lutetium Lu 177 rofapitide tetraxetan (AAA614) / Clovis, 3B Pharma, Novartis - LARVOL DELTA

Exploratory Analysis of [68Ga]Ga-FAP-2286 PET/CT Quantitative Parameters for Predicting Response to [177Lu]Lu-FAP-2286 Therapy in Non-small Cell Lung Cancer. (PubMed, Clin Nucl Med) - "Quantitative parameters derived from [68Ga]Ga-FAP-2286 PET/CT are valuable predictors of [177Lu]Lu-FAP-2286 treatment efficacy in NSCLC patients. Dynamic monitoring of these metrics allows for early identification of treatment responses and supports personalized therapy strategies."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • FAP

Visualization of the Gallbladder on 177Lu-FAP-2286 SPECT/CT Imaging: A Potential Pitfall. (PubMed, Clin Nucl Med) - "Following radiolabeling, FAP-2286 has demonstrated favorable diagnostic performance and promising therapeutic potential in cancer. The image illustrates the accumulation of 177Lu-FAP-2286 in the gallbladder, but correlative imaging and knowledge of the radiopharmaceutical helped to avoid a diagnostic pitfall."

Journal • Oncology • Solid Tumor

Fibroblast activation protein (FAP)-targeted dedicated breast PET for primary invasive lobular carcinoma: A pictorial review (SABCS 2025) - "After undergoing whole-body PET/CT with FAP-targeted radiotracer (6mCi +/-20% of 68Ga-FAP-2286) on a separate research protocol, they underwent dedicated breast imaging using the MAMMI dbPET scanner (OncoVision, Spain) without additional radiotracer injection...In combination with novel tracers such as FAP that may provide unique insight into the biology of primary breast tumors and drug mechanism of action, dbPET provides a cost-effective and clinically-feasibly technology that will facilitate use of PET biomarkers in clinical trials testing novel drugs in the neoadjuvant setting. Based on these preliminary results, we plan to expand our FAP-dbPET study with advanced qualitative and quantitative analyses, over time, to better measure response to therapy and ultimately to help evaluate how best to target therapy in the setting of lobular cancer."

Review • Breast Cancer • Oncology

Squaric-acid-engineered FAP2286: A next-generation 68Ga/177Lu theranostic ligand with synergistically enhanced affinity, hydrophilicity, and tumor retention. (PubMed, Bioorg Chem) - "Squaric acid derivatization synergistically elevates affinity, hydrophilicity, and intratumoral residence while preserving safety, establishing 68Ga/177Lu-FAP2286-SA as a clinically translatable, next-generation theranostic pair for FAP-positive malignancies."

Journal • Hematological Disorders • Oncology • FAP

Revisiting the Segmentation Threshold for Lu-177 SPECT (EANM 2025) - "1) Sphere-to-background ratios (SBRs): no background, 10:1, 5:1, 3.5:1 and 2:1 Phantom SPECT acquisitions Digital Jaszczak phantom 120 realistic noisy projections from SIMIND Monte Carlo simulation Physical Jaszczak phantom Dual-head NaI(Tl) SPECT system (Symbia T16, Siemens Healthineers, Germany) 120 projections, 25 s per view Fixed radius-of-rotation (ROR) of 24 cm 99m Tc imaging Primary energy window centered at 140 keV with a 15% window width (129.3-150.3 keV) A scatter window at 108.4-129.3 keV for the dual energy window scatter correction (SC) Low-energy high-resolution parallel hole collimators 177 Lu imaging Primary energy window centered at 208 keV with a 15% window width (192.4-223.6 keV) Two scatter windows at 161.2-192.4 keV and 223.6-244.4 keV for the triple energy window SC Medium energy general purpose parallel hole collimators Image reconstruction Filtered back projection (FBP) with Butterworth filter (cutoff frequency: 0.4, order 8 for 99m Tc; cutoff..."

A preliminary study on the safety and efficacy of 177Lu-FAP-2286 in gastrointestinal tumours with positive FAP expression. (PubMed, Radiother Oncol) - "177Lu-FAP-2286 demonstrated good feasibility and safety in treating FAP-positive gastrointestinal tumors, resulting in disease stabilization in a subset of patients."

