SCIENCE
Our Lead Asset is an Isoquercetin based drug code-named Kinisoquin™, a multi-dimensional therapeutic asset (MDTA) targeting PD-L1, PDI, VEGF and Tissue Factor (TF) as well as inflammasome triggering through TMEM176 allowing for development in multiple indications. In combination with Zafirlukast, a repurposed Leukotriene Inhibitor, this therapy will be a potentially Best-in-Class Oral Therapeutic overcoming the main unmet medical needs in the PD-1/PDL1 and VEGF market:
· Potential efficacy advantages: Better response in solid tumors (higher penetration into tumor tissue and higher target engagement).
· Potential safety advantages: Better management of immune-related side effects (shorter half-life allows faster washout); potential for reduced clinic-based infection; strong inhibition of PDI leakage and Tissue Factor reduction activity reduces risk of thrombosis
· Potential for increased penetration as an oral asset reduces burden to patients and to the healthcare system
The Combo improves outcomes significantly as it is synergistic with Kinisoquin™. Both Kinisoquin™ and the Combo significantly improve the effects of Keytruda® and improve further a combination of Cisplatin™ and Gemcitabine® while reducing the risk of Cancer Associated Thrombosis. TMEM176b and PDI inhibition are being used to develop next-generation anti-thrombotics that turn off blood clotting mechanisms inside the vascular system unlike anticoagulants which thin the blood and have significant adverse effects such as bruising and bleeding.
Our scientific programs are exploring:
The Newly Discovered Innate Immune Pathway (NDIIP) and how inflammation influences disease progression across multiple pathways.
The role of TMEM176 in inflammosome modulation and activation and how this influences mast cells, macrophages, neutrophils, interleukins and iron metabolism.
Links between PDI release, endothelial cell damage and the thrombotic cascade.
The relationship of the NDIIP with PD-L1, VEGF and TF.
Cancer-associated thrombosis (CAT):
In a multi-center Phase 2 trial, Kinisoquin™ treatment resulted in inhibition of PDI activity and favorable biomarker changes, with no major bleeding events observed.
JCI Insight
Sickle Cell Disease (SCD):
In collaboration with the National Institutes of Health (NIH), a Phase 2 randomized, double-blind, placebo-controlled study in adults with steady state SCD found Kinisoquin™ to be safe and well tolerated. A significant decrease in whole blood coagulation in steady state SCD patients was seen and a Phase 3 study is in active development.
ScienceDirect
SCIENTIFIC PROGRAMS
Overview
Thrombosis remains the world’s leading cause of death through heart attack, stroke, cancer, COPD and viral disease. Current anticoagulants carry significant bleeding risks, limiting their preventive use.
Up to 30% of cancer patients develop venous thromboembolism (VTE), a major driver of mortality.
2.5-3.6 Fold
Increased mortality in cancer patients who develop VTE
2nd
VTE is 2nd leading cause of death in many cancers, after the cancer itself
of all cancer related deaths are attributable to VTE
Lead Program
Kinosiquin
™
Novel mechanism of action targeting protein disulfide isomerase (PDI).
Significant reduction in thrombosis in cancer patients with reduced bleeding risk in Phase II.
Two additional Phase 3 clinical trials are currently being initiated:
- Lowering D-Dimer and prevention of VTE in Ovarian Cancer together with NIH and MSKCC
- Reduction of whole blood coagulation and crises in Sickle Cell Disease (SCD)
"Developing an effective and safe antithrombotic agent would greatly improve adoption of primary prevention strategies in the cancer community. The primary concern with currently available anticoagulants is the increased risk of hemorrhage."
Jeffrey Zwicker, MD
Professor of Medicine, Memorial Sloan Kettering Cancer Center (MSK)
Pipeline
Phase III investigational therapy with potential to reduce thrombotic events and pain crises.
Phase II program exploring novel combinations and biomarkers.
Phase III program studying the intersection of inflammation, thrombosis, and respiratory decline.
Phase II assessing anti-thrombotic and antiviral potential in collaboration with Administration for Strategic Preparedness and Response (ASPR).
These statements have not been evaluated or approved by the FDA.
