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.
This is a first-in-human, Phase 1, non-randomized, multi-centre, open-label clinical trial designed to investigate the safety, tolerability, dosimetry, biodistribution, and pharmacokinetics (PK) of \[225Ac\]-FPI-2059 and \[111In\]-FPI-2058, as well as the pharmacodynamics and preliminary anti-tumour activity of \[225Ac\]-FPI-2059 in participants with neurotensin receptor 1 (NTSR1)-expressing advanced, metastatic and/or recurrent solid tumours. The study will employ a 3+3 dose escalation design to identify the recommended phase 2 dose (RP2D) and regimen of \[225Ac\]-FPI-2059 administered intravenously every 56 days. After the RP2D for \[225Ac\]-FPI-2059 is determined, enrolment will continue into an expansion cohort, to confirm the safety and tolerability of the RP2D, as well as to identify any preliminary evidence of efficacy in selected NTSR1-expressing tumour types.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
19
\[225Ac\]-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.
\[111In\]-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.
University of Alabama at Birmingham Hospital
Birmingham, Alabama, United States
City of Hope Medical Center
Duarte, California, United States
Hoag Family Cancer Institute
Newport Beach, California, United States
University of Kentucky
Lexington, Kentucky, United States
Advanced Molecular Imaging and Therapy
Glen Burnie, Maryland, United States
Washington University
St Louis, Missouri, United States
XCancer Omaha / Urology Cancer Center
Omaha, Nebraska, United States
Westmead Hospital
Sydney, New South Wales, Australia
Incidence of Adverse Events to evaluate safety and tolerability of [225Ac]-FPI-2059 and [111In]-FPI-2058
Time frame: approximately 5 years post final administration
Maximum tolerated dose (MTD) of [225Ac]-FPI-2059
Time frame: 56 days post administration
Radiation dose of [111In]-FPI-2058 and [225Ac]-FPI-2059 to whole body, organs, and selected regions of interest
Time frame: within 56 days of administration
Anti-tumor activity of [225Ac]-FPI-2059 regimen measured by response per RECIST v1.1
Time frame: approximately 5 years post final administration
Tumor uptake of [111In]-FPI-2058 by evaluating SPECT/CT and planar images
Time frame: 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
Time frame: approximately 36 days of final administration
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.