One molecule. Five pathways.
Kinisoquin™ targets PD-L1, PDI, VEGF, tissue factor and TMEM176B, giving a single oral asset reach across oncology, hematology, neurology, respiratory and infectious disease.
PIPELINE
Lead Program
Kinisoquin
™
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 clinical trials are currently being initiated:
- Phase 2/3: Lowering D-Dimer and prevention of VTE in Ovarian Cancer together with NIH and MSKCC
- Phase 3: 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)
Additional Programs / 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.
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
9%
of all cancer related deaths are attributable to VTE
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 TMEM176B 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.
Efficacy
Better response in solid tumours, with higher penetration into tumour tissue and higher target engagement.
Safety
Shorter half-life allows faster washout and better management of immune-related side effects. Strong inhibition of PDI leakage and tissue factor reduction lowers thrombosis risk.
Access
An oral asset reduces the burden on patients and on 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 TMEM176B in inflammasome 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™ produced zero VTE events and no major bleeding in 57 patients across 11 US sites, with statistically significant reductions across all key biomarkers: PDI −73%; D-Dimer −22%; sP-selectin −58%.
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. Significant reductions in whole-blood coagulation, platelet aggregation, PDI activity and tissue factor expression were observed, and a Phase 3 study is in active development.
ScienceDirect