An Open-Label, Non-Randomized, Dose Escalation, Single-Center, Investigator-Initiated Trial to Determine the Safety, Dosimetry, and Preliminary Effectiveness of 177Lu-DOTA-EB-FAPI in Metastatic Radioactive Iodine Refractory Thyroid Cancer Patients With Progressive Disease After Tyrosine Kinase Inhibitors Treatment

Increased fibroblast activation protein expression is positively correlated with the dedifferentiation and aggressiveness of thyroid cancer. Radiolabeled fibroblast activation protein inhibitor therapy, also known as radioligand therapy has become a novel treatment for patients with radioactive iodine refractory thyroid cancer and disease progression after first-line treatment. However, a major problem in the therapeutic use of 177Lu-DOTA-FAPI has been its short half-life and fast rate of clearance. This study was designed to evaluate the safety, tolerability, and maximum tolerated dose of a long-lasting radiolabeled fibroblast activation protein inhibitor 177Lu-DOTA-EB-FAPI in mRAIR-TC patients with PD after TKIs treatment.

Start Date15 Jun 2022

Sponsor / Collaborator

The First Affiliated Hospital of Xiamen University

NCT05963386 / CompletedPhase 2IIT

An Open-Label, Non-Randomized, Single-Center, Investigator-initiated Phase II Trial to Determine the Efficacy and Safety of 177Lu-DOTA-EB-FAPI in Patients with Various End-stage Solid Tumors

Increased fibroblast activation protein expression is positively correlated with the aggressiveness of cancer. Radiolabeled fibroblast activation protein inhibitor therapy, also known as radioligand therapy has become a novel treatment for patients with refractory cancer and disease progression after multiple-lines treatment. However, a major problem in the therapeutic use of 177Lu-DOTA-FAPI has been its short half-life and fast rate of clearance. This study was designed to investigate the efficacy and safety of 177Lu-DOTA-EB-FAPI in patients with various solid tumors who had failed standard therapies.

Start Date22 Feb 2022

Sponsor / Collaborator

The First Affiliated Hospital of Xiamen University

100 Clinical Results associated with 177Lu-DOTA-EB-FAPI

100 Translational Medicine associated with 177Lu-DOTA-EB-FAPI

100 Patents (Medical) associated with 177Lu-DOTA-EB-FAPI

Literatures (Medical) associated with 177Lu-DOTA-EB-FAPI

01 Nov 2024·Clinical Nuclear Medicine

68Ga-DOTA-IBA PET/CT and 18F-FDG PET/CT in Ewing Sarcoma

Article

Author: Ma, Wenzhe ; Tan, Xiaoqi ; Xiang, Feifan ; Chen, Yue ; Liu, Huipan

AbstractA 29-year-old man with Ewing sarcoma in the right ankle underwent 68Ga-DOTA-IBA PET/CT and 18F-FDG PET/CT, both of which showed high radiotracer activity for the primary tumor. Interestingly, bone metastases were detected early using 68Ga-DOTA-IBA PET/CT for the sixth thoracic vertebrae and with 18F-FDG PET/CT for the bilateral humerus. Higher uptake of 68Ga-DOTA-IBA was found in both primary and metastatic sites of Ewing sarcoma. 177Lu-DOTA-IBA may be one of the possible therapies for metastatic or recurrent Ewing sarcoma.

01 Oct 2024·Clinical Nuclear Medicine

68Ga-FAPI-RGD PET/CT Detected Skull Metastasis Better Than 18F-FDG in a Patient With Radioiodine-Refractory Differentiated Thyroid Cancer

Article

Author: Chen, Yun ; Zang, Jie ; Wu, Zenan ; Miao, Weibing

AbstractA 60-year-old woman underwent resection of a right humeral tumor 1 year ago, and postoperative pathology indicated metastatic papillary thyroid cancer. She had her first 131I treatment after a total thyroidectomy. Subsequent whole-body imaging after 131I administration revealed 131I-avid metastases in the left parietal bone. These metastases were observed to be larger during her second 131I treatment, conducted 6 months later. Consequently, the patient was diagnosed with radioiodine-refractory differentiated thyroid cancer. 68Ga-FAPI-RGD PET/CT demonstrated higher tracer uptake and clearer lesion boundaries compared with 18F-FDG PET/CT. This suggests that 177Lu-FAPI-RGD could potentially serve as a treatment option for radioiodine-refractory differentiated thyroid cancer.

