Qualigen Therapeutics Announces Four Posters on QN-302 Presented at the American Association of Cancer Research (AACR) 2023 Annual Meeting in Orlando, FL
18 Abril 2023 - 9:45AM
Qualigen Therapeutics, Inc. (“Qualigen” or “the Company,” Nasdaq:
QLGN), a diversified life sciences company focused on developing
treatments for adult and pediatric cancers with potential for
Orphan Drug Designation, while also commercializing diagnostics,
today announces data from the Company’s four posters regarding its’
lead program, QN-302, was presented at the American Association for
Cancer Research (AACR) Annual Meeting 2023 held April 14-19 in
Orlando, FL.
“These data corroborate our approach in
utilizing QN-302 as a potential treatment for pancreatic cancer, as
they provide significant and encouraging understanding of how the
compound interacts with in vitro and in vivo PDAC models,”
commented Dr. Tariq Arshad, Qualigen’s Chief Medical Officer. “We
continue to be on track to complete our preparations for submitting
an Investigational New Drug (IND) package to the FDA with the goal
to proceed to Phase 1 trials with QN-302, and we believe these data
will play an integral role in that regard toward becoming a
clinical stage company.”
The Annual AACR Conference is a focal point of
the cancer research community, where scientists, clinicians, other
health care professionals, survivors, patients, and advocates
gather to share the latest advances in cancer science and
medicine.
Highlights from QN-302
Posters
Abstract #390 - “A
comparison of the activity of the quadruplex-targeting experimental
drugs QN-302 and CX-5461 (Pidnarulex) in wild-type and
gemcitabine-resistant pancreatic cancer cell
lines” Ahmed Ahmed, Tariq Arshad,
and Stephen Neidle – Results demonstrated that QN-302 (10-fold
more potent than CM03), retains potency in the two gemcitabine
resistant cell lines. Up-regulated G4 genes in the resistant line
are down-regulated by QN-302. The retention of QN-302 activity in
chemo-resistant PDAC cell lines suggests that it may potentially
offer significant advantage in the clinic over gemcitabine-based
therapies. Gemcitabine either alone or in combination is still
among the standard of care for current PDAC treatment. Resistance
to gemcitabine is common and is a major contributor to the poor
outcomes for most PDAC patients.
Compound |
MIA-PaCa2 Parental (S) |
MIA-PaCa2 GemResist |
PANC-1 Parental |
PANC-1GemResist |
|
Gemcitabine |
6.5 ± 0.7 |
11055.7 ± 540.0 |
23.3 ± 8.4 |
28750.9 ± 6121.3 |
|
CM03 |
13.0 ± 8.4 |
14.9 ± 8.3 |
10.4 ± 1.2 |
15.5 ± 1.8 |
|
CX-5461 |
90.3 ± 30.7 |
88.7 ± 22.0 |
32.9 ± 7.6 |
58.8 ± 13.8 |
|
QN-302 |
2.6 ± 1.0 |
3.8 ± 1.2 |
2.3 ± 0.4 |
3.3 ± 0.7 |
|
Abstract #4981 - “The potent
quadruplex-binding compound QN-302 down-regulates the S100P gene in
vitro and in vivo models of pancreatic cancer: a
potential therapeutic target and biomarker for
PDAC” Nicole Williams, Jenny
Worthington, Ahmed Ahmed, Tariq Arshad and Stephen Neidle
– The poster highlighted that QN-302 showed lower expression of the
S100P gene on xenograft models following dosing either twice or
four times weekly with QN-302 (P < 0.05, P < 0.01). S100P is
elevated in human PDAC. Investigators posit that S100P may be a
potential biomarker for QN-302 therapy as it contains a G4 in its
promoter region and binds QN-302.
Abstract #6240 - “The potent
quadruplex-binding compound QN-302 shows anti-tumor activity as a
monotherapy in an orthotopic in vivo model of pancreatic
cancer” Nicole Williams, Danielle Santos, Jenny
Worthington, Ahmed Ahmed, Tariq Arshad and Stephen
Neidle – Study authors identify orthotopic study as the fourth in
vivo pancreatic cancer model showing anticancer activity for
QN-302, further confirming its potential for human cancer
treatment.
Abstract #3098 - “Structure-based design
rules for potent quadruplex-binding compounds
based on the naphthalene diimide core” Stephen Neidle -
The study author concluded that the available data indicates that
G4 affinity is necessary but insufficient for cellular activity.
The ND core contributes little to G4 affinity. Charged side chains
are important for strong G4 binding and cellular activity; >2
cationic side chains are required for both G4 binding and activity.
Four highly cationic side chains reduce cellular activity but
enhance G4 affinity - less basic morpholine groups enhance it.
Molecular modeling suggests that enhancing the ND core with a
planar hydrophobic group could increase G4 affinity and enhance
cellular uptake. Four basic side chains, two of which are
morpholino, are used to optimize the series without excess
basicity. Docking QN-302 into the G4-duplex structure (using
MOLSOFT) indicates that the phenyl substituent is well stacked on a
G of the quartet, as predicted.
About QN-302
QN-302 is a small molecule G-Quadruplex
(G4)-selective transcription inhibitor in development for the
treatment of G4-expressing tumors, such as pancreatic cancer
(PDAC), prostate cancer, sarcomas, Gastrointestinal Stromal Tumors
(GIST), and others. Orphan Drug Designation (ODD) was granted by
the FDA in January of this year for pancreatic cancer. QN-302 is
currently in IND enabling studies toward submission of an
Investigational New Drug (IND) application.
About Qualigen
Therapeutics, Inc.
Qualigen Therapeutics, Inc. is a diversified
life sciences company focused on developing treatments for adult
and pediatric cancer, while also commercializing diagnostics. Our
investigational QN-302 compound is a small molecule selective
transcription inhibitor with strong binding affinity to G4s
prevalent in cancer cells; such binding could, by stabilizing the
G4s against “unwinding,” help inhibit cancer cell proliferation.
The investigational compounds within Qualigen’s family of RAS
oncogene protein-protein interaction inhibitor small molecules are
believed to inhibit or block the binding of mutated RAS genes’
proteins to their effector proteins, thereby leaving the proteins
from the mutated RAS unable to cause further harm. In theory, such
mechanism of action may be effective in the treatment of about one
quarter of all cancers, including certain forms of pancreatic,
colorectal, and lung cancers. Our investigational QN-247 compound
inhibits nucleolin, a key multi-functional regulatory protein that
is overexpressed in cancer cells; QN-247 may thereby be able to
inhibit the cells’ proliferation. QN-247 has shown promise in
preclinical studies for the treatment of acute myeloid leukemia
(AML). In addition to its oncology drug pipeline, Qualigen has an
established diagnostics business which manufactures and distributes
proprietary and highly accurate rapid blood testing systems to
physician offices and small hospitals for the management of
prostate cancer and other diseases and health conditions.
For more information about Qualigen
Therapeutics, Inc., please visit www.qualigeninc.com.
Contact:
Jules AbrahamJQA Partners,
Inc.917-885-7378jabraham@jqapartners.com
Source: Qualigen Therapeutics, Inc.
- Qualigen Therapeutics, Inc.
- Qualigen Therapeutics, Inc.
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