Olema Oncology KAT6 Inhibitor Compounds Demonstrate Potent Anti-Tumor Activity
12 Outubro 2023 - 8:01AM
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 new preclinical data regarding
the discovery of novel compounds targeting KAT6, an epigenetic
target that is dysregulated in breast and other cancers. These data
will be presented today at a poster session at the 2023
AACR-NCI-EORTC International Conference on Molecular Targets and
Cancer Therapeutics (ANE 2023) in Boston,
Massachusetts.
The poster, titled “The discovery of potent KAT6 inhibitors that
demonstrate anti-tumor activity in preclinical models of ER+ breast
cancer”, describes the discovery and preclinical characterization
of orally bioavailable, potent KAT6A and KAT6B-selective inhibitors
developed by Olema in collaboration with Aurigene Oncology. The
poster highlights that:
- Olema KAT6 compounds were selective
and potent against KAT6A and KAT6B (<20 nM IC50) with
>250-fold selectivity over other KAT family members, including
the essential genes KAT5 and KAT8.
- In KAT6-amplified and overexpressing
breast cancer cell lines, Olema KAT6 compounds strongly inhibited
cell proliferation whereas KAT6-low cell lines were insensitive to
the compounds.
- Olema KAT6 inhibitor compounds
caused dose-dependent tumor growth inhibition and tumor regression
comparable to or better than a positive-control patented KAT6
inhibitor.
- Olema KAT6 inhibitor compounds are
orally bioavailable with desirable pharmacokinetics.
- Olema KAT6 inhibitor compounds
demonstrate histone target engagement and efficacy, as well as
synergism with palbociclib or palazestrant (OP-1250).
“The dysregulation of KAT6 activity is observed across breast
and other cancers, and inhibition of the KAT6 histone
acetyltransferase enzyme reduces breast cancer cell proliferation
through downregulation of genes involved in estrogen receptor
signaling and other signaling pathways,” said David C. Myles,
Ph.D., Chief Discovery and Non-Clinical Development Officer of
Olema Oncology. “As noted in our poster today, the KAT6 inhibitors
we are developing have demonstrated attractive potency and
selectivity at inhibiting KAT6-amplified estrogen-receptor-positive
(ER+) breast cancer cells, both wild-type and ESR1 mutated.
Additionally, the compounds demonstrated synergistic activity in
combination with CDK4/6 inhibitors and endocrine agents such as
palazestrant (OP-1250).”
Olema’s KAT6 program has been developed in collaboration with
Aurigene Oncology. A copy of the poster is available on Olema’s
website under the Science section.
About Olema OncologyOlema Oncology is a
clinical-stage biopharmaceutical company focused on the discovery,
development and commercialization of targeted therapies for women’s
cancers. Olema’s lead product candidate, palazestrant (OP-1250), is
a proprietary, orally-available small molecule with dual activity
as both a complete estrogen receptor (ER) antagonist (CERAN) and a
selective ER degrader (SERD). It is currently being evaluated both
as a single agent in an ongoing Phase 2 clinical trial, and in
combination with CDK4/6 inhibitors (palbociclib and ribociclib) and
a PI3Ka inhibitor (alpelisib), in patients with recurrent, locally
advanced or metastatic ER-positive (ER+), human epidermal growth
factor receptor 2-negative (HER2-) breast cancer. Palazestrant has
been granted 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. Olema is headquartered in
San Francisco and has operations in Cambridge, Massachusetts. For
more information, please visit us at www.olema.com, or follow us on
Twitter and LinkedIn.
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 its KAT6 inhibitor
compounds and its applicability to breast and other cancers, and
the potential synergistic activity of Olema’s KAT6 inhibitor
compounds with CDK4/6 inhibitors or palazestrant (OP-1250). 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 June 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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