Invention:
This invention is for a novel class of MDM2 degraders for treatment of acute myeloid leukemia (AML) and other cancers. This new therapeutic avenue leverages promote ubiquitination of the molecule-MDM2 complex to induce self-degradation in tumors.
Background:
The American Cancer Society’s estimates for acute myeloid leukemia (AML) in the United States for 2024 estimate that about 20,800 people will be diagnosed with AML. Most cases will be in adults, with about 11,220 people will die from AML. Current treatment options for AML and other cancer types, include MDM2 PROTACs, though these options possess high molecular weight among other negative physicochemical properties and a lack of success in clinical trials. This new treatment option utilizes ubiquitination of the MDM2 complex to unlock degradative properties in tumor lines for treatment of a variety of cancers.
Applications:
- Acute myeloid leukemia (AML) therapeutic
- Cancer therapeutics
- Oncology research
Advantages:
- Promotes ubiquitination to induce degradation
- Expected improved preclinical pharmacokinetic efficacy compared to other options
- Decreased toxicity profiles
