A Novel 68Ga Labeled FAP Ligand PET/CT in Patients With Various Malignant Tumors

The investigators designed and synthesized a novel fibroblast activation protein (FAP) ligand (DOTA-GPFAPI-04) by assembling three functional moieties: a quinoline-based FAP inhibitor for specifically targeting FAP, a FAP substrate Gly-Pro as a linker for increasing the FAP protein interaction, and a 2,2',2",2‴-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetic acid (DOTA) chelator for radiolabeling with different radionuclides. Molecular docking studies investigated the FAP targeting ability of DOTA-GPFAPI-04. DOTA-GPFAPI-04 was then radiolabeled with 68Ga to give 68Ga-DOTA-GPFAPI-04 for positron emission tomography (PET) imaging. The investigators found that the 68Ga-DOTA-GPFAPI-04 has high stability, targeted specificity, and longer retention time. The tumor-to-muscle (T/M) ratio for 68Ga-DOTA-GPFAPI-04 reached 9.15.

Sex

All

Minimum age

18 Years

Maximum age

80 Years

Inclusion Criteria:

1. Patients with high clinical suspicion of malignant tumors;
2. Those who have undergone endoscopic biopsy or puncture biopsy indicating malignant tumors but have not undergone surgery or chemotherapy;
3. Previous history of malignant tumor surgery, suspected of recurrence or distant metastasis;
4. There is a willingness for puncture biopsy or surgery, and there are no contraindications for puncture biopsy or surgery, and there are no contraindications for anesthesia;
5. Sign an informed consent form and undergo a nuclear medicine examination, without any contraindications, with the ability and willingness to participate in the follow-up plan.

Exclusion Criteria:

1. Those who cannot tolerate puncture biopsy or surgical contraindications;
2. Those who have undergone radiotherapy and chemotherapy in the past 3 months;
3. Individuals who are allergic to multiple drugs or foods;
4. Those who refuse nuclear medicine examinations;
5. Those who do not agree to sign an informed consent form and are unable or willing to follow up.

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• RESULTLai C, Cao R, Li R, He C, Wang X, Shi H, Qu C, Qian K, Song S, Chen WH, Cheng Z. Fibroblast Activation Protein Targeting Probe with Gly-Pro Sequence for PET of Glioblastoma. Mol Pharm. 2023 Aug 7;20(8):4120-4128. doi: 10.1021/acs.molpharmaceut.3c00248. Epub 2023 Jul 24. PMID 37487027