FDA greenlights phase 1 trial of theranostic radiopharmaceutical for mCRPC

The FDA has granted clearance to an investigational new drug (IND) application for ART-101, a novel receptor-based PSMA-targeting small molecule under investigation for the imaging and treatment of patients with metastatic castration-resistant prostate cancer (mCRPC), Archeus Technologies announced in a news release.¹

ART-101 adds to Archeus’ portfolio of radiopharmaceuticals therapies.

The IND clearance will initiate the launch of a phase 1 trial of the agent in PSMA-positive mCRPC, which the company plans to begin later this year.

“This IND clearance marks an important milestone for Archeus as we prepare to initiate the first of multiple clinical trials set to begin this year from our broader portfolio of differentiated radiopharmaceutical assets for difficult-to-treat cancers,” said Evan Sengbusch, PhD, MBA, CEO of Archeus Technologies, in the news release.¹ “ART-101 represents a promising approach to targeting PSMA-positive prostate cancer with the potential to deliver meaningful clinical benefit and reduced side effects for patients. We are eager to begin evaluating ART-101 in patients to better understand its full therapeutic potential.”

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 an assistant professor of medical physics at the University of Wisconsin School of Medicine and Public Health.

In preclinical studies, the agent demonstrated higher tumor uptake and retention as well as lower uptake in normal tissues and salivary glands compared with currently approved PSMA-targeting agents, Archeus noted.

According to the company, “Archeus plans to evaluate ART-101 as a theranostic radiopharmaceutical agent with the potential to deliver alpha particle-emitting isotopes with greater efficacy and safety compared with current standards of care.”

The company also noted that ART-101 is compatible with multiple therapeutic isotopes, including actinium-225, lutetium-177, and terbium-161. Preclinical data further showed that when paired with these isotopes, ART-101 could deliver a significant potential benefit for prostate cancer.²

ART-101 adds to Archeus’ portfolio of radiopharmaceuticals therapies for difficult-to-treat cancers. In October 2024, the company received FDA clearance of an IND application for their lead candidate, ARC-706, and companion diagnostic, ARC-166. The 2 agents are being developed as a theranostic pair for use in combination with certain validated immunotherapies across a range of tumor types.

Preclinical data showed that ARC-706 may yield clinical activity and immune memory against tumors that were resistant to prior treatment with these immunotherapies.

Clinical development of the agent is also set to commence later this year.

REFERENCES

1. Archeus Technologies receives FDA clearance of investigational New Drug application for ART-101 in development for the treatment of prostate cancer. News release. Archeus Technologies. Published online and accessed June 20, 2025. https://www.archeustech.com/resources/archeus-receives-fda-clearance-of-ind-application-for-art-101-for-prostate-cancer

2. Archeus Technologies and Wisconsin Alumni Research Foundation partner to advance radiopharmaceutical therapy ART-101 into clinical development for prostate cancer. News release. May 28, 2025. Accessed June 20, 2025. https://www.archeustech.com/resources/archeus-and-warf-partner-to-advance-art-101-into-clinical-development-for-prostate-cancer