Delving into the Latest Updates on 177Lu-DOTA-EB-FAPI with Synapse

Overview

Basic Info

Drug Type

Radionuclide Drug Conjugates (RDC), Therapeutic radiopharmaceuticals

Synonyms-

Target

FAP

Mechanism

FAP antagonists(Fibroblast activation protein alpha antagonists), Ionising radiation emitters

Therapeutic Areas

NeoplasmsRespiratory DiseasesEndocrinology and Metabolic Disease+ [1]

Active Indication

progressive non-small cell lung cancerFollicular AdenocarcinomaPapillary thyroid cancer+ [2]

Inactive Indication-

Originator Organization

The First Affiliated Hospital of Xiamen University

Active Organization

The First Affiliated Hospital of Xiamen University

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

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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

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

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

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15

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

01 Dec 2024·Clinical Nuclear Medicine

Biodistribution and Radiation Dosimetry for 68Ga-DOTA-CCK-66, a Novel CCK2R-Targeting Compound for Imaging of Medullary Thyroid Cancer

Article

Author: Günther, Thomas ; Kircher, Malte ; Wienand, Georgine ; Pfob, Christian H. ; Rinscheid, Andreas ; Dierks, Alexander ; Holzleitner, Nadine ; Lapa, Constantin ; Viering, Oliver ; Wester, Hans-Jürgen ; Patt, Marianne ; Bundschuh, Ralph A.

AbstractCholecystokinin 2 receptor (CCK2R) is a promising target for imaging and treatment of medullary thyroid cancer due to its overexpression in over 90% of tumor cells. 68Ga-DOTA-CCK-66 is a recently introduced PET tracer selective for CCK2R, which has shown favorable pharmacokinetics in vivo in preclinical experiments. In order to further investigate safety and suitability of this tracer in the human setting, whole-body distribution and radiation dosimetry were evaluated.Patients and MethodsSix patients with a history of medullary thyroid cancer were injected intravenously with 169 ± 19 MBq of 68Ga-DOTA-CCK-66. Whole-body PET/CT scans were acquired at 10 minutes, 1 hour, 2 hours, and 4 hours after tracer injection. Time-activity curves per organ were determined, and mean organ-absorbed doses and effective doses were calculated using OLINDA/EXM.ResultsInjection of a standard activity of 150 MBq of 68Ga-DOTA-CCK-66 results in an effective dose of 4.5 ± 0.9 mSv. The highest absorbed organ doses were observed in the urinary bladder wall (40 mGy) and the stomach (15 mGy), followed by the kidneys (6 mGy), as well as the liver and the spleen (3 mGy each). CCK2R-expressing tumor manifestations could be detected in 2 of the 6 patients, including lymph node, bone, and liver metastases.Conclusions68Ga-DOTA-CCK-66 exhibits a favorable dosimetry. Beyond physiologic receptor expression of the stomach, no other relevant tracer accumulation could be observed, rendering this organ at risk in case of subsequent radioligand therapy using 177Lu-DOTA-CCK-66.

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.

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

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
progressive non-small cell lung cancer	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