Zelenirstat Shows Potent in vitro Radiosensitization in Human Glioblastoma Models

We recently announced results generated at NIH using its lead drug, zelenirstat, presented at the Canadian Association of Radiation Oncology Annual Meeting in Montreal, Canada, on September 23, 2023.

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The presentation, titled “Radiosensitization with Glioblastoma using Targeted Inhibition of N-Myristoylation” highlighted that:

• Zelenirstat was more effective than clinically used radiosensitizers, which generally augment the effects of radiation by 10% to 30%, increasing the effects of radiation by 40% - 140%;
• Orally administered zelenirstat is also predicted to cross the blood brain barrier more efficiently than temozolomide, the current standard of care radiosensitizer for aggressive brain cancers.

Dr. Deepak Dinakaran, MD, PhD, a radiation oncologist and clinician scientist who conducted this research at the US National Institute of Health, said, "Our results show that zelenirstat is a potent radiosensitizer in preclinical models of glioblastoma, and that it works through pathways that differ from available radiosensitizers, including temozolomide.”

“Dr. Dinakaran's exciting mechanistic work and the magnitude of the radiosensitization effect he identified suggests that zelenirstat, which has a broad spectrum of preclinical anticancer activity, might also be added to radiation for a variety of non-brain cancers, including cancers of the head and neck, lung, rectum, and uterine cervix.” said John Mackey, CMO of Pacylex. “This opens up many new opportunities to benefit patients with common solid cancers.”

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