Zantrene® kills melanoma cancer cells that overproduce FTO

30 September 2021 | Thursday | News


Race Oncology Limited ("Race") is pleased to share interim results from our collaborative preclinical melanoma research program with the University of Newcastle (ASX Announcement: 19 Mar 2021). Eminent melanoma researchers, Professor Xu Dong Zhang and Associate Professor Lei Jin, are leading the project.
Melanoma cells stained with the BAK1 (red) and Dapi (blue).

Melanoma cells stained with the BAK1 (red) and Dapi (blue).

  • Zantrene® at low concentrations kills high FTO producing melanoma cancer cells
  • Sensitivity to Zantrene® correlates with FTO levels, where high FTO producing cells show up to 60x greater sensitivity than low FTO producing cells
  • Results are highly supportive of future clinical trials in melanoma using Zantrene® in combination with standard of care treatments

Race Oncology Limited ("Race") is pleased to share interim results from our collaborative preclinical melanoma research program with the University of Newcastle (ASX Announcement: 19 Mar 2021). Eminent melanoma researchers, Professor Xu Dong Zhang and Associate Professor Lei Jin, are leading the project.

This program is exploring the use of Zantrene® (bisantrene dihydrochloride) as a novel potential treatment for melanoma using cellular and mouse models. The aim is to identify drug combinations and melanoma subtypes that show improved treatment responses, with a focus on treatment-resistant melanomas.

These interim results showed Zantrene to be highly effective at killing a diverse range of high FTO producing melanoma cell subtypes. Data from the expression of the Fat Mass and Obesity-associated protein (FTO) showed an association between FTO expression level and sensitivity to Zantrene.

 

Zantrene has been identified as a potent targeted inhibitor of the Fat Mass and Obesity associated protein (FTO).[1] Previous studies have observed that FTO is over-produced in approximately 50% of metastatic melanomas[2] and that inhibition of FTO can overcome PD-1 immune checkpoint resistance in mouse melanoma models.[2,3] PD-1 immune checkpoint inhibitors have emerged as a front-line treatment for many types of cancer, including melanoma. While there have been major advances in melanoma treatments in recent decades, the five-year survival rate for advanced melanoma remains low.[4]

Race CSO Dr Daniel Tillett said: "These interim results are highly encouraging and support our clinical plans for Zantrene, with the correlation between FTO overexpression and sensitivity to Zantrene suggesting a strong anti-FTO therapeutic opportunity. The high sensitivity of many of the melanoma cell lines to Zantrene as a single agent at concentrations well below chemotherapeutic doses is unexpected and may offer new treatment options for melanoma patients."

Race CEO & MD Phillip Lynch said: "While challenged by COVID-19 related shutdowns we appreciate the encouraging and continued work from the team at the University of Newcastle. Zantrene continues to positively surprise us – we are very pleased with these early results. Melanoma remains a difficult cancer to treat, and one that's of particular relevance to the Australian community, so as we continue with this work, we look forward to learning more about our potential to offer new treatment options to patients."

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