Cerenis May Develop HDL Cholesterol as Tumor Visualization Tool for Targeted Cancer Therapy

Cerenis May Develop HDL Cholesterol as Tumor Visualization Tool for Targeted Cancer Therapy

Cerenis Therapeutics has recruited its first patients into a trial to test whether HDL particles — more commonly known as good cholesterol — can be used to visualize tumors.

If proven effective, the French pharmaceutical company says its method could be developed into a tool to deliver cancer medications specifically to tumor cells, sparing healthy tissues the toxic side effects.

While HDL is mostly known for its role in fat metabolism, researchers have realized that many tumors use HDL to get the material needed for their growth. Such tumors have HDL receptors on their surfaces. This feature makes HDL a good candidate to develop methods of visualizing tumors.

But the longer-term goal is to use HDL to deliver drugs straight to a tumor instead of exposing the entire body to a harsh therapy.

The compound used in the trial is CER-001 —  a man-made version of one of the main components of HDL particles. Researchers have linked CER-001 to Zirconium 89 (89Zr)— a factor that lights up on a scan.

Animal experiments suggest the method would work, but the trial, called TARGET, is the first time the concept will be tried in humans — adults with primary esophageal carcinoma.

The study will evaluate the concentrations of 89Zr-labeled CER-001 in tumor tissue and evaluate how the compound is distributed in the rest of the body. Tests will also allow researchers to analyze the degree of tumor selectivity.

By comparing factors seen in tumor tissue samples and the signal elicited by 89Zr-labeled CER-001, researchers will relate the compound to various tumor features.

“TARGET is our first step in the clinic and this imaging study in patients will validate HDL selective tumor targeting by demonstrating that cancer cells which over-express HDL receptors facilitate HDL targeted drug delivery,” Dr. Jean-Louis Dasseux, founder and CEO of Cerenis, said in a press release.

The study will serve as a basis to develop the compound as a drug delivery tool. Used along with what Cerenis calls NanoDisk technology, the company believes it can load the HDL particles with a large variety of cancer drugs — an idea to be explored in later studies if the current trial is successful.

“CER-001 targeting particles associated with the NanoDisk technology hold the promise to treat cancer with lowered systemic toxicity,” said principal investigator Dr. Hanneke Van Laarhoven of Amsterdam Medical Center. “The fact that a wide variety of drugs can be embedded in HDL nanoparticles could increase efficacy compared to available drug delivery technologies and open a new generation of drugs in oncology.”

Cerenis, which expects to finish the study by mid-2018, is also testing CER-001 in patients with metabolic and genetic diseases.