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- | QN-302 / Qualigen Therap
Journal: The G-quadruplex experimental drug QN-302 impairs liposarcoma cell growth by inhibiting MDM2 expression and restoring p53 levels. (Pubmed Central) - Feb 19, 2025
In patient-derived xenograft mouse models, QN-302 treatment reduced tumour volume distribution and was well tolerated. We have identified a novel and effective therapeutic strategy to reduce MDM2 expression and promote p53 reactivation in tumours harbouring wild-type TP53, such as WD/DDLPSs.
- QN-302 / Qualigen Therap
Structure-activity relationships for the pan-quadruplex experimental drug QN-302 and two analogs probed with comparative transcriptome profiling and molecular modeling (Section 26) - Mar 5, 2024 - Abstract #AACR2024AACR_8153;
The distinct pattern of genes affected by QN-302 is hypothesized to contribute to its superior potency compared to CM03 and SOP1247. Its superior ability to stabilize quadruplex structures has been attributed to its benzyl-pyrrolidine substituent fitting into and filling most of the space in a quadruplex groove compared to the hydrogen atom in CM03 or the methoxy group in SOP1247.
- QN-302 / Qualigen Therap
Characterization of the biological effects of a quadruplex-interacting molecule in dedifferentiated liposarcoma cells (Section 26) - Mar 5, 2024 - Abstract #AACR2024AACR_8147;
In the present study, the biological activity of a tetra-substituted naphthalene diimide (NDI) G4-L derivative (SOP1812/QN-302) has been characterized in two patient-derived DDLPS cell lines...These effects were paralleled by a 3-4 time increase in the number of ?-H2AX foci, the appearance of the cleaved form of PARP-1 and a pronounced inhibition of cell growth over time. Altogether, our findings indicate that targeting G4 structures by quadruplex-interacting molecules may represent a potential novel and effective therapeutic strategy in DDLPS.
- QN-302 / Qualigen Therap
The pan-quadruplex drug QN-302 targets up-regulated genes in pancreatic cancer and in other cancer types and correlate with poor patient prognosis (Section 29) - Mar 5, 2024 - Abstract #AACR2024AACR_5398;
They are especially favored in colorectal, liver and renal cancers, suggesting that QN-302 may have anticancer effects in these cancers as well as in PDAC. We also do not exclude the strong possibility that each cancer type also has its own group of G-quadruplex containing genes that are sensitive to QN-302.
- Early clinical experience with a novel first-in-class G-quadruplex experimental anti-cancer drug (Section 48) - Mar 5, 2024 - Abstract #AACR2024AACR_5176;
We also do not exclude the strong possibility that each cancer type also has its own group of G-quadruplex containing genes that are sensitive to QN-302. Abstract is embargoed at this time.
- QN-302 / Qualigen Therap
The pan-quadruplex drug QN-302 selectively down-regulates key pathway targets in pancreatic cancer cells that are up-regulated in human pancreatic cancer (Section 23) - Mar 5, 2024 - Abstract #AACR2024AACR_2657;
Data from a xenograft model for pancreatic cancer is also available for four of these genes, which concurs with the cellular data. We suggest that the identification of these 11 genes may also provide a basis for biomarker selection and possible patient stratification based on transcriptome data.
- | QN-302 / Qualigen Therap
Journal: Structure-activity relationships for the G-quadruplex-targeting experimental drug QN-302 and two analogues probed with comparative transcriptome profiling and molecular modeling. (Pubmed Central) - Feb 12, 2024
This distinctive pattern of genes affected by QN-302 is hypothesized to contribute to its superior potency compared to CM03 and SOP1247. Its enhanced ability to stabilize G4 structures has been attributed to its benzyl-pyrrolidine substituent fitting into and filling most of the space in a G4 groove compared to the hydrogen atom in CM03 or the methoxy group substituent in SOP1247.
- | QN-302 / Qualigen Therap
Journal: QN-302 demonstrates opposing effects between i-motif and G-quadruplex DNA structures in the promoter of the S100P gene. (Pubmed Central) - Nov 17, 2023
QN-302 exhibits exceptional combined synergistic effects compared to many other G-quadruplex and i-motif interacting compounds. This work further emphasises the importance of considering G-quadruplex and i-motif DNA structures as one dynamic system.
- ||| QN-302 / Qualigen Therap
Enrollment open: Trial to Evaluate Safety, PD & PK of IV Study Drug, QN-302, in Pts w/ Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - Oct 30, 2023
P1, N=54, Recruiting, Sponsor: Qualigen Theraputics, Inc.
