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Targeted Alpha Therapy: A Breakthrough in Treating Intractable Skin Cancer

Targeted Alpha Therapy: A Breakthrough in Treating Intractable Skin Cancer

 


Metastatic melanoma, also known as stage IV melanoma, is a type of skin cancer that spreads to other parts of the body. This is one of the most aggressive forms of skin cancer, with current therapies, including immunotherapy and targeted drugs showing limited efficacy. Although radiation therapy is a new treatment for melanoma, traditional beta radionuclide therapy is limited due to low energy transfer and long-range radiation, which can cause unintended damage to healthy tissue.

Enhance the effectiveness of radiation therapy (TAT) as a promising alternative to traditional beta therapy, a Japanese research team led by Professor Suzuki of Japan, including Suzuki of Chiba University, Doctor of Chiba University, Doctor of Chiba University, Doctor of Chiba University, Doctor of Science and Technology, Dr Tanaka of Throne, Dr. Jundendo, and Dr. Tadashi Watab, Targeted Dr. Tanaka of Targeted Dr. Tadashi Watab, Doctor of Targeted Dr. Tagetta Osacca. They developed astatin-211 (211at) can provide potential breakthroughs for the treatment of metastatic melanoma – labeled peptide drugs. This research was conducted in collaboration with the National Institute of Quantum Science and Technology, European nuclear medicine and molecular imaging January 20th, 2025.

TAT is a type of radiotherapy that involves drugs labeled with alpha particle luminescent radioisotopes. Compared to other forms of radioactive emissions (beta and gamma emissions), alpha particles are heavier and therefore have shorter distances. Because of its large mass, alpha particles also have relatively high energy. This is beneficial in the destruction of cancer cells.

To develop the treatment, researchers first identified the optimal hydrophilic linker to enhance tumor targeting and reduce untargeted accumulation. The team then designed the Astatin-211 (211at) – labeled α-melanocyte-stimulating hormone (α-MSH) peptide analogue [211At]NPG-GGN4C specifically targets melanocortin-1 receptor (MC1R) that is overexpressed in melanoma cells. “Tagned peptides also acquired receptor targets, which increased tumor selectivity while minimizing radiation exposure to surrounding tissues,” commented Dr. Suzuki.

The synthesized peptides were then tested in a mouse model containing B16F10 melanoma, and then the team conducted biodistribution analysis comparing tumor uptake, clearance from organs, and overall stability of the compounds. Dr. Uehara explained the methodology in detail, saying, “We treated mice with different doses of compounds, monitoring tumor response, weight and survival over time. We discovered dose-dependent inhibitory effects in mouse models with melanoma and confirmed the effectiveness of the approach.”

The findings were surprising. [211At]NPG-GGN4C showed high tumor accumulation and rapid clearance from non-target organs, confirming the specificity of MC1R in melanoma cells. Monitoring tumor growth revealed significant dose-dependent tumor suppression. moreover, [211At]NPG-GGN4C also showed high plasma stability, minimizing the risk of radioactive leakage in the body.

While bringing exciting results, Dr. Suzuki asserts that the molecular design of their synthetic drugs could be useful for other developments. 211Labeled radiation drugs. He says, “We believe our approach can open up new possibilities for treating fire-resistant cancer beyond melanoma.”

The team also 211Base tat. “If human trials are successful, this treatment could emerge as a viable treatment option for patients with progressive melanoma in the coming years,” says Suzuki. “This could provide new treatment opportunities for patients with refractory cancer.”

Sources

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2/ https://www.sciencedaily.com/releases/2025/03/250312124420.htm

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What Are The Main Benefits Of Comparing Car Insurance Quotes Online

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