Journal • Gastrointestinal Cancer • Oncology • Solid Tumor • FAP

Innovative Peptide Therapeutics in the Pipeline: Transforming Cancer Detection and Treatment. (PubMed, Int J Mol Sci) - "Innovative peptide platforms now enable three transformative applications: (1) precision molecular diagnostics (e.g., 18F-PSMA-1007 for prostate cancer detection), (2) targeted therapies (e.g., BT5528 and SAR408701 targeting tumour-specific antigens), and (3) theranostic systems (e.g., RAYZ-8009 and 177Lu-FAP-2286 integrating imaging and radiotherapy). By overcoming current limitations, peptide drugs are poised to redefine cancer management, offering safer, more effective alternatives to conventional therapies. Their integration into clinical practice could mark a critical milestone in achieving precision oncology."

IO biomarker • Journal • Review • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

An exploratory study of 177Lu-FAP-2286 combined with 177Lu-TBM-001 in the treatment of solid tumors with bone metastasis (ChiCTR) - P=N/A | N=30 | Recruiting | Sponsor: The affiliated hospital of southwest medical university; The affiliated hospital of southwest medical university

New trial • Oncology • Solid Tumor

Preclinical evaluation, and clinical translation of 68Ga/177Lu-JH04, a novel FAP-targeting radiolabeled agent (AACR 2025) - "The objective of this study is to evaluate the specificity, biodistribution, pharmacokinetics, and dosimetry of 68Ga/177Lu-JH04 through preclinical and preliminary clinical investigations, and to compare these findings with those of 68Ga/177Lu-FAP-2286. The FAP-positive cell line HT1080-FAP was employed in in vitro and in vivo studies. 68Ga/177Lu-JH04, novel FAP-targeting agent with excellent binding affinity, high tumor uptake, prolonged retention, and robust tumor-suppressive effects. These promising results encourage us to conduct further clinical research."

Preclinical • Oncology • FAP

FAUNUS: 177Lu-FAP-2286 Treatment in Urethelial Neoplasms: Utility and Safety as a Novel Treatment. (clinicaltrials.gov) - P2 | N=10 | Not yet recruiting | Sponsor: Ankara University

New P2 trial • Oncology

177Lu-FAP-2286 Therapy in a Case of Squamous Lung Cancer. (PubMed, Clin Nucl Med) - "Radiological remission was observed on follow-up FAP imaging 7 months later with squamous cell carcinoma antigen decreased to normal level. No other abnormality monitored by routine laboratory examination was noted."

Journal • Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma

Comprehensive Preclinical Study and Administration Protocol for 177Lu-FAP-2286: Validation, Tumor Uptake, and Dosimetry Investigations (EANM 2024) - "The validation of production and quality control processes for 177Lu-FAP-2286, along with the comprehensive preclinical studies and dosimetry investigations, demonstrate the potential for effective clinical translation. The use of lysine and arginine for kidney blockage, in combination with furosemide, shows promise in minimizing background activity in normal organs."

Preclinical • Oncology

Development of Multivalent OncoFAP Derivatives for the Tumor-Targeted Delivery of Theranostic Radionuclides (EANM 2024) - "When compared to 177Lu-FAP-2286, the most advanced FAP-targeted RLT in clinical development, 177Lu-TriOncoFAP exhibited a ~2.7-fold higher overall uptake in tumors, with a ~1.8-fold lower kidney uptake... The data presented in this work strongly supports the clinical development of 177Lu-TriOncoFAP. We are launching a Phase I clinical trial to define the 177Lu-TriOncoFAP maximum tolerated dose, evaluating its safety profile, and collecting preliminary signs of efficacy. The compound will be given as single agent or in combination with L19-IL2 in patients with multiple types of FAP-positive tumors."

Oncology • Solid Tumor • FAP • IL2

Initial experience with 177Lu-FAP-2286 peptide targeted radionuclide therapy in advanced solid tumors (EANM 2024) - " Treatment protocol: Patients were pre-medicated with I.V. ondansetron, pantoprazole & Dexamethasone. 177Lu-FAP-2286 PTRT seems to be a viable therapeutic option for FAP-positive tumors. However, due to variability in objective response, use in combination with single-agent chemo or immunotherapeutic agent is to be explored for better results."

Metastases • Endometrial Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pain • Solid Tumor • Triple Negative Breast Cancer • FAP • PD-L1

Preclinical Evaluation of 177Lu-OncoFAP-23, a Multivalent FAP-Targeted Radiopharmaceutical Therapeutic for Solid Tumors. (PubMed, J Nucl Med) - "177Lu-OncoFAP and 177Lu-FAP-2286 were included in the biodistribution study as controls. OncoFAP-23 presents enhanced tumor uptake and tumor retention and low accumulation in healthy organs, findings that correspond to a strongly improved in vivo antitumor efficacy. The data presented in this work support the clinical development of 177Lu-OncoFAP-23 for the treatment of FAP-positive solid tumors."

