Trial launches of PSMA-targeting radioligand therapy in mCRPC

The first patient has been dosed in a phase 1 trial of ART-101 in patients with metastatic castration-resistant prostate cancer (mCRPC), Arteus Technologies announced in a news release.¹

According to the company, ART-101 “is a novel receptor-based targeting small molecule developed for the imaging and treatment of prostate cancer.” Preclinical data showed that relative to other currently approved prostate-specific membrane antigen (PSMA)-targeting radioligand therapies, ART-101 demonstrated higher tumor uptake and retention and lower uptake by normal tissues and salivary glands.

“While current radioligand therapies provide a meaningful therapeutic benefit to patients with advanced prostate cancer, there are opportunities to even further enhance a patient’s quality of life and reduce even minimal [adverse] effects,” said principal investigator Harshad Kulkarni, MD, chief medical advisor at BAMF Health, in the news release.¹ “This is especially important with upcoming alpha emitter-based therapies, where lower salivary gland uptake may help mitigate xerostomia.”

ART-101 was discovered and developed by a team at the Advanced Radiotheranostics Lab at the University of Wisconsin, Madison, led by Reinier Hernandez, PhD, MS. Hernandez is the chief technology officer of Archeus Technologies and an assistant professor of medical physics at the University of Wisconsin School of Medicine and Public Health in Madison.

The phase 1 study of the agent will assess the safety, feasibility, biodistribution and kinetics, and tumor targeting of SPECT/CT imaging with [111In]In-ART-101. In total, the investigators plan to enroll approximately 10 patients with mCRPC who are candidates for radioligand therapy with [¹⁷⁷Lu]Lu-PSMA-617 (Pluvicto). Patients are not eligible for enrollment if they are undergoing other concurrent cytotoxic chemotherapy, immunotherapy, radiopharmaceutical therapy, or investigational therapy.

Each patient in the trial will undergo 8 SPECT/CT scans—4 after administration of [111In]In-ART-101 and 4 after administration of [¹⁷⁷Lu]Lu-PSMA-617. Patients will be followed for approximately 2 months.

“With significant development support, and promising preclinical data, ART-101 is an innovative therapeutic candidate with the potential to address key limitations of currently available radiopharmaceutical therapies for patients with prostate cancer,” concluded Hernandez in the news release.¹ “This clinical trial reflects Archeus’ foundational belief that precision imaging and dosimetry are essential to realizing the full potential of radiopharmaceutical therapy, as well as our commitment to advancing the broader portfolio and platform we are building.”

REFERENCES

1. Archeus Technologies doses first patient with ART-101 in phase 1 prostate cancer study. News release. Archeus Technologies. December 2, 2025. Accessed December 8, 2025. https://www.archeustech.com/resources/archeus-technologies-doses-first-patient-with-art-101-in-phase-1-prostate-cancer-study

2. BAMF Health. Prostate Cancer Imaging | Archeus ART-101. Accessed December 8, 2025. https://www.bamfhealth.com/clinical-trials/#a-9824