A Study of [225Ac]-FPI-2059 in Adult Participants With Solid Tumours

NCT05605522 | Terminated Phase 1 FDA Drug

• 1 other identifier: FPI-2059-101
• Study Type: interventional
• Target: 19
• Locations: 2 countries
• Sites: 8

Brief Summary

This is a first-in-human Phase 1 clinical trial designed to investigate the safety, tolerability, pharmacokinetics, and biodistribution of \[225Ac\]-FPI-2059 and \[111In\]-FPI-2058 in participants with neurotensin receptor 1 (NTSR1)-expressing solid tumours.

Conditions

Pancreatic Ductal Adenocarcinoma (PDAC); Squamous Cell Carcinoma of Head and Neck; Colorectal Cancer; Gastric Cancer; Ewing Sarcoma; NTSR1 Expressing Solid Tumours; Neuroendocrine Differentiated (NED) Prostate Cancer

Keywords

Solid Tumor; FPI-2059; FPI-2058; Pancreas; Prostate; Neuroendocrine; Stomach cancer; Gastric; Ewing sarcoma; HNSCC; Squamous cell carcinoma; CRC; Colorectal; actinium; targeted alpha therapy; radiopharmaceuticals

Outcome Measures

Primary Outcomes (3)

• Incidence of Adverse Events to evaluate safety and tolerability of [225Ac]-FPI-2059 and [111In]-FPI-2058

  approximately 5 years post final administration

• Maximum tolerated dose (MTD) of [225Ac]-FPI-2059

  56 days post administration

• Radiation dose of [111In]-FPI-2058 and [225Ac]-FPI-2059 to whole body, organs, and selected regions of interest

  within 56 days of administration

Secondary Outcomes (3)

• Anti-tumor activity of [225Ac]-FPI-2059 regimen measured by response per RECIST v1.1

  approximately 5 years post final administration

• Tumor uptake of [111In]-FPI-2058 by evaluating SPECT/CT and planar images

  within 56 days of administration

• Pharmacokinetics (PK) of [225Ac]-FPI-2059 and [111In]-FPI-2059 by measuring changes in clearance, AUC, Cmax, and half-life

  approximately 36 days of final administration

Study Arms (2)

Phase 1 Dose Escalation

EXPERIMENTAL

Drug: [225]-FPI-2059; Drug: [111In]-FPI-2058

Phase 1 Dose Expansion

EXPERIMENTAL

Drug: [225]-FPI-2059; Drug: [111In]-FPI-2058

Interventions

[225]-FPI-2059 DRUG

\[225Ac\]-FPI-2059 is a targeted alpha therapeutic that consists of an NTSR1-targeting small molecule that is linked to Ac-225, an alpha particle emitting radionuclide. Participants will be dosed through IV administration every 56 days up to four cycles. The dose depends on cohort assignment. In the Dose Expansion arm, \[225Ac\]-FPI-2059 will be administered at the RP2D as determined in Phase 1 Dose Escalation.

Phase 1 Dose Escalation; Phase 1 Dose Expansion

[111In]-FPI-2058 DRUG

\[111In\]-FPI-2058 is an imaging agent that consists of an NTSR1-targeting small molecule linked to In-111.Participants will receive \[111In\]-FPI-2058 by IV Injection for imaging once during screening period. The dose is consistent across cohorts.

Phase 1 Dose Escalation; Phase 1 Dose Expansion

Eligibility Criteria

• Age: 18 Years+
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Signed ICF prior to initiation of any study-specific procedures
• Histologically and/or cytologically confirmed solid tumor that is metastatic or locally advanced, inoperable, or recurrent. Solid tumors indications may include PDAC, CRC, NED prostate cancer, gastric cancer, SCCHN, and Ewing sarcoma.
• Disease that has progressed despite prior treatment, and for which additional effective standard therapy is not available or is contraindicated, not tolerable, or the patient refuses standard therapy
• Measurable disease per RECIST v.1.1
• Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1
• Sufficient target expression in at least one measurable lesion as determined by imaging following injection of \[111In\]-FPI-2058
• Adequate organ function
• Tumor tissue (either archival within the last 24 months or fresh biopsy)

You may not qualify if:

• Previous treatment with any radiopharmaceutical
• Contraindications to or inability to perform the imaging procedures required in this study
• Anti-cancer therapy, such as chemotherapy, immunotherapy, hormonal therapy, targeted therapy, or investigational agents within certain amount of time prior to administration of the first dose of \[111In\]-FPI-2058
• Radiation therapy (RT) within 28 days prior to the first dose of \[111In\]-FPI-2058
• Patients with known CNS metastatic disease
• Concurrent severe and/or uncontrolled illness that would limit compliance with study requirements
• Known or suspected allergies or contraindication to the investigational treatment
• Received any type of vaccine within 30 days prior to the first dose of \[111In\]-FPI-2058

Sponsors & Collaborators

• 3B Pharmaceuticals GmbH: lead

Study Sites (8)

University of Alabama at Birmingham Hospital

Birmingham, Alabama, 35249, United States

Location

City of Hope Medical Center

Duarte, California, 91010, United States

Location

Hoag Family Cancer Institute

Newport Beach, California, 92663, United States

Location

University of Kentucky

Lexington, Kentucky, 40536, United States

Location

Advanced Molecular Imaging and Therapy

Glen Burnie, Maryland, 21061, United States

Location

Washington University

St Louis, Missouri, 63110, United States

Location

XCancer Omaha / Urology Cancer Center

Omaha, Nebraska, 68130, United States

Location

Westmead Hospital

Sydney, New South Wales, 2145, Australia

Location

MeSH Terms

Conditions

Squamous Cell Carcinoma of Head and Neck; Colorectal Neoplasms; Stomach Neoplasms; Sarcoma, Ewing; Prostatic Neoplasms; Carcinoma, Squamous Cell

Condition Hierarchy (Ancestors)

Carcinoma; Neoplasms, Glandular and Epithelial; Neoplasms by Histologic Type; Neoplasms; Head and Neck Neoplasms; Neoplasms by Site; Intestinal Neoplasms; Gastrointestinal Neoplasms; Digestive System Neoplasms; Digestive System Diseases; Gastrointestinal Diseases; Colonic Diseases; Intestinal Diseases; Rectal Diseases; Stomach Diseases; Osteosarcoma; Neoplasms, Bone Tissue; Neoplasms, Connective Tissue; Neoplasms, Connective and Soft Tissue; Sarcoma; Genital Neoplasms, Male; Urogenital Neoplasms; Genital Diseases, Male; Genital Diseases; Urogenital Diseases; Prostatic Diseases; Male Urogenital Diseases; Neoplasms, Squamous Cell

Study Officials

• Aaron Enke

  3B Pharmaceuticals GmbH

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 31, 2022
• First Posted: November 4, 2022
• Study Start: February 7, 2023
• Primary Completion: July 19, 2024
• Study Completion: February 20, 2025
• Last Updated: August 24, 2025

Record last verified: 2025-08

Locations

AU (1); US (7)