse mannequin of prostate most cancers related to resistance to anti-androgen brokers.

MRT-6160, VAV1-directed MGD for systemic and neurological autoimmune/inflammatory ailments

• The MRT-6160 program is on observe for an anticipated Investigational New Drug (IND) submission to the U.S. Meals and Drug Administration (FDA) in Q2 2024, and initiation of a Part 1 single ascending dose/a number of ascending dose (SAD/MAD) research in mid-2024. Part 1 outcomes are anticipated in Q1 2025.
• The Firm right this moment introduced further outcomes from accomplished preclinical GLP toxicology research of MRT-6160 in rats and non-human primates (NHPs). The information display a extremely favorable security profile with no vital modifications in peripheral immune cell compartments.
• Monte Rosa expects to current further preclinical information for MRT-6160 in fashions of autoimmune and inflammatory ailments on the upcoming Digestive Illness Week (DDW) and European Alliance of Associations for Rheumatology (EULAR) medical conferences.

MRT-8102, NEK7-directed MGD for inflammatory ailments pushed by IL-1β and the NLRP3 inflammasome

• In March 2024, Monte Rosa announced the initiation of IND-enabling research for MRT-8102, a first-in-class NEK7-directed MGD for the therapy of inflammatory ailments pushed by interleukin-1β (IL-1β) and the NLRP3 inflammasome, vital parts of the inflammatory course of. That is the primary growth candidate to be declared from the Firm’s NEK7 growth program.
• Monte Rosa right this moment introduced that MRT-8102 has demonstrated extremely favorable CNS publicity and degradation in a research in cynomolgus monkeys. The information help the potential for growth of MRT-8102 in ailments together with Parkinson’s illness, Alzheimer’s illness, and weight problems. The Firm is evaluating purposes throughout a number of inflammatory issues.
• Monte Rosa expects to submit an IND utility for MRT-8102 in Q1 2025.

CCNE1-directed MGD program for CCNE1-amplified tumors

• Monte Rosa right this moment introduced a brand new discovery program for CCNE1 (Cyclin E1)-directed MGDs for the therapy of CCNE1-amplified tumors. CCNE1, a key element of the cell cycle and a recognized driver of many cancers, is mostly thought-about an undruggable goal by typical modalities.

Extra company updates

• In October 2023, Monte Rosa entered right into a strategic collaboration and licensing settlement with Roche, a world healthcare chief, to find and develop MGDs in opposition to targets in most cancers and neurological ailments. The collaboration continues to advance analysis actions in line with plan.

ANTICIPATED MILESTONES

• Announce the beneficial Part 2 dose for the MRT-2359 Part 1/2 research in Q2 2024 and report Part 1 scientific leads to H2 2024. Provoke the Part 2 portion of the research earlier than year-end. The Firm is evaluating Part 2 growth cohorts in high-prevalence c-MYC-driven tumors together with hormone receptor-positive breast most cancers and prostate most cancers, in addition to tumor sorts and affected person populations pushed by L- and N-MYC together with non-small cell lung most cancers (NSCLC), small cell lung most cancers (SCLC), and strong tumors with amplifications of L- and N-MYC.
• Submit an IND utility for MRT-6160 in Q2 2024 and provoke a Part 1 SAD/MAD research in wholesome volunteers in mid-2024; report outcomes from the Part 1 research in Q1 2025. Monte Rosa expects to subsequently provoke proof-of-concept (POC) research in autoimmune/inflammatory ailments together with ulcerative colitis and rheumatoid arthritis, with further potential POC research in dermatology, rheumatology, and neurology indications.
• Submit an IND utility for MRT-8102 in Q1 2025.
• Nominate a growth candidate for the CDK2 preclinical program in 2024.

UPCOMING PRESENTATIONS

• Monte Rosa plans to current a poster on the Digestive Illness Week (DDW) Convention on Might 21, 2024, in Washington, DC, titled, “MRT-6160, a VAV1-Directed Molecular Glue Degrader, Inhibits Illness Development in a T-cell Switch Mediated Murine Colitis Mannequin Concomitant with Diminished Calprotectin Expression.”
• Monte Rosa plans to current a poster on the European Alliance of Associations for Rheumatology (EULAR) Convention on June 14, 2024, in Vienna, Austria, titled, “MRT-6160, a VAV1-Directed Molecular Glue Degrader, Reduces Joint Irritation, Cytokine Manufacturing, and Autoantibody Ranges in a Collagen-Induced Arthritis Illness Mannequin.”

FIRST QUARTER 2024 FINANCIAL RESULTS

Collaboration Income: Collaboration income for the primary quarter of 2024 was $1.1 million, in contrast with $0 throughout the identical interval in 2023. Collaboration income represents income recorded below the Roche License and Collaboration settlement.

