Inhibitors of sPLA2 as a Treatment for Cancer

SK2019-064

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SUMMARY OF INVENTION

Ras gene mutations occur in up to 30%  of all cancers, including about 45% of colorectal, 32% of lung and nearly all pancreatic cancers.  MSK investigators have observed that Ras mutations trigger senescence-associated proliferation in cell culture and animal models, that ultimately leads to inflammation. In particular, a large family of lipolytic serine hydrolase-encoding inflammatory genes, called secretory phospholipase A2 (sPLA2), are observed in malignant tissues harboring Ras mutations. 

Scientists at MSK have identified a group of sPLA2 inhibitors that promote the death of viable stressed cells harboring oncogenic Ras. sPLA2 inhibitors represent a class of drugs that has been used to treat atherosclerosis, such as darapladib, and potentially may be effective in treating cancer.

ADVANTAGES

  • This invention offers a novel approach to cancer treatment, by  targeting Ras, the most mutated gene in many cancer types.
  • Dr. Daniel Heller’s team at MSK is experienced in focusing on biomaterials and nanoscale engineering for molecular sensors and targeted therapeutics.

MARKET OPPORTUNITIES

KRAS G12V mutation occurs in nearly 5% of cancer cases, with pancreatic adenocarcinoma, lung adenocarcinoma, colon adenocarcinoma, colorectal adenocarcinoma, and rectal adenocarcinoma displaying the greatest prevalence. Overall, this proposed approach could target about 600,000 patients worldwide.

 AREAS OF APPLICATION

  • KRAS G12V mutated cancers
  • Non-small cell lung cancer (NSCLC)
  • Colon cancer
  • Colorectal cancer
  • Rectal cancer
  • Pancreatic cancer

PATENT INFORMATION

PCT/US2020/042162

LEAD INVESTIGATOR

Daniel A. Heller, PhD, Cancer Nanomedicine Laboratory Head, Memorial Sloan Kettering Cancer Center

CONTACT INFORMATION

Eileen Flowers, Ph.D.

Associate Director, Technology Development
Tel: 646-888-1067
E-mail: flowerse@mskcc.org

Stage of Development

In vitro