Journal • Preclinical • Oncology • Solid Tumor • FAP

A Study of 177Lu-FAP-2286 in Advanced Solid Tumors (LuMIERE) (clinicaltrials.gov) - P1/2 | N=222 | Recruiting | Sponsor: Novartis Pharmaceuticals | Active, not recruiting ➔ Recruiting

Enrollment open • Metastases • Oncology • Solid Tumor • FAP

Efficacy and Safety Evaluation of 177Lu-FAP-2286 in the Treatment of Advanced Lung Cancer. (PubMed, Clin Nucl Med) - "177Lu-FAP-2286 has the potential to be a viable PTRT option for patients with advanced lung cancer."

Clinical • Journal • Metastases • Lung Cancer • Metabolic Disorders • Oncology • Pain • Pulmonary Disease • Solid Tumor

Feasibility and therapeutic potential of [177Lu]Lu-FAPI-2286 in patients with advanced metastatic sarcoma. (PubMed, Eur J Nucl Med Mol Imaging) - "[177Lu]Lu-FAPI-2286 PTRT, utilized for diverse cancer types, exhibited favorable tolerability in sarcoma patients, with minimal side effects, long-lasting retention of the radiopeptide within the tumor, and promising therapeutic effects. Preliminary findings of this prospective study need to be confirmed through further clinical trials."

Journal • Metastases • Oncology • Pain • Sarcoma • Solid Tumor

Comparison of 68Ga-FAP-2286 and 18F-FDG PET/CT in the diagnosis of advanced lung cancer. (PubMed, Front Oncol) - "However, the detection sensitivity for primary tumors using both modalities was comparable [100% (13/13) for both]. Compared to 18F-FDG PET/CT, 68Ga-FAP-2286 PET/CT demonstrated better lesion detection capabilities for lung cancer, particularly in lymph nodes and bone metastases, providing compelling imaging evidence for the efficacy of 177Lu-FAP-2286 treatment."

FDG PET • Journal • Metastases • Lung Cancer • Oncology • Solid Tumor

Development of Multivalent OncoFAP Derivatives for the Tumor-Targeted Delivery of Theranostic Radionuclides (SNMMI 2024) - "When compared to 177Lu-FAP-2286, the most advanced FAP-targeted RLT in clinical development, 177Lu-TriOncoFAP exhibited a ~2... The data presented in this work strongly supports the clinical development of 177Lu-TriOncoFAP. We have recently completed GMP central labeling set-up. Philogen is launching a Phase I clinical trial to define the 177Lu-TriOncoFAP maximum tolerated dose, evaluating its safety profile, and collecting preliminary signs of efficacy."

Hepatology • Oncology • Solid Tumor • FAP • IL2

177Lu-FAP-2286 Therapy in a Patient With Metastatic Rhabdoid Meningioma. (PubMed, Clin Nucl Med) - "Herein, we reported a patient of rhabdoid meningioma with multiple liver, pancreas, and bone metastases, who received 177Lu-FAP-2286 therapy. After 1 treatment cycle, 68Ga-FAP-2286 PET/CT revealed partial remission of the lesions."

Journal • Metastases • Brain Cancer • CNS Tumor • Meningioma • Oncology • Pancreatic Cancer • Solid Tumor

Metastatic Lung Adenocarcinoma Received Combined 177Lu-FAP-2286 Radiation Therapy and Targeted Therapy. (PubMed, Clin Nucl Med) - "After 1 treatment cycle, improvement of symptoms and radiological remission was observed. Moreover, the patient did not report any adverse effects."

Journal • Metastases • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

177Lu-FAP-2286 Therapy in a Metastatic Bone Malignant Solitary Fibrous Tumor. (PubMed, Clin Nucl Med) - "After 1 treatment cycle, 68Ga-FAP-2286 PET/CT revealed remission of the lesions. Moreover, the patient did not report any adverse effects."

Journal • Metastases • Oncology

A Study of 177Lu-FAP-2286 in Advanced Solid Tumors (LuMIERE) (clinicaltrials.gov) - P1/2 | N=222 | Active, not recruiting | Sponsor: Novartis Pharmaceuticals | Recruiting ➔ Active, not recruiting

Enrollment closed • Oncology • Solid Tumor • FAP

177Lu-FAP-2286 Therapy in a Case of Recurrent Bladder Cancer With Multiple Metastatic Lesions. (PubMed, Clin Nucl Med) - "Encouragingly, radiological remission and alleviation of his symptom were noted. In addition, the patient did not have any adverse effects."

Journal • Metastases • Bladder Cancer • Genito-urinary Cancer • Oncology • Solid Tumor