Overview

We have invented a cancer treatment that consists of administering an anti-cancer maleimide derivative together with an immune checkpoint blockade.

Market Opportunity

Globally, colorectal cancer (CRC) ranks third in incidence and second in mortality. The U.S. Food and Drug Administration recently approved the checkpoint inhibitors nivolumab and pembrolizumab for microsatellite instability-high (MSI-H) CRC cases after chemotherapy. Although immune checkpoint blockade (ICB) clinical trials have demonstrated their efficiency in cases of MSI-H CRC, a notable lack of response has been observed in microsatellite stable (MSS) CRC. Thus, there remains a significant unmet need for the ~85% of patients with MSS CRC for whom ICB is less effective.

Innovation and Meaningful Advantages

We have invented a cancer treatment that consists of administering an anti-cancer maleimide derivative together with an ICB. Immune checkpoints, a normal part of the immune system, prevent an immune response from being so strong that it destroys healthy cells. Immune checkpoint inhibitors work by blocking checkpoint proteins from binding with their partner proteins. We have identified several maleimide derivatives that have the potential to upregulate programmed death-ligand (PD-L1) expression for therapeutic synergy with an ICB. Glycogen synthase kinase 3 (GSK-3), which plays key roles in many biological processes such as tumor progression. is an especially promising treatment target.

We have found that the maleimide derivative elraglusib, in particular, has superior pharmacokinetic properties and is significantly more potent than other GSK-3 inhibitors. The types of cancer that can be treated using our invention include breast cancer, central nervous system cancer, colon cancer, hepatic cancer, leukemia, melanoma, non-small cell lung cancer, ovarian cancer, prostate cancer, and renal cancer.

Collaboration Opportunity

We are interested in exploring 1) research collaborations with leading pharmaceutical companies to develop this method of treatment; and 2) licensing opportunities with pharmaceutical companies.

Principal Investigator

IP Information

PCT/US23/14817, Filed March 8, 2023

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