04 Sep 2024·Molecular Cancer Therapeutics

Pretargeted Radioimmunotherapy with the Novel Anti-oxMIF/HSG Bispecific Antibody ON105 Results in Significant Tumor Regression in Murine Models of Cancer

Article

Author: Thiele, Michael ; Mirkina, Irina ; Bachmann, Friedmund ; Rossmueller, Gregor ; Kerschbaumer, Randolf J. ; Puchol Tarazona, Alejandro A. ; Schinagl, Alexander

AbstractRadioimmunotherapy (RIT) uses monoclonal antibodies to deliver radionuclides to cancer cells or the tumor microenvironment and has shown promise in treating localized and diffuse tumors. Although RIT agents have gained FDA/EMA approval for certain hematologic malignancies, effectiveness of RIT in treating solid tumors remains limited. In this study, we present PreTarg-it, a novel approach for pretargeted RIT, providing optimized delivery of payloads in a two-step regimen. The effectiveness of PreTarg-it is demonstrated by a powerful combination of ON105, a novel bispecific antibody against both oxidized macrophage migration inhibitory factor (oxMIF) and the histamine-succinyl-glycyl (HSG) hapten, as the first component and the radioactively labeled DOTA-di-HSG peptide as the second component in murine models of cancer. Mice bearing either subcutaneous mouse colorectal CT26 or human pancreatic CFPAC-1 tumors received an i.v. injection of ON105. After ON105 had accumulated in the tumor and cleared from circulation to approximately 1% to 3% of its peak concentration, 177Lu-DOTA-di-HSG peptide was administered. A single PreTarg-it treatment cycle resulted in tumor regression when mice bearing CT26 tumors were given the highest treatment dose with a pretargeting delay of 3 days. Administered with a 5-day interval, the highest dose arrested tumor growth in both CT26 syngrafts and CFPAC-1 xenografts. In all cases, the highest treatment dose resulted in 100% survival at the study endpoint, whereas the control cohorts showed 0% and 60% survival in the CT26 and CFPAC-1 models, respectively. Therefore, PreTarg-it holds potential as a novel and potent therapy for patients with hard-to-treat solid tumors, such as pancreatic cancer, as well as those with late-stage malignancies.

News (Medical) associated with 177Lu-DOTA-EB-FAPI

12 May 2023

·www.prnewswire.com

First Patient Imaged in SOFIE's 18F-FAPI Phase 2 trial

DULLES, Va., May 12, 2023 /PRNewswire/ -- SOFIE Biosciences (SOFIE), an established US manufacturer and developer of radiopharmaceuticals, has dosed and imaged the first patient with [18F]FAPI-74 in its US Clinical Trial of flourine-18 labeled Fibroblast Activation Protein Inhibitor (FAPI). This study is a Phase 2, Multicenter, Non-randomized Study of [18F]FAPI-74 PET for imaging patients with gastrointestinal cancers, including hepatocellular carcinoma, cholangiocarcinoma, gastric, pancreatic and colorectal cancer (NCT05641896). The clinical trial comes after the US FDA granted SOFIE an active IND in support of this study in November of 2022. The study was launched at its first site in Boston under Principal Investigator, Shadi Esfahani, MD, MPH. Additional sites are in the process of activation and anticipated to begin recruitment in the coming weeks. Sherly Mosessian, Ph.D., SOFIE's Chief Scientific Officer, commented, "We are thrilled to see the launch of the study and imaging of the first patient in this prospective study. Tremendous promise exists in diagnostic and companion diagnostic use of FAPI family of compounds, especially in gastrointestinal cancers. Flourine-18 labeled FAPI opens up many possibilities in FAP targeting, and we are excited to be driving this product forward to unlock more of its potential." The commitment to improving patient care through utilization of radiopharmaceuticals for imaging and therapy is a professional and personal mission of SOFIE's. Frank Valla, SOFIE's Director of Clinical Development and FAPI CMC lead, added, "The promise of FAP targeting in gastrointestinal cancers and the recognition of this important milestone for patient care brings great excitement to the field as well as sense of personal fulfillment after having lost my father to Colorectal Cancer in 2007." This study is the second SOFIE FAPI product in a clinical study. SOFIE is currently conducting a Phase 2 clinical study with the lead Galium-68 labelled FAPI product, [68Ga]FAPI-46, in Pancreatic Ductal Adenocarcinoma patients (NCT05262855). About SOFIE SOFIE's vision is to improve patient outcomes by developing and delivering molecular diagnostics and therapeutics (theranostics). With its robust radiopharmaceutical production and distribution network, mature contract manufacturing services, and now, high value theranostic intellectual property, SOFIE is poised to deliver on the promise of radiopharmaceuticals. For more information, contact [email protected]. About FAPI Fibroblast Activation Protein (FAP) is highly expressed in cancer associated fibroblasts (CAF) across several tumor entities. Developed by the team at the Heidelberg University, quinoline-based PET tracers that act as FAP inhibitors (FAPI) have shown encouraging results in pre-clinical and clinical studies. SOFIE has licensed the rights for diagnostic and companion diagnostic use of FAPI family of compounds from Heidelberg University. About [18F]FAPI-74 [18F]FAPI-74 is the lead Fluorine-18 radiolabeled PET tracer of FAPI family of compounds. It has demonstrated favorable dosimetry, avidity, safety and biodistribution profile amenable for detection of FAP-expressing cells in patients with various cancers. This radioligand for imaging is currently optimized for production within SOFIE and its clinical trial partners. Media Contact: Dawn Allen [email protected] SOURCE Sofie Biosciences

