Clinical Translation of a Novel FAPI Dimer [68Ga]Ga-LNC1013

Fibroblast activation protein (FAP) emerges as a highly promising target for cancer diagnostic imaging and targeted radionuclide therapy. To exploit the therapeutic potential of current FAP inhibitors (FAPIs), this study presented the design and synthesis of a series of FAPI dimers to increase tumor uptake and retention. Preclinical evaluation and a pilot clinical PET imaging study were conducted to screen the lead compound with the potential for radionuclide therapy.

Study Overview

• Status: Completed
• Conditions: Gastrointestinal Cancer
• Intervention / Treatment: Diagnostic test: 68Ga-FAPI dimer(68Ga-LNC1013)

Detailed Description

Three new FAPI dimers were synthesized by linking two quinoline-based FAPIs with different spacers. The in vitro binding affinity and preclinical small animal PET imaging of the compounds were compared with their monomeric counterparts, FAPI-04 and FAPI-46. The lead compound, 68Ga-LNC1013, was then evaluated in a pilot clinical PET imaging study involving seven patients with gastrointestinal cancer.

• Study Type: Observational
• Enrollment (Actual): 7

Contacts and Locations

Study Locations

• China
  • Hunan
    • Changsha, Hunan, China
      • Jian Li

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult; Older Adult
• Accepts Healthy Volunteers: N/A

• Sampling Method: Non-Probability Sample

Study Population

Claustrophobia (unable to accept PET/CT scanning)

Description

Inclusion Criteria:

1. Histologically and/or clinically confirmed and/or suspicious of gastrointestinal cancer.
2. Signed informed consent.

Exclusion Criteria:

1. pregnancy;
2. breastfeeding;
3. any medical condition that in the opinion of the investigator may significantly interfere with study compliance.

Study Plan

How is the study designed?

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of discrepancies between [68Ga]Ga-LNC1013 and 68Ga-FAPI-46 or 18F-FDG PET scans	Compare the diagnostic performance between [68Ga]Ga-LNC1013 and 68Ga-FAPI-46 or 18F-FDG in patients with gastrointestinal cancer	5 months
SUVmaxFAPI and SUVmaxFDG for each target (Standardized Uptake Value)	Comparison of 68Ga]Ga-LNC1013, 68Ga-FAPI-46 and 18F-FDG Standardized Uptake Value in the primary tumor and possible metastases	5 months

Collaborators and Investigators

• Sponsor: Xiangya Hospital of Central South University
• Investigators: Study Chair: Shuo Hu, Dr, Xiangya Hospital, Central South University, Changsha, P.R. China

Study record dates

Study Major Dates

• Study Start (Actual): July 21, 2022
• Primary Completion (Actual): July 21, 2022
• Study Completion (Actual): November 25, 2022

Study Registration Dates

• First Submitted: September 17, 2023
• First Submitted That Met QC Criteria: November 28, 2023
• First Posted (Estimated): December 6, 2023

Study Record Updates

• Last Update Posted (Estimated): December 6, 2023
• Last Update Submitted That Met QC Criteria: November 28, 2023
• Last Verified: September 1, 2023

More Information

Terms related to this study

• Keywords: FAPI dimer
• Additional Relevant MeSH Terms: Digestive System Diseases; Neoplasms; Neoplasms by Site; Digestive System Neoplasms; Gastrointestinal Diseases; Gastrointestinal Neoplasms
• Other Study ID Numbers: PETcenter

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No