Monte Rosa Therapeutics Advances Second Development Candidate, MRT-6160, a Novel, Highly Selective Molecular Glue Degrader Targeting VAV1 for the Treatment of Autoimmune Diseases
May 23 2023 - 7:30AM
Monte Rosa Therapeutics, Inc. (Nasdaq: GLUE), a clinical-stage
biotechnology company developing novel molecular glue degrader
(MGD)-based medicines, today announced its second development
candidate, MRT-6160, a novel, potent, and selective molecular glue
degrader (MGD) of VAV1. The Company plans to file an
Investigational New Drug (IND) application for MRT-6160 in the
first half of 2024 and to develop the molecule as a potential
treatment for autoimmune diseases.
“MRT-6160 is a potent, orally bioavailable MGD designed to
degrade VAV1, an important protein involved in the signaling
pathways of T and B cells. Our in vitro studies have shown that
MRT-6160 selectively degrades VAV1 without detectable effects on
other proteins. By targeting VAV1, MRT-6160 attenuates multiple
aspects of T- and B-cell function and inhibits disease progression
in established in vivo models of autoimmunity,” said Owen Wallace,
Ph.D., Chief Scientific Officer of Monte Rosa. “The underlying
biology and our preclinical data both demonstrate that MRT-6160
acts as an immune modulator, which has the potential to avoid the
broad immune suppression seen with other approaches. We look
forward to progressing our clinical plan developed with the goal of
providing early insights into safety, PK and PD, and proof of
concept regarding differentiated effects on key immunomodulatory
signaling pathways.”
“Our goal centers on pioneering therapeutically meaningful new
drugs for patients with serious diseases. By addressing VAV1, a
validated but previously undruggable target, we believe we've
created a potentially groundbreaking therapy for patients suffering
from a range of serious autoimmune conditions, particularly those
involving both T- and B cell-mediated autoimmunity,” said Markus
Warmuth, M.D., CEO of Monte Rosa. “MRT-6160 is expected to be our
second MGD to enter clinical trials, showcasing the continued
productivity of our QuEEN™ platform. We anticipate significant
progress and milestones in our portfolio in the upcoming year,
including initial clinical data from our GSPT1 MGD, MRT-2359, in
the second half of this year and filing of an IND application for
MRT-6160 in the first half of next year.”
About VAV1 and MRT-6160VAV1, a Rho-family
guanine nucleotide exchange factor, is a key signaling protein
downstream of both the T-and B-cell receptors. VAV1 expression is
restricted to blood and immune cells, including T and B cells.
Preclinical studies have shown that targeted degradation of VAV1
protein via an MGD modulates both T- and B-cell receptor-mediated
activity. This modulation is evident both in vitro and in vivo,
demonstrated by a significant decrease in cytokine secretion,
proteins vital for maintaining autoimmune diseases. Moreover,
VAV1-directed MGDs have shown promising activity in preclinical
models of autoimmune diseases and thus we believe have the
potential to provide therapeutic benefits in multiple autoimmune
indications, such as multiple sclerosis, rheumatoid arthritis, and
dermatological disorders. MRT-6160 is a potent, highly selective,
and orally bioavailable degrader of VAV1, which has shown deep
degradation of its target with no detectable effects on other
proteins. Preclinical studies demonstrate MRT-6160 inhibits disease
progression in in vivo autoimmunity models.
About Monte RosaMonte Rosa Therapeutics is a
biotechnology company developing novel molecular glue degrader
(MGD) medicines for patients with serious diseases such as
oncology, autoimmune and inflammatory diseases. MGDs are small
molecule protein degraders that employ the body’s natural
mechanisms to selectively eliminate therapeutically relevant
proteins. The Company’s QuEEN™ (Quantitative and Engineered
Elimination of Neosubstrates) platform enables it to rapidly
identify protein targets and design highly selective degraders by
combining diverse libraries of proprietary MGDs with in-house
proteomics, structural biology, AI/machine learning, and
computational chemistry capabilities. For more information,
visit www.monterosatx.com
Forward-Looking StatementsThis communication
includes express and implied “forward-looking statements,”
including forward-looking statements within the meaning of the
Private Securities Litigation Reform Act of 1995. Forward-looking
statements include all statements that are not historical facts,
and in some cases, can be identified by terms such as “may,”
“might,” “will,” “could,” “would,” “should,” “expect,” “intend,”
“plan,” “objective,” “anticipate,” “believe,” “estimate,”
“predict,” “potential,” “continue,” “ongoing,” or the negative of
these terms, or other comparable terminology intended to identify
statements about the future. Forward-looking statements contained
in herein include, but are not limited to, statements about our
product development activities, including our expectations around
the potential of molecular glue degraders, the potential of our
pipeline of molecular glue degraders, including our molecular glue
degrader for VAV1, known as MRT-6160, GSPT1, known as MRT-2159,
NEK7, and CDK2, and our earlier stage, undisclosed molecular glue
degraders, our expectations regarding the advancement, and timing
thereof, of our pipeline and the various products therein, our
ability to advance our development candidates, including MRT-6160,
toward IND, our ability to initiate and the timing of initiation of
additional lead optimization programs, and our expectations
regarding our ability to nominate and the timing of our nominations
of additional development candidates, our expectations regarding
potential therapeutic opportunities for our molecular glue
degraders, and our clinical development expectations therefor, our
expectations regarding patient populations and medical needs for
any potential therapeutic opportunities for our molecular glue
degraders, our expectations for our ongoing clinical trial for
MRT-2359 and the timing thereof, our expectations regarding our
proprietary QuEEN™ platform and its potential for the discovery of
product candidates, and the strength of our financial position,
among others. By their nature, these statements are subject to
numerous risks and uncertainties, including those risks and
uncertainties set forth in our most recent Annual Report on Form
10-K for the year ended December 31, 2022, filed with the U.S.
Securities and Exchange Commission on March 16, 2023, and any
subsequent filings, that could cause actual results, performance or
achievement to differ materially and adversely from those
anticipated or implied in the statements. You should not rely upon
forward-looking statements as predictions of future events.
Although our management believes that the expectations reflected in
our statements are reasonable, we cannot guarantee that the future
results, performance, or events and circumstances described in the
forward-looking statements will be achieved or occur. Recipients
are cautioned not to place undue reliance on these forward-looking
statements, which speak only as of the date such statements are
made and should not be construed as statements of fact. We
undertake no obligation to publicly update any forward-looking
statements, whether as a result of new information, any future
presentations, or otherwise, except as required by applicable
law.
Investors Shai Biran Monte Rosa Therapeutics
ir@monterosatx.com
Media Cory Tromblee, Scient
PRmedia@monterosatx.com
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