CDK12 Inhibitor Demonstrates Strong Anti-Tumor
Activity as Single Agent and in Combination with a DNA Damaging
Agent and a PARP Inhibitor in Models of Breast, Lung, and Ovarian
Cancer
On Track to Nominate CDK12 Inhibitor as Next
Development Candidate in 2H 2022
Syros Pharmaceuticals (NASDAQ:SYRS), a leader in the development
of medicines that control the expression of genes, today announced
new preclinical data from our CDK12 inhibitor program,
demonstrating robust anti-tumor activity of our oral, selective
CDK12 inhibitors in models of breast, lung, and ovarian cancer,
including in a PARP inhibitor resistant model. The data support the
advancement of a development candidate from Syros’ CDK12 inhibitor
program towards clinical development. These findings were presented
in an e-poster as part of the American Association for Cancer
Research (AACR) Annual Meeting 2022.
“CDK12 is an attractive cancer target due to its role in
transcription and DNA damage repair regulation. Leveraging our
selective CDK inhibition expertise, we discovered potent,
selective, and oral CDK12 inhibitors, which affect the expression
of genes involved in DNA damage response to drive anti-tumor
activity,” said Eric R. Olson, Ph.D., Chief Scientific Officer of
Syros. “Based on the promising new data presented at AACR, in which
CDK12 inhibition induced strong tumor growth inhibition and
demonstrated synergies in combination with existing standard of
care approaches, we believe a CDK12 inhibitor has the potential to
play a key role in breast, lung, and ovarian cancer treatment. We
look forward to nominating our next development candidate from our
CDK12 program in the second half of this year, as we aim to address
a significant unmet need for patients, including those who are
resistant to DNA damaging agents or PARP inhibitors.”
Preclinical Data from Oral CDK12 Inhibitor Program
Syros designed a series of CDK12 inhibitors that were profiled
in biochemical and cellular assays. The data presented at AACR
detail for the first time the potency, selectivity, and anti-tumor
activity from a representative member of the class, which exhibited
low nanomolar potency and selectivity over CDK2, CDK7, and CDK9 of
46-, 27-, and 9-fold, respectively.
As a single agent in cancer cell models, this CDK12 inhibitor
induced DNA damage, cell cycle dysregulation and genomic
instability leading to growth inhibition and apoptosis.
Additionally, as a single agent in in vivo cancer models this CDK12
inhibitor demonstrated tumor regressions in small cell lung cancer
and breast cancer models, at well tolerated doses.
In combination in vitro, this CDK12 inhibitor showed synergistic
or additive antiproliferative effects in combination with the DNA
damaging agent, lurbinectedin, and the PARP inhibitor, olaparib,
with increases in DNA damage and impaired DNA damage repair. In
vivo, CDK12 inhibition in combination with lurbinectedin showed
enhanced anti-tumor activity in a cell line derived model of small
cell lung cancer, and in combination with olaparib showed enhanced
anti-tumor activity in a PARP inhibitor resistant patient-derived
model (PDX) of ovarian cancer.
The poster is now available on the Publications and Abstracts
section of the Syros website at www.syros.com.
About Syros Pharmaceuticals
Syros is redefining the power of small molecules to control the
expression of genes. Based on its unique ability to elucidate
regulatory regions of the genome, Syros aims to develop medicines
that provide a profound benefit for patients with diseases that
have eluded other genomics-based approaches. Syros is advancing a
robust clinical-stage pipeline, including: tamibarotene, a
first-in-class oral selective RARα agonist in RARA-positive
patients with higher-risk myelodysplastic syndrome and acute
myeloid leukemia; SY-2101, a novel oral form of arsenic trioxide in
patients with acute promyelocytic leukemia; and SY-5609, a highly
selective and potent oral CDK7 inhibitor in patients with select
solid tumors and blood cancers. Syros also has multiple preclinical
and discovery programs in oncology and monogenic diseases. For more
information, visit www.syros.com and follow us on Twitter
(@SyrosPharma) and LinkedIn.
Cautionary Note Regarding Forward-Looking Statements
This press release contains forward-looking statements within
the meaning of The Private Securities Litigation Reform Act of
1995, including without limitation statements regarding the ability
to nominate a development candidate from Syros’ CDK12 inhibitor
program and the timing thereof, and the role of CDK12 inhibition in
breast, lung, and ovarian cancer treatment. The words
‘‘anticipate,’’ ‘‘believe,’’ ‘‘continue,’’ ‘‘could,’’ ‘‘estimate,’’
‘‘expect,’’ “hope,” ‘‘intend,’’ ‘‘may,’’ ‘‘plan,’’ ‘‘potential,’’
‘‘predict,’’ ‘‘project,’’ ‘‘target,’’ ‘‘should,’’ ‘‘would,’’ and
similar expressions are intended to identify forward-looking
statements, although not all forward-looking statements contain
these identifying words. Actual results or events could differ
materially from the plans, intentions and expectations disclosed in
these forward-looking statements as a result of various important
factors, including Syros’ ability to: advance the development of
its CDK12 program under the timelines it projects; demonstrate in
any current and future clinical trials the requisite safety,
efficacy and combinability of its drug candidates; replicate the
results seen in preclinical studies in human clinical trials;
obtain and maintain patent protection for its drug candidates and
the freedom to operate under third party intellectual property;
obtain and maintain necessary regulatory approvals; identify, enter
into and maintain collaboration agreements with third parties;
manage competition; manage expenses; raise the substantial
additional capital needed to achieve its business objectives;
attract and retain qualified personnel; and successfully execute on
its business strategies; risks described under the caption “Risk
Factors” in Syros’ Annual Report on Form 10-K for the year ended
December 31, 2021 which is on file with the Securities and Exchange
Commission; and risks described in other filings that Syros makes
with the Securities and Exchange Commission in the future. In
addition, the extent to which the COVID-19 pandemic continues to
impact Syros’ workforce and its clinical trial operations
activities, and the operations of the third parties on which Syros
relies, will depend on future developments, which are highly
uncertain and cannot be predicted with confidence, including the
duration and severity of the pandemic, additional or modified
government actions, and the actions that may be required to contain
the virus or treat its impact. Any forward-looking statements
contained in this press release speak only as of the date hereof,
and Syros expressly disclaims any obligation to update any
forward-looking statements, whether because of new information,
future events or otherwise.
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version on businesswire.com: https://www.businesswire.com/news/home/20220408005014/en/
Media Contact Courtney Solberg Syros Pharmaceuticals
917-698-9253 csolberg@syros.com Investor Contact Hannah
Deresiewicz Stern Investor Relations, Inc. 212-362-1200
hannah.deresiewicz@sternir.com
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