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

Early Phase 1CompletedNCT07299253

Lanzhou University Second Hospital5 enrolled

Overview

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.

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.

Study Type

INTERVENTIONAL

Allocation

Purpose

OTHER

Masking

NONE

Enrollment

Conditions

Metastatic Solid Tumors (Any Localization)

Interventions

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

A Novel Albumin-Binding FAPI Radiopharmaceutical for Theranostics

Eligibility

Sex: ALLMin age: 18 Years

Medical Language ↔ Plain English

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

Locations (1)

The Second Hospital & Clinical Medical School, Lanzhou University

Lanzhou, Gansu, China

Outcomes

Primary Outcomes

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

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.

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

Secondary Outcomes

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

\[18F\]-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.

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

Change from Baseline in Tumor-Specific Serum Marker Levels

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.

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

Data from ClinicalTrials.gov

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