Analysis and Improvement (R&D) Bills: R&D bills for the primary quarter of 2024 had been $27.0 million, in comparison with $26.8 million throughout the identical interval in 2023. R&D bills had been pushed by the profitable achievement of key milestones in our R&D group, together with the continuation of the MRT-2359 scientific research, the development and development of our preclinical pipeline, the preparation of MRT-6160 to enter the clinic, and the continued growth of the Firm’s QuEEN™ discovery engine. Non-cash stock-based compensation constituted $2.7 million of R&D bills for Q1 2024, in comparison with $2.1 million in the identical interval in 2023.

Normal and Administrative (G&A) Bills: G&A bills for the primary quarter of 2024 had been $9.0 million in comparison with $7.5 million throughout the identical interval in 2023. The rise in G&A bills was a results of elevated headcount, stock-based compensation expense, and charges paid to consultants to be able to help our development and operations. G&A bills included non-cash stock-based compensation of $2.2 million for the primary quarter of 2024, in comparison with $1.8 million for a similar interval in 2022.

Web Loss: Web loss for the primary quarter of 2024 was $32.0 million, in comparison with $33.3 million for the fourth quarter of 2023.

Money Place and Monetary Steering: Money, money equivalents, restricted money, and marketable securities as of March 31, 2024, had been $197.8 million, in comparison with money, money equivalents, restricted money, and marketable securities of $237.0 million as of December 31, 2023. The lower of $39.2 million was primarily as a result of operational use of money.

The Firm expects its money and money equivalents to be ample to fund deliberate operations and capital expenditures into the primary half of 2026.

About MRT-2359
MRT-2359 is a potent, extremely selective, and orally bioavailable investigational molecular glue degrader (MGD) that induces the interplay between the E3 ubiquitin ligase element cereblon and the interpretation termination issue GSPT1, resulting in the focused degradation of GSPT1 protein. The MYC transcription elements (c‑MYC, L-MYC and N-MYC) are well-established drivers of human cancers that preserve excessive ranges of protein translation, which is vital for uncontrolled cell proliferation and tumor development. Preclinical research have proven this dependancy to MYC-induced protein translation creates a dependency on GSPT1. By inducing degradation of GSPT1, MRT-2359 is designed to take advantage of this vulnerability, disrupting the protein synthesis equipment, resulting in anti-tumor exercise in MYC-driven tumors.

About MRT-6160
MRT-6160 is a potent, extremely selective, and orally bioavailable investigational molecular glue degrader of VAV1, which in our in vitro research has proven deep degradation of its goal with no detectable results on different proteins. VAV1, a Rho-family guanine nucleotide alternate issue, is a key signaling protein downstream of each the T- and B-cell receptors. VAV1 expression is restricted to blood and immune cells, together with T and B cells. Preclinical research have proven that focused degradation of VAV1 protein by way of an MGD modulates each T- and B-cell receptor-mediated exercise. This modulation is clear each in vitro and in vivo, demonstrated by a big lower in cytokine secretion, proteins very important for sustaining autoimmune ailments. Furthermore, VAV1-directed MGDs have proven promising exercise in preclinical fashions of autoimmune ailments and thus have the potential to supply therapeutic advantages in a number of systemic and neurological autoimmune indications, equivalent to a number of sclerosis, rheumatoid arthritis, inflammatory bowel illness, and dermatological issues. Preclinical research have demonstrated that MRT-6160 can inhibit illness development in in vivo autoimmunity fashions.

About MRT-8102
MRT-8102 is a potent, extremely selective, and orally bioavailable investigational molecular glue degrader (MGD) that targets NEK7 for the therapy of inflammatory ailments pushed by IL-1β and the NLRP3 inflammasome. NEK7 has been proven to be required for NLRP3 inflammasome meeting, activation and IL-1β launch each in vitro and in vivo. Aberrant NLRP3 inflammasome activation and the following launch of energetic IL-1β and interleukin-18 (IL-18) has been implicated in a number of inflammatory issues, together with gout, heart problems, neurologic issues together with Parkinson’s illness and Alzheimer’s illness, ocular illness, diabetes, weight problems, and liver illness. In a non-human primate mannequin, MRT-8102 was proven to potently, selectively, and durably degrade NEK7, and resulted in near-complete reductions of IL-1β fashions following ex vivo stimulation of complete blood. MRT-8102 has proven a positive profile in non-GLP toxicology research.

About Monte Rosa
Monte Rosa Therapeutics is a clinical-stage biotechnology firm growing extremely selective molecular glue degrader (MGD) medicines for sufferers dwelling with critical ailments within the areas of oncology, autoimmune and inflammatory ailments, and extra. MGDs are small molecule protein degraders which have the potential to deal with many ailments that different modalities, together with different degraders, can not. Monte Rosa’s QuEEN™ (Quantitative and Engineered Elimination of Neosubstrates) discovery engine combines AI-guided chemistry, numerous chemical libraries, structural biology, and proteomics to establish degradable protein targets and rationally design MGDs with unprecedented selectivity. The QuEEN discovery engine allows entry to a wide-ranging and differentiated goal area of well-validated biology throughout a number of therapeutic areas. Monte Rosa has developed the trade’s main pipeline of MGDs, which spans oncology, autoimmune and inflammatory illness and past, and has a strategic collaboration with Roche to find and develop MGDs in opposition to targets in most cancers and neurological ailments beforehand thought-about not possible to drug. For extra info, go to www.monterosatx.com.