This work further emphasises the importance of considering G-quadruplex and i-motif DNA structures as one dynamic system. Not yet recruiting --> Recruiting
- | QN-302 / Qualigen Therap
New P1 trial: Trial to Evaluate Safety, PD & PK of IV Study Drug, QN-302, in Pts w/ Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - Oct 16, 2023
P1, N=54, Not yet recruiting, Sponsor: Qualigen Theraputics, Inc.
- QN-302 / Qualigen Therap
The potent quadruplex-binding compound QN-302 shows anti-tumor activity as a monotherapy in an orthotopic in vivo model of pancreatic cancer (Section 19; Poster Board #10) - Mar 14, 2023 - Abstract #AACR2023AACR_8443;
This orthotopic model is the 4th in vivo study in a pancreatic cancer model showing anti-tumor activity for QN-302, further confirming the potential of this compound for human disease. QN-302 is currently in an advanced stage of pre-IND development by Qualigen Inc.
- QN-302 / Qualigen Therap
The potent quadruplex-binding compound QN-302 down-regulates the S100P gene in in vitro and in vivo models of pancreatic cancer: a potential therapeutic target and biomarker for PDAC (Section 16; Poster Board #27) - Mar 14, 2023 - Abstract #AACR2023AACR_7319;
QN-302 is bio-available at therapeutic doses and is well tolerated at these levels in the animal models. It is being developed for clinical evaluation by Qualigen Therapeutics Inc and is currently at the pre-IND stage.
- QN-302 / Qualigen Therap
Structure-based design rules for potent quadruplex-binding compounds based on the naphthalene diimide core (Section 31; Poster Board #11) - Mar 14, 2023 - Abstract #AACR2023AACR_4533;
This strongly implies that most of the contribution to ND-G4 affinity comes from the side chains, and especially from the protonated end groups. These and other observations have led us to develop a structure-activity framework for tetra-substituted NDs, which has culminated in their optimization and the design of QN-302, with enhanced cellular potency and G4 affinity compared to previous NDs.
- pidnarulex (CX-5461) / Senhwa Biosci, QN-302 / Qualigen Therap
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 (Section 14; Poster Board #16) - Mar 14, 2023 - Abstract #AACR2023AACR_2493;
QN-302 is bio-available at therapeutic doses and is well tolerated at these levels in animal models. It is being developed for clinical evaluation by Qualigen Therapeutics Inc and is currently at the pre-IND stage.
- QN-302 / Qualigen Therap, QN-247 / Qualigen Therap, RAS-F3 / Qualigen Therap
Qualigen Therapeutics (Theater 3) - Jun 4, 2022 - Abstract #BIO2022BIO_319;
Our therapeutics pipeline includes cancer drug compounds such as QN-302, QN-247 (formerly referred to as AS1411-GNP or ALAN), and RAS-F, as well as STARS, a DNA/RNA-based treatment device. By combining our demonstrated ability to develop and commercialize innovative medical products with the advanced capabilities of leading cancer research centers, we are committed to providing exciting new therapeutic technologies to physicians and patients.
- QN-302 / Qualigen Therap
The potent quadruplex-binding compound SOP1812 shows anti-tumor activity in patient-derived in vivo models of pancreatic cancer (Section 27) - Mar 9, 2022 - Abstract #AACR2022AACR_6012;
SOP1812 is bio-available at therapeutic doses and is well tolerated at these levels in these animal models. It is currently being evaluated as a candidate for clinical development by Qualigen Therapeutics Inc.
- QN-302 / Qualigen Therap
The potent quadruplex-binding compound SOP1812 shows potent anti-proliferative activity in a prostate cancer cell panel and anti-tumor activity in an in vivo model of metastatic prostate cancer (Section 27) - Mar 9, 2022 - Abstract #AACR2022AACR_6011;
SOP1812 is bio-available at therapeutic doses and is well tolerated at these levels in this animal model. It is currently being evaluated as a candidate for clinical development by Qualigen Therapeutics Inc.
- QN-302 / Qualigen Therap
Structure-based design of quadruplex-binding small molecule compounds: The essential role of water molecules (Section 40) - Mar 9, 2022 - Abstract #AACR2022AACR_4528;
The compounds CM03 and SOP1812 are tri- and tetra-substituted naphthalene diimide derivatives with high affinity for several human DNA quadruplexes...The rest of each groove is filled by a second cluster of waters, suggesting that larger substituents can be accommodated. Data from a library of naphthalene diimide derivatives is being examined to validate the role of these waters, especially with respect to their relative mobilities and ease of displacement.