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NCT Number: NCT07299253

Preclinical Safety Evaluation and First-in-Human Translational Study of [177Lu]Lu-TEFAPI-06

This study aims to systematically evaluate the safety, biodistribution, dosimetry, and preliminary therapeutic potential of [177Lu]Lu-TEFAPI-06 through an exploratory first-in-human (FIH) trial.

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Key information

Conditions

Metastatic Solid Tumors (Any Localization)

Age range

18 year and older

Sex eligibility

All sexes

Study type

Interventional

Phase

Early Phase 1

Primary location

The Second Hospital & Clinical Medical School, Lanzhou University

Lanzhou, Gansu, 730000, China

About this study

This study represents a comprehensive "bench-to-bedside" translational investigation, providing the first systematic report on the safety profile of [177Lu]Lu-TEFAPI-06-a novel albumin-binding fibroblast activation protein inhibitor (FAPI) radiopharmaceutical-and its successful transition into a FIH. The investigators preliminarily evaluated its safety, dosimetry, and therapeutic response in patients with ibroblast activation protein (FAP)-overexpressing metastatic solid tumors.

Who can participate

Healthy volunteers accepted: No

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Age > 18 years
  • Histologically confirmed advanced metastatic solid tumors refractory or intolerant to standard therapies
  • ECOG performance status 0-2
  • Life expectancy > 3 months
  • At least one FAP-avid lesion confirmed by baseline [18F]-FAPI PET/CT
  • Adequate organ and bone marrow function prior to the first dose

Exclusion criteria

  • Chemotherapy, radiotherapy, or targeted therapy within 4 weeks
  • Severe hepatic or renal dysfunction
  • Uncontrolled active infection or severe comorbidities

Treatment and study plan

radionuclide therapy with [177Lu]Lu--TEFAPI-06

Drug

A Novel Albumin-Binding FAPI Radiopharmaceutical for Theranostics

Primary outcomes

  1. Incidence and Severity of Treatment-Emergent Adverse Events (TEAEs) as Assessed by CTCAE v5.0

    Time frame: From Baseline up to 30 days after the last dose of study intervention (approximately 4 weeks)

    Safety and tolerability will be assessed by recording the frequency, duration, and severity of Adverse Events (AEs) and Serious Adverse Events (SAEs). The assessment includes clinically significant changes in vital signs (blood pressure, heart rate, respiratory rate, temperature), physical examination findings, 12-lead Electrocardiogram (ECG) parameters, and clinical laboratory tests (including Complete Blood Count [CBC], Urinalysis, Liver Function Tests [LFTs], and Renal Function Tests). Severity of adverse events will be graded according to the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) Version 5.0.

Secondary outcomes

  1. Change from Baseline in [18F]-FAPI PET/CT Parameters in Target Lesions

    Time frame: Baseline (Day 0) and 1 month post-treatment.

    [18F]-FAPI PET/CT images will be acquired to evaluate the expression of FAP within the tumor stroma. The efficacy assessment will be based on the quantitative analysis of Standardized Uptake Values (SUVmax and SUVmean) and Tumor-to-Background Ratios (TBR) of the target lesions. Changes in tracer uptake between the baseline scan and the follow-up scan will be calculated.

  2. Change from Baseline in Tumor-Specific Serum Marker Levels

    Time frame: Baseline (Day 0) and 1 month post-treatment.

    Peripheral blood samples will be collected to measure the serum concentration of tumor-specific biomarkers relevant to the indication (e.g., CEA, CA19-9, PSA, or other applicable markers). The change in concentration levels will be assessed to evaluate biochemical response.

Other outcomes

  1. Biodistribution and Pharmacokinetics of [177Lu]Lu-TEFAPI-06

    Time frame: 0.5, 2, 24, 48, 72, and 120 hours post-injection.

    Biodistribution will be assessed by quantitative analysis of Whole-Body planar and SPECT/CT images. Tracer uptake in blood, normal organs (kidneys, liver, etc.), and tumor tissues will be quantified at serial time points. Parameters to be analyzed include the percentage of injected dose (%ID) and percentage of injected dose per gram (%ID/g) for each regions of Interest (ROI) .

  2. Radiation Absorbed Doses in Normal Organs and Tumor Lesions

    Time frame: Post-injection at 0.5, 2, 24, 48, 72, and 120 hours.

    Radiation dosimetry will be calculated based on biodistribution data derived from serial imaging. Following the administration of [177Lu]Lu-TEFAPI-06, Whole-Body (WB) planar scintigraphy and SPECT/CT scans will be performed. ROIs will be drawn over source organs and tumor lesions to generate time-activity curves. Absorbed doses (in Gy/GBq) will be estimated using standard dosimetry software (e.g., OLINDA/EXM or IDAC) based on the MIRD scheme.

Sponsors and collaborators

Lead sponsor

Lanzhou University Second Hospital

Other

Registry information

Official study title

Preclinical Safety Evaluation and First-in-Human Translational Study of [177Lu]Lu-TEFAPI-06: A Novel Albumin-Binding FAPI Radiopharmaceutical for Theranostics

Important dates

Study start
2023
Primary completion
2024
Study completion
2025
First posted
Dec 23, 2025
Registry last updated
Dec 23, 2025

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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