Ahead-Wanting Statements
This communication contains categorical and implied “forward-looking statements,” together with forward-looking statements throughout the which means of the Personal Securities Litigation Reform Act of 1995. Ahead-looking statements embody all statements that aren’t historic details and in some instances, will be recognized by phrases equivalent to “might,” “would possibly,” “will,” “may,” “would,” “ought to,” “count on,” “intend,” “plan,” “goal,” “anticipate,” “imagine,” “estimate,” “predict,” “potential,” “proceed,” “ongoing,” or the detrimental of those phrases, or different comparable terminology supposed to establish statements concerning the future. Ahead-looking statements contained herein embody, however usually are not restricted to, statements about our capability to develop our product pipeline, statements across the Firm’s QuEEN™ discovery engine and the Firm’s view of its potential to establish degradable protein targets and rationally design MGDs with unprecedented selectivity, statements across the energy and differentiation of the QuEEN discovery engine and the potential of the Firm’s MGDs in opposition to a broad spectrum of targets, statements concerning the development and timeline of our preclinical and scientific applications, pipeline and the varied merchandise therein, together with (i) our product growth actions, our ongoing scientific growth of MRT-2359, our expectations to announce the beneficial Part 2 dose later within the second quarter of 2024, the timing for our disclosure of any preliminary information from our Part 1 scientific trial of MRT-2359 within the second half of 2024, and our plans to provoke the Part 2 portion of the research earlier than year-end, (ii) the continued growth of MRT-6160, and the deliberate submission of an IND to the FDA for MRT-6160 within the second quarter of 2024, our expectations of timing for initiation of a Part 1 SAD/MAD research mid-2024 and the timing for our disclosure of Part 1 scientific information of MRT-6160 within the first quarter of 2025, in addition to our expectation to current further preclinical information in fashions of autoimmune and inflammatory ailments on the upcoming DDW and EULAR medical conferences and our expectation to provoke POC research for MRT-6160 in autoimmune/inflammatory ailments together with ulcerative colitis and rheumatoid arthritis, with further potential POC research, dermatology, rheumatology, and neurology indications in mid-2024, (iii) our ongoing growth of MRT-8102 and our expectations round its potential throughout neurologic indications and weight problems amongst others, in addition to potential use in gout, pericarditis, and different peripheral inflammatory circumstances, together with our expectations to submit an IND to the FDA within the first quarter of 2025, and (iv) our expectations to appoint a growth candidate for the CDK2 preclinical program in 2024, statements across the development and utility of our platform, and statements regarding our expectations concerning our capability to appoint and the timing of our nominations of further targets, product candidates, and growth candidates, statements concerning regulatory filings for our growth applications, together with the deliberate timing of such regulatory filings, equivalent to IND purposes, and potential overview by regulatory authorities in addition to our expectations of success for our applications and the power of our monetary place, our use of capital, bills and different monetary outcomes sooner or later, availability of funding for current applications, capability to fund operations into the primary half of 2026, amongst others. By their nature, these statements are topic to quite a few dangers and uncertainties, together with these dangers and uncertainties set forth in our most up-to-date Annual Report on Type 10-Okay for the yr ended December 31, 2023, filed with the U.S. Securities and Change Fee on March 14, 2024, and any subsequent filings, that might trigger precise outcomes, efficiency or achievement to vary materially and adversely from these anticipated or implied within the statements. You shouldn’t depend on forward-looking statements as predictions of future occasions. Though our administration believes that the expectations mirrored in our statements are cheap, we can not assure that the long run outcomes, efficiency, or occasions and circumstances described within the forward-looking statements can be achieved or happen. Recipients are cautioned to not place undue reliance on these forward-looking statements, which communicate solely as of the date such statements are made and shouldn’t be construed as statements of truth. We undertake no obligation to publicly replace any forward-looking statements, whether or not on account of new info, any future displays, or in any other case, besides as required by relevant regulation. Sure info contained in these supplies and any statements made orally throughout any presentation of those supplies that relate to the supplies or are based mostly on research, publications, surveys and different information obtained from third-party sources and our personal inside estimates and analysis. Whereas we imagine these third-party research, publications, surveys and different information to be dependable as of the date of those supplies, we’ve got not independently verified, and make no representations as to the adequacy, equity, accuracy or completeness of, any info obtained from third-party sources. As well as, no unbiased supply has evaluated the reasonableness or accuracy of our inside estimates or analysis and no reliance must be made on any info or statements made in these supplies regarding or based mostly on such inside estimates and analysis.

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