Phase 2IND

17 Jan 2023

·www.prnewswire.com

IND granted for FAP targeting therapeutic in SOFIE partnership

DULLES, Va., Jan. 17, 2023 /PRNewswire/ -- SOFIE Biosciences (SOFIE), an established US manufacturer and developer of radiopharmaceuticals, will be supporting, through companion diagnostic [68Ga]FAPI-46 PET, Yantai LNC Biotechnology's recently FDA accepted clinical study. On Jan 6th, 2023 Yantai LNC Biotechnology received FDA clearance to proceed with a Phase 1 clinical study of 177Lu-LNC1004 injection, targeting fibroblast activation protein (FAP). The study accepted as part of the FDA IND review is a Phase I, open label study of the safety and dosimetry of a 4-dose regimen of escalating doses of 177Lu-LNC1004 injection in adult patients with advanced FAP-positive solid tumors. As the companion diagnostic agent of 177Lu-LNC1004 Injection, [68Ga]FAPI-46 PET will be used to screen subjects and assess therapeutic effect. Yantai obtained access to [68Ga]FAPI-46 through a letter of cross reference to SOFIE Biosciences' IND along with corresponding precursor and reference standard for use. Prof. Xiaoyuan (Shawn) Chen, co-founder of Yantai LNC Biotechnology and editor-in-chief of the journal Theranostics, stated, "we appreciate the opportunity to work closely with SOFIE in pushing the long-acting FAPI formula 177Lu-LNC1004 forward. Applying Evans blue derivatives to modify pharmacokinetics and pharmacodynamics is a platform technology Yantai LNC Biotechnology has successfully implemented to multiple radioligands such as FAP inhibitors." Sherly Mosessian, Ph.D., SOFIE's Chief Scientific Officer, added, "as license holders of FAPI family of compounds for diagnostic and companion diagnostic use, we are excited to support this very promising study by having [68Ga]FAPI-46 serve as a companion diagnostic tool for patient selection and treatment monitoring with 177Lu-LNC1004. This highlights the power of theranostics in utilizing the same target, FAP, for imaging and treatment interventions." The study is expected to enroll up to 24 subjects in advanced solid tumors that show high level of FAP expression detected by [68Ga]FAPI-46 and will establish the recommended expansion phase dose with 177Lu-LNC1004. Site feasibility and selection is complete and the study is expected to launch in Singapore Q2 2023. About Yantai LNC Biotechnology Yantai LNC Biotechnology Singapore Pte. Ltd. is a wholly owned subsidiary of Yantai Dongcheng Pharmaceutical Group. As the unique innovative nuclear medicine development platform in Dongcheng Group, Yantai LNC Biotech is committed to radionuclide diagnosis and therapy innovation. For more information, contact [email protected]. About 177Lu-LNC1004 177Lu-LNC1004 is a fibroblast activation protein inhibitor (FAPI) modified with Evans blue (EB) and a metal chelator (DOTA), radiolabeled with beta-emitting radionuclide lutetium Lu-177. As a first-in-class drug the FAP-targeting probe will be used to treat adult patients with advanced FAP-positive solid tumors. About FAPI Fibroblast Activation Protein (FAP) is highly expressed in cancer associated fibroblasts (CAF) across several tumor entities. Developed by the team at the Heidelberg University Hospital (UKHD), quinoline-based PET tracers that act as FAP inhibitors (FAPI) have shown encouraging results in pre-clinical and clinical studies. SOFIE has licensed the rights for diagnostic and companion diagnostic use of FAPI family of compounds from Heidelberg University. [68Ga]FAPI-46 is the lead gallium-68 and [18F]FAPI-74 is the lead fluorine-18 radiolabeled PET tracer of FAPI family of compounds. They have demonstrated favorable dosimetry, avidity, safety and biodistribution profile amenable for detection of FAP-expressing cells in patients with various cancers. Both products have active INDs for Phase 2 studies in cancers of the digestive system. About SOFIE SOFIE's vision is to improve patient outcomes by developing and delivering molecular diagnostics and therapeutics (theranostics). With its robust radiopharmaceutical production and distribution network, mature contract manufacturing services, and now, high value theranostic intellectual property, SOFIE is poised to deliver on the promise of radiopharmaceuticals. For more information, contact [email protected]. SOURCE SOFIE

Phase 1INDPhase 2

100 Deals associated with 177Lu-DOTA-EB-FAPI

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Solid tumor	Phase 2	CN	The First Affiliated Hospital of Xiamen University	22 Feb 2022
Follicular Adenocarcinoma	Phase 1	CN	The First Affiliated Hospital of Xiamen University	15 Jun 2022
Papillary thyroid cancer	Phase 1	CN	The First Affiliated Hospital of Xiamen University	15 Jun 2022
Refractory Thyroid Gland Carcinoma	Phase 1	CN	The First Affiliated Hospital of Xiamen University	15 Jun 2022
Thyroid Cancer, Hurthle Cell	Phase 1	CN	The First Affiliated Hospital of Xiamen University	15 Jun 2022

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