Kura Oncology Presents Preclinical Data on KO-947 and Menin-MLL Inhibitor Program at the EORTC-NCI-AACR Symposium on Molecula...
December 01 2016 - 07:30AM
Kura Oncology, Inc. (Nasdaq:KURA), a clinical stage
biopharmaceutical company, today presented preclinical data
highlighting the identification and characterization of KO-947, its
development candidate targeting ERK1/2 kinases. The company has
also presented preclinical data relating to the identification and
optimization of potent and selective inhibitors of the menin-MLL
interaction. Both presentations took place at the EORTC-NCI-AACR
Symposium on Molecular Targets and Cancer Therapeutics (EORTC) in
Munich, Germany.
“We are excited to present preclinical data from these two
innovative programs at EORTC, both of which showed compelling
activity in preclinical models of cancer,” said Yi Liu, Ph.D.,
Chief Scientific Officer. “Looking forward, we anticipate
nominating a development candidate for our menin-MLL program by the
end of 2016, and initiating a Phase 1 clinical trial for KO-947 in
the first half of 2017.”
KO-947 - A potent and selective inhibitor of ERK1/2
kinases
The RAS/RAF/MEK pathway is estimated to be activated in more
than 30% of human cancers, including cancers arising from mutations
in KRAS, NRAS and BRAF. Although inhibitors of both BRAF and MEK
have been approved for treatment of melanoma, acquired resistance
to these inhibitors has been documented both in preclinical and
clinical samples due to reactivation of ERK1/2 kinases.
In preclinical studies presented today at EORTC, KO-947 showed
potent inhibition of ERK signaling pathways and proliferation of
tumor cells exhibiting dysregulation of MAPK pathway, including
mutations in BRAF, NRAS or KRAS. KO-947 also inhibits MAPK
signaling and cell proliferation in preclinical models that are
resistant to BRAF and MEK inhibitors. Results obtained from
screening a large panel of PDX models demonstrate that KO-947
induces tumor regressions in BRAF or RAS mutated tumor models as
well as in tumor models lacking BRAF/RAS mutations but
characterized by other dysregulation of the MAPK pathway.
KO-947 appears to be differentiated from other published ERK
inhibitors by an extended residence time and prolonged pathway
inhibition in vitro and in vivo. The data further suggest that the
drug properties of KO-947 may allow Kura to maximize the
therapeutic window with flexible administration routes and
schedules, including intermittent dosing.
Inhibitors of the Menin-MLL Interaction
Chromosomal translocations that affect the mixed lineage
leukemia (MLL) gene result in aggressive acute myeloid and lymphoid
leukemias that are often resistant to standard chemotherapy.
Approximately 5-10% of acute leukemias in adults, and 70% of acute
leukemias in infants, are characterized by tumors with abnormal MLL
fusions. MLL fusion proteins require menin for leukemogenic
activity and selective disruption of the menin-MLL interaction
represents a potential therapeutic approach for the treatment of
acute leukemias with MLL rearrangements.
In preclinical studies presented at EORTC, inhibitors of the
menin-MLL interaction showed potent inhibition of the proliferation
of MLL leukemic cells. Inhibitors of the menin-MLL interaction
displayed a greater than 50-fold reduction in potency in
non-MLL-fusion leukemia cell lines and induced regression in a
MV4:11 mouse xenograft model. The data show that the anti-tumor
activity of menin-MLL inhibitors correlates with target engagement
in tumors as well as inhibition of expression of downstream genes
under the regulation of the fusion protein. Moreover, the
inhibitors demonstrated potent efficacy in subcutaneous and
disseminated models of MLL-fusion leukemias.
Both of the posters presented at EORTC can be found on Kura’s
website in the Scientific Presentations and Papers section or by
clicking here.
About Kura Oncology
Kura Oncology is a clinical-stage biopharmaceutical company
committed to realizing the promise of precision medicines for the
treatment of cancer. The company’s pipeline consists of small
molecules that target cancer signaling pathways where there is a
strong scientific and clinical rationale to improve outcomes by
identifying those patients most likely to benefit from treatment.
Kura Oncology’s lead drug candidate is tipifarnib, a farnesyl
transferase inhibitor, which is currently being studied in multiple
Phase 2 clinical trials. The preclinical pipeline includes KO-947,
an ERK inhibitor, and a menin-MLL program. For additional
information about Kura Oncology, please visit the company’s website
at www.kuraoncology.com.
Forward Looking Statements
This news release contains certain forward-looking statements
that involve risks and uncertainties that could cause actual
results to be materially different from historical results or from
any future results expressed or implied by such forward-looking
statements. Such forward-looking statements include statements
regarding, among other things, the potential utility KO-947 and
Kura Oncology’s other compounds and product candidates, the
conduct, results and timing of preclinical studies and clinical
trials and plans regarding future research and development. Factors
that may cause actual results to differ materially include the risk
that compounds that appeared promising in early research or
clinical trials do not demonstrate safety and/or efficacy in later
preclinical studies or clinical trials, the risk that Kura Oncology
may not obtain approval to market its product candidates,
uncertainties associated with regulatory filings and applications,
the risks associated with reliance on outside financing to meet
capital requirements, and the risks associated with reliance on
collaborative partners for further research, clinical trials,
development and commercialization of product candidates. You are
urged to consider statements that include the words “may,” “will,”
“would,” “could,” “should,” “believes,” “estimates,” “projects,”
“promise,” “potential,” “expects,” “plans,” “anticipates,”
“intends,” “continues,” “designed,” “goal,” or the negative of
those words or other comparable words to be uncertain and
forward-looking. For a further list and description of the risks
and uncertainties the Company faces, please refer to the Company's
periodic and other filings with the Securities and Exchange
Commission, which are available at www.sec.gov. Such
forward-looking statements are current only as of the date they are
made, and Kura Oncology assumes no obligation to update any
forward-looking statements, whether as a result of new information,
future events or otherwise.
CONTACT INFORMATION
INVESTOR CONTACT:
Robert H. Uhl
Managing Director
Westwicke Partners, LLC
(858) 356-5932
robert.uhl@westwicke.com
MEDIA CONTACT:
Mark Corbae
Vice President
Canale Communications
(619) 849-5375
mark@canalecomm.com
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