Zentalis Pharmaceuticals to Present Preclinical Azenosertib Data at ESMO 2024
September 09 2024 - 7:00AM
Zentalis® Pharmaceuticals, Inc. (Nasdaq: ZNTL), a clinical-stage
biopharmaceutical company discovering and developing clinically
differentiated small molecule therapeutics targeting fundamental
biological pathways of cancers, today announced that the company
will present preclinical data from its selective WEE1 inhibitor
azenosertib at the European Society of Medical Oncology (ESMO) 2024
Congress, occurring September 13-17 in Barcelona, Spain.
“The confluence of DNA damage induced by TOP1 inhibitors and
cell cycle deregulation and genomic instability induced by
azenosertib provides a mechanistic rationale for this combination,
as well as more broadly with antibody drug conjugates (ADCs)
utilizing these inhibitors as payloads,” said Mark Lackner, PhD,
Chief Scientific Officer. “The preclinical data demonstrated this
synergistic effect and suggest that azenosertib in combination with
ADCs could be an important therapeutic approach in treating
patients with advanced solid tumors.”
Presentation Details:Poster
#35P: The Selective WEE1 Inhibitor Azenosertib Shows
Synergistic Antitumor Effects in Combination with Topoisomerase I
Inhibitor-Based Antibody-Drug ConjugatesPresenter:
Jianhui Ma, Zentalis Pharmaceuticals Poster Display
Date: Sunday, September 15, 2024
Data in the abstract showed that the combination of azenosertib
with TOP1 inhibitors demonstrated significant synergistic effects
in all cell lines tested. In HER2+ breast cancer animal models,
those treated with the combination of azenosertib plus trastuzumab
deruxtecan (T-Dxd) resulted in 50% of animals showing complete
tumor regression (CR), compared with no CRs in monotherapy arms.
Significant combination effects were also observed in a HER2+
ovarian model and a HER2-low breast cancer model. These data
suggest that azenosertib significantly improves the anti-tumor
effect of TOP1 inhibitors as well as ADCs with TOP1 inhibitor
payload and that the combination could be a generalizable
therapeutic approach for improving responses to ADCs in patients
with advanced solid tumors.
About AzenosertibAzenosertib is a novel,
selective, and orally bioavailable inhibitor of WEE1 currently
being evaluated as a monotherapy and combination clinical studies
in ovarian cancer and additional tumor types. WEE1 acts as a master
regulator of the G1-S and G2-M cell cycle checkpoints, through
negative regulation of both CDK1 and CDK2, to prevent replication
of cells with damaged DNA. By inhibiting WEE1, azenosertib enables
cell cycle progression, despite high levels of DNA damage, thereby
resulting in the accumulation of DNA damage and leading to mitotic
catastrophe and cancer cell death.
About Zentalis Pharmaceuticals
Zentalis® Pharmaceuticals, Inc. is a clinical-stage
biopharmaceutical company discovering and developing clinically
differentiated small molecule therapeutics targeting fundamental
biological pathways of cancers. The Company’s lead product
candidate, azenosertib (ZN-c3), is a potentially first-in-class and
best-in-class WEE1 inhibitor for advanced solid tumors and
hematologic malignancies. Azenosertib is being evaluated as a
monotherapy and in combination across multiple clinical trials and
has broad franchise potential. In clinical trials, azenosertib has
been well tolerated and has demonstrated anti-tumor activity as a
single agent across multiple tumor types and in combination with
several chemotherapy backbones. As part of its azenosertib clinical
development program, the Company is exploring enrichment strategies
targeting tumors of high genomic instability, such as Cyclin E1
positive tumors, homologous recombination deficient tumors and
tumors with oncogenic driver mutations. The Company is also
leveraging its extensive experience and capabilities across cancer
biology and medicinal chemistry to advance its research on protein
degraders. Zentalis has operations in San Diego.
For more information, please visit www.zentalis.com. Follow
Zentalis on X/Twitter at @ZentalisP and on LinkedIn
at www.linkedin.com/company/zentalis-pharmaceuticals.
Forward-Looking StatementsThis press release
contains forward-looking statements within the meaning of the U.S.
Private Securities Litigation Reform Act of 1995. All statements
contained in this press release that do not relate to matters of
historical fact should be considered forward-looking statements,
including statements regarding the potential benefits of
azenosertib in combination with ADCs as a therapeutic approach. The
terms “could” and similar references are intended to identify
forward-looking statements, although not all forward-looking
statements contain these identifying words. These statements are
neither promises nor guarantees, but involve known and unknown
risks, uncertainties and other important factors that may cause our
actual results, performance or achievements to be materially
different from any future results, performance or achievements
expressed or implied by the forward-looking statements, including,
but not limited to, the following: our ability to resolve the
ongoing partial clinical hold on azenosertib; our limited operating
history, which may make it difficult to evaluate our current
business and predict our future success and viability; we have and
expect to continue to incur significant losses; our need for
additional funding, which may not be available; our plans,
including the costs thereof, of development of any diagnostic
tools; our substantial dependence on the success of our lead
product candidate, azenosertib; the outcome of preclinical testing
and early trials may not be predictive of the success of later
clinical trials; failure to identify additional product candidates
and develop or commercialize marketable products; potential
unforeseen events during clinical trials could cause delays or
other adverse consequences; risks relating to the regulatory
approval process or ongoing regulatory obligations; failure to
obtain U.S. or international marketing approval; our product
candidates may cause serious adverse side effects; inability to
maintain our collaborations, or the failure of these
collaborations; our reliance on third parties; effects of
significant competition; the possibility of system failures or
security breaches; risks relating to intellectual property; our
ability to attract, retain and motivate qualified personnel, and
risks relating to management transitions; significant costs as a
result of operating as a public company; and the other important
factors discussed under the caption “Risk Factors” in our most
recently filed periodic report on Form 10-K or 10-Q and subsequent
filings with the U.S. Securities and Exchange Commission (SEC) and
our other filings with the SEC. Any such forward-looking statements
represent management’s estimates as of the date of this press
release. While we may elect to update such forward-looking
statements at some point in the future, we disclaim any obligation
to do so, even if subsequent events cause our views to change.
ZENTALIS® and its associated logo are trademarks of Zentalis
and/or its affiliates. All website addresses and other links in
this press release are for information only and are not intended to
be an active link or to incorporate any website or other
information into this press release.
Contact:Elizabeth Pingpank
Hickinehickin@zentalis.com860-463-0469
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