Pre-clinical data demonstrates first-in-class MERTK selective
inhibitor with novel mechanism of action
Rgenix has initiated IND-enabling studies of RGX-019
NEW YORK–(BUSINESS WIRE)–lt;a href="https://twitter.com/hashtag/biotech?src=hash" target="_blank"gt;#biotechlt;/agt;–Rgenix, Inc., a clinical stage biopharmaceutical company developing
first-in-class small molecule and antibody cancer therapeutics,
announced today it is presenting pre-clinical data from ongoing research
of RGX-019, a monoclonal antibody that targets MERTK, for the treatment
of advanced cancer. In a presentation of a late-breaking abstract, “Characterization
of the anti-cancer and immunologic activity of RGX-019, a novel
pre-clinical stage humanized monoclonal antibody targeting the MERTK
receptor,” which was accepted for the 2019 American Association of
Cancer Research Annual Meeting, Isabel Kurth Ph.D., Rgenix VP of
Research, discussed data showing RGX-019 to be a potent and selective
inhibitor of MERTK signaling, resulting in suppression of cancer growth
and activation of the innate immune response.
RGX-019 is a humanized monoclonal antibody that selectively targets
MERTK, a receptor tyrosine kinase of the TYRO3/AXL/MERTK (TAM) family.
MERTK is expressed in immune cells such as macrophages, dendritic cells
and NK cells, and is also overexpressed in a wide variety of liquid and
solid cancers.
Activation of MERTK on cancer cells via ligand binding activates several
tumor-promoting signaling pathways, stimulating tumor proliferation,
migration and angiogenesis, and decreasing apoptosis and
chemosensitivity. When activated on macrophages, MERTK promotes an
immune-suppressive M2 phenotype.
RGX-019 binds to human MERTK with high affinity and selectivity, without
detectible binding to other related TAM kinases. RGX-019 has a unique
mechanism of action that not only leads to blockade of ligand binding,
but also to MERTK degradation via receptor internalization.
This novel mechanism of action leads to inhibition of cancer growth in
vitro and in vivo as well as activation of M1
(pro-inflammatory) cytokine release from immune-suppressive M2
macrophages.
Masoud Tavazoie, MD, PhD, and Chief Executive Officer of Rgenix, said,
“We are excited to have an opportunity to reveal the pre-clinical data
that demonstrates the positive progress we are making with the
development of RGX-019, our third proprietary program. The ability of
RGX-019 to selectivity degrade MERTK in cancers cells and M2 macrophages
provides a distinct advantages over current small-molecule approaches to
targeting MERTK which are hampered by off-target binding to other
related kinases. This data provides a strong foundation for IND enabling
studies.”
Sohail Tavazoie, MD, PhD, and Chair of Rgenix’s Scientific Advisory
Board, said, “RGX-019 shows great potential as a cancer therapeutic and
its ability to selectively modulate both cancer growth and innate immune
activation is illustrative of that possibility. We look forward to
continuing our research on this antibody and its impact on various MERTK
expressing cancers.”
About Rgenix
Rgenix, Inc., is a privately-held clinical-stage biopharmaceutical
company focused on the discovery and development of novel cancer drugs
that target key pathways in cancer progression. The company is pursuing
several first-in-class drug candidates to treat cancers of high unmet
need. Rgenix identifies novel cancer targets using a microRNA based
target discovery platform originally developed by Rgenix’s scientific
co-founders at The Rockefeller University and now exclusively licensed
to Rgenix. The company brings together distinguished scientific
founders, a seasoned Board, and a leadership team comprised of
experienced drug developers. The company is funded by leading
biotechnology investors, including Novo Holdings A/S, Sofinnova
Partners, Lepu Holdings Limited, Oceanpine Capital, WuXi PharmaTech
Healthcare Fund I, LP, Alexandria Venture Investments,LLC, and the
Partnership Fund for New York City. For more information, please visit www.rgenix.com.
About RGX-019
RGX-019 is an investigational drug candidate and a humanized monoclonal
antibody that targets MERTK being developed by Rgenix for the treatment
of advanced cancer. Rgenix in-licensed RGX-019 related antibody
intellectual property from Rockefeller University as part of a
world-wide exclusive licensing agreement.
MERTK is a receptor tyrosine kinase of the TAM family and is
over-expressed in several human cancers. The MERTK pathway drives cancer
progression, tumor angiogenesis, and innate immune suppression.
Targeting MERTK inhibits the growth of MERTK-expressing cancer cells and
induces an M1 pro-inflammatory cytokine expression profile in
tumor-associated macrophages. Rgenix has initiated IND-enabling studies
of RGX-019.
Contacts
RooneyPartners
Marion Janic
212-223-4017
mjanic@rooneyco.com