Olema Oncology Announces Publication of Data Highlighting Palazestrant’s Ability to Inhibit Wild-Type and Mutant ER+ Breast Cancer Both as Monotherapy and in Combination with CDK4/6 Inhibitors
06 Mars 2024 - 1:03PM
Olema Pharmaceuticals, Inc. (“Olema” or “Olema Oncology,” Nasdaq:
OLMA), a clinical-stage biopharmaceutical company focused on the
discovery, development and commercialization of targeted therapies
for women’s cancers, today announced that Molecular Cancer
Therapeutics, an American Association for Cancer Research journal,
has selected as a featured article a data publication that
describes the distinct properties of palazestrant (OP-1250). The
paper, titled “Palazestrant (OP-1250), a Complete Estrogen Receptor
Antagonist, Inhibits Wild-type and Mutant ER-positive Breast Cancer
Models as Monotherapy and in Combination”, describes the scientific
background underlying the design, discovery and optimization of
palazestrant.
“The research described in this paper reviews the deliberate
design and processes used in discovering and optimizing
palazestrant as a molecule purpose-built to address a crucial unmet
need in the treatment of women’s cancers, and we are delighted that
Molecular Cancer Therapeutics has featured our work,” said David C.
Myles, Ph.D., Olema’s Chief Discovery and Non-Clinical Development
Officer. “What’s even more exciting is to see how faithfully the
pre-clinical research predicted the behavior of palazestrant now
that it is in late-stage clinical development. We saw the potential
then, as told in the paper, and we believe that every day brings us
closer to having a real impact transforming the treatment paradigm
for women with cancer.”
As part of the discovery and optimization process, palazestrant
was assessed across an extensive series of biochemical, cell
culture, and in vivo assays comparing it with other antiestrogens
and compounds that are either approved for use by the FDA or are
currently in clinical development, including aromatase inhibitors,
selective ER modulators (SERMs), traditional SERDs, and
proteolysis-targeting chimeras (PROTACs). As a CERAN, palazestrant
has a distinct mechanism of action (MOA), and though it actively
degrades the ER, the paper shows that degradation alone is not a
reliable mechanism to drive the efficacy of an endocrine agent. In
mouse xenograft models, palazestrant demonstrated excellent
pharmacokinetics, was well tolerated, showed synergy with CDK4/6
inhibitors, and was highly effective at reducing tumor growth in
both wild-type and ESR1-mutant ER+ breast cancer. In addition, in
an ESR1-mutant intercranial xenograft model, palazestrant inhibited
tumor growth and improved survival of animals with CNS metastases,
even after stopping drug treatment.
The paper can be accessed in the latest print edition of
Molecular Cancer Therapeutics or online at
https://aacrjournals.org/mct/article/doi/10.1158/1535-7163.MCT-23-0351/731746/Palazestrant-OP-1250-a-Complete-Estrogen-Receptor.
About Palazestrant (OP-1250)
Palazestrant (OP-1250) is a novel, orally-available small
molecule with dual activity as both a complete estrogen receptor
(ER) antagonist (CERAN) and selective ER degrader (SERD). It is
currently being investigated in patients with recurrent, locally
advanced or metastatic ER-positive (ER+), human epidermal growth
factor receptor 2-negative (HER2-) breast cancer. In clinical
studies, palazestrant completely blocks ER-driven transcriptional
activity in both wild-type and mutant forms of metastatic ER+
breast cancer and has demonstrated anti-tumor efficacy along with
attractive pharmacokinetics and exposure, favorable tolerability,
CNS penetration, and combinability with CDK4/6 inhibitors.
Palazestrant has been granted U.S. Food and Drug Administration
(FDA) Fast Track designation for the treatment of ER+/HER2-
metastatic breast cancer that has progressed following one or more
lines of endocrine therapy with at least one line given in
combination with a CDK4/6 inhibitor. It is currently being
evaluated both as a single agent in an ongoing Phase 3 clinical
trial, OPERA-01, and in Phase 2 combination studies with CDK4/6
inhibitors (palbociclib and ribociclib) and a PI3Ka inhibitor
(alpelisib). For more information, please visit
www.opera01study.com.
About Olema Oncology
Olema Oncology is a clinical-stage biopharmaceutical company
committed to transforming the standard of care and improving
outcomes for women living with cancer. Olema is advancing a
pipeline of novel therapies by leveraging our deep understanding of
endocrine-driven cancers, nuclear receptors, and mechanisms of
acquired resistance. In addition to our lead product candidate,
palazestrant (OP-1250), a proprietary, orally-available complete
estrogen receptor (ER) antagonist (CERAN) and a selective ER
degrader (SERD), Olema is developing a potent KAT6 inhibitor. Olema
is headquartered in San Francisco and has operations in Cambridge,
Massachusetts. For more information, please visit us
at www.olema.com.
Forward Looking Statements
Statements contained in this press release regarding matters
that are not historical facts are “forward-looking statements”
within the meaning of Section 27A of the Securities Act of 1933 and
Section 21E of the Securities Exchange Act of 1934. Words such as
“anticipate,” “expect,” “will,” “may,” “goal,” “potential” and
similar expressions (as well as other words or expressions
referencing future events, conditions or circumstances) are
intended to identify forward-looking statements. These statements
include those related to Olema’s preclinical program, including the
potential beneficial characteristics of palazestrant (OP-1250),
both as a monotherapy and in combination with CDK4/6 inhibitors,
palazestrant’s potential to address to address an unmet need in the
treatment of women’s cancers, and palazestrant’s ability to
transform the treatment paradigm for women with cancer. Because
such statements deal with future events and are based on Olema’s
current expectations, they are subject to various risks and
uncertainties, and actual results, performance or achievements of
Olema could differ materially from those described in or implied by
the statements in this press release. These forward-looking
statements are subject to risks and uncertainties, including,
without limitation, those discussed in the section titled “Risk
Factors” in Olema’s Quarterly Report on Form 10-Q for the quarter
ended September 30, 2023, and future filings and reports that Olema
makes from time to time with the U.S. Securities and Exchange
Commission. Except as required by law, Olema assumes no obligation
to update these forward-looking statements, including in the event
that actual results differ materially from those anticipated in the
forward-looking statements.
Contact:Geoffrey Mogilner, Vice President, Investor Relations
and Communicationsir@olema.com
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