As an new dual targeting PET radiotracer, 68Ga-FAP-RGD is promising as an excellent imaging agent applicable to various cancers. In this study, we observed the safety, biodistribution and radiation dosimetry of 68Ga-FAP-RGD in patients with various types of cancer and compared them with the results of 68Ga-FAPI-02 or 18F-FDG imaging to evaluate the dosimetric characteristics and diagnostic efficacy of 68Ga-FAP-RGD.

Start Date01 May 2022

Sponsor / Collaborator

First Affiliated Hospital Of Fujian Medical University

100 Clinical Results associated with 68Ga-FAP-RGD

100 Translational Medicine associated with 68Ga-FAP-RGD

100 Patents (Medical) associated with 68Ga-FAP-RGD

Literatures (Medical) associated with 68Ga-FAP-RGD

01 May 2024·European Journal of Nuclear Medicine and Molecular Imaging

Peptidic heterodimer-based radiotracer targeting fibroblast activation protein and integrin αvβ3

Article

Author: Chen, Bei ; Liu, Kehuang ; Yin, Xiaoqin ; Rao, Wanqian ; Xu, Pengfei ; Jiang, Tao ; Hu, Shuo

PURPOSESeveral studies have demonstrated the advantages of heterodimers over their corresponding monomers due to the multivalency effect. This effect leads to an increased number of effective targeted receptors and, consequently, improved tumor uptake. Fibroblast activation protein (FAP) and integrin α_vβ₃ are found to be overexpressed in different components of the tumor microenvironment. In our pursuit of enhancing tumor uptake and retention, we designed and developed a novel peptidic heterodimer that synergistically targets both FAP and integrin α_vβ₃.METHODSFAP-RGD was synthesized from FAP-2286 and c(RGDfK) through a multi-step organic synthesis. The dual receptor binding property of ⁶⁸Ga-FAP-RGD was investigated by cell uptake and competitive binding assays. Preclinical pharmacokinetics were determined in HT1080-FAP and U87MG tumor models using micro-positron emission tomography/computed tomography (micro-PET/CT) and biodistribution studies. The antitumor efficacy of ¹⁷⁷Lu-FAP-RGD was assessed in U87MG tumor models. The radiation exposure and clinical diagnostic performance of ⁶⁸ Ga-FAP-RGD were evaluated in healthy volunteers and cancer patients.RESULTSBi-specific radiotracer ⁶⁸Ga-FAP-RGD exhibited high binding affinity for both FAP and integrin α_vβ₃. In comparison to ⁶⁸Ga-FAP-2286 and ⁶⁸Ga-RGDfK, ⁶⁸Ga-FAP-RGD displayed enhanced tumor uptake and longer tumor retention time in preclinical models. ¹⁷⁷Lu-FAP-RGD could efficiently suppress the growth of U87MG tumor in vivo when applied at an activity of 18.5 and 29.6 MBq. The effective dose of ⁶⁸Ga-FAP-RGD was 1.06 × 10^-2 mSv/MBq. ⁶⁸Ga-FAP-RGD demonstrated low background activity and stable accumulation in most neoplastic lesions up to 3 h.CONCLUSIONTaking the advantages of multivalency effect, the bi-specific radiotracer ⁶⁸Ga-FAP-RGD showed superior tumor uptake and retention compared to its corresponding monomers. Preclinical studies with ⁶⁸Ga- or ¹⁷⁷Lu-labeled FAP-RGD showed favorable image contrast and effective antitumor responses. Despite the excellent performance of ⁶⁸Ga-FAP-RGD in clinical diagnosis, experimental efforts are currently underway to optimize the structure of FAP-RGD to increase its potential for clinical application in endoradiotherapy.

100 Deals associated with 68Ga-FAP-RGD

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Phase 2	CN	First Affiliated Hospital Of Fujian Medical University	01 May 2022

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