A new cancer treatment that delivers radiation directly to tumours by targeting two key markers simultaneously has been shown to be safe and effective in human trials.

Acting like a “smart missile,” the dual-targeting radiopharmaceutical is designed to attach to two vulnerable sites on cancer cells, enabling more precise and potent therapy.

Early results show that nearly 90 percent of patients experienced either tumour shrinkage or disease stabilisation.

These findings were presented at the Society of Nuclear Medicine and Molecular Imaging 2025 Annual Meeting.

“Radiopharmaceutical therapy is a promising new tool for anti-tumour treatment, and is already used clinically, most notably for prostate cancer and neuroendocrine tumours,” said Jialing Xiang, PhD student at Peking Union Medical College Hospital in Beijing, China.

“While most existing therapies target a single molecular biomarker, my colleagues and I explored a dual-targeting strategy to simultaneously engage two tumour-associated markers, with the aim of enhancing tumour uptake and therapeutic efficacy across multiple types of cancer.”

This first-in-human study assessed preliminary safety, biodistribution, and dosimetry of ¹⁷⁷Lu-labelled FAPI-RGD, the combined radiopharmaceutical therapy drug.

Nine patients with advanced adenocarcinomas—including pancreatic, pulmonary, renal, and ovarian cancers—received a single treatment cycle of the investigational agent.

Baseline uptake was confirmed using ⁶⁸Ga-FAPI-RGD PET/CT imaging, which also assessed dynamic distribution throughout the whole body.

Safety evaluations were conducted and a repeat ⁶⁸Ga-FAPI-RGD PET/CT scan was performed after each treatment cycle to assess early response.

Treatment with ¹⁷⁷Lu-DOTA-FAPI-RGD was well tolerated by all patients, with no noticeable side effects reported.

The therapy showed strong and lasting uptake in tumours, allowing for a high dose of targeted radiation to be delivered directly to cancer cells.

In total, 88.9 percent of patients responded positively, with their cancer either shrinking or stopping its growth.

Many also experienced relief from physical symptoms—reporting less pain, better appetite, and an overall improvement in quality of life compared to previous treatments.

“The beauty of this drug is that it stays in tumours for days, allowing prolonged damage to cancer cells,” noted Xiang.

“It offers real hope for patients with advanced cancers who have exhausted other treatment options. Future prospective trials are planned to optimise dosage for maximum patient benefit, and we look forward to promising developments ahead.”

Source: Society of Nuclear Medicine and Molecular Imaging