Lead Compound KULA101 Demonstrates Significant Inhibition Of Multiple Immune Checkpoint Proteins Including PD-1, CTLA-4 and Lag-3

SUNRISE, FL, USA I December 4, 2015 I Partikula LLC, a preclinical-stage biotechnology company, today announced results from a study designed to assess the ability of its first-in-class compound, KULA101 to modify the tumor microenvironment and thereby increase immunological activation against cancer cells. The study found that treatment with KULA101 was able to increase the percent of CD4+ and CD8+ T-cells in tumors relative to a vehicle treatment group in a syngeneic mouse model of breast cancer.

In the same study, treatment with KULA101 lowered the expression of multiple checkpoint proteins on CD4+ and CD8+ T-cells relative to vehicle treated tumors, re-activating these tumor-bound immune cells. Specifically KULA101 lowered the expression of PD-1, CTLA-4, Lag-3 and Tim-3, with median decreases of between 37% and 80%. KULA101 is designed to selectively inhibit glycolysis in cancer cells while limiting its effect on other cell types in the tumor microenvironment, including tumor-infiltrating leukocytes.

KULA101 is the first of the company’s Precision Tumor Microenvironment Modifiers (TMEM™) discovered via its advanced chemistry platform. Further IND-enabling studies are ongoing for KULA101 along with additional studies being conducted on other TMEM™ therapies. “Immune checkpoint inhibitors such as Opdivo™, Keytruda™ and Yervoy™ have proven to be valuable weapons in the fight against cancer and a broad-spectrum multiple checkpoint inhibitor like KULA101 might advance the class of cancer immunotherapies significantly if proven clinically. Additionally, by modifying the tumor microenvironment KULA101 might also prove itself to be a valuable pre-treatment or co-treatment regimen for chimeric antigen receptor therapy (CAR-T) and other adoptive cell immunotherapies,” commented Dr. Marc Lippman, chief medical officer and Deputy Director of the University of Miami’s Sylvester Comprehensive Cancer Center.

“Metabolic modulation of cancer cells by glycolysis inhibition can indirectly provide more nutrients to cancer associated immune cells such as T-cells that generally suffer from nutrient deprivation in the tumor milieu. Re-establishing nutrient availability to immune cells can thus make an otherwise immunosuppressive environment more balanced,” said Dr. Shanta Dhar, Professor of Chemistry at University of Georgia and scientific founder of Partikula.

“The real challenge is not just getting enough drug to the tumor but in getting a selective effect on cancer cells over other cell types in the tumor microenvironment that might help fight cancer, like immune cells. The war on cancer will be fought in the trenches and we believe this begins with controlling the battlefield, or in this case, the tumor microenvironment,” added David Kolb, chief executive officer and co-founder of Partikula.

About Partikula

Partikula is a preclinical stage biotechnology company focused on developing novel therapies for cancer and other diseases based on platform chemistry technologies, including its first-in-class precision Tumor Microenvironment Modifiers (TMEM™), that are designed to deliver therapeutics to the mitochondria and other intracellular targets. Partikula was founded in 2013 and is a spinout of the University of Georgia.

SOURCE: Partikula