- |||||||||| actinium-225 zalsenertant tetraxetan (225Ac-FPI-2059) / 3B Pharma, AstraZeneca
Enrollment closed: A Study of [225Ac]-FPI-2059 in Adult Participants With Solid Tumours (clinicaltrials.gov) - Jan 28, 2025 P1, N=42, Active, not recruiting, Examination of the therapeutic potential of [177Lu]Lu-NA-ET1 and further exploration of the chemical biology of this approach is underway. Recruiting --> Active, not recruiting
- |||||||||| AAA614 / 3B Pharma, Novartis
Journal: 177Lu-FAP-2286 Therapy in a Case of Squamous Lung Cancer. (Pubmed Central) - Dec 3, 2024 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.
- |||||||||| AAA614 / 3B Pharma, Novartis
Journal, Metastases: Feasibility and therapeutic potential of [177Lu]Lu-FAPI-2286 in patients with advanced metastatic sarcoma. (Pubmed Central) - Nov 26, 2024 [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.
- |||||||||| AAA614 / 3B Pharma, Novartis
Enrollment open: LuMIERE: A Study of 177Lu-FAP-2286 in Advanced Solid Tumors (clinicaltrials.gov) - Aug 14, 2024 P1/2, N=222, Recruiting, It can not only be used to efficiently detect NTSR1 expression in lung cancer (for diagnosis, patient screening, and treatment monitoring), but also has the great potential to treat NTSR-positive lesions once chelating to the beta emitter 67Cu. Active, not recruiting --> Recruiting
- |||||||||| AAA614 / 3B Pharma, Novartis
Journal, Metastases: 177Lu-FAP-2286 Therapy in a Patient With Metastatic Rhabdoid Meningioma. (Pubmed Central) - Aug 5, 2024 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.
- |||||||||| ITM-91 / 3B Pharma, ITM Isotopen Technologien Munchen
Trial completion date, Trial primary completion date, Metastases: GaLuCi: A Study to Assess Safety, Tolerability and Imaging Characteristics of [68Ga]Ga-DPI-4452 and to Assess Safety, Tolerability, and Efficacy of [177Lu]Lu-DPI-4452 in Participants With Unresectable Locally Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - Jul 17, 2024 P1/2, N=170, Recruiting, After 1 treatment cycle, 68Ga-FAP-2286 PET/CT revealed partial remission of the lesions. Trial completion date: Jan 2027 --> Mar 2029 | Trial primary completion date: Jan 2026 --> Jun 2027
- |||||||||| AAA614 / 3B Pharma, Novartis
Journal, FDG PET, Metastases: Comparison of 68Ga-FAP-2286 and 18F-FDG PET/CT in the diagnosis of advanced lung cancer. (Pubmed Central) - Jul 16, 2024 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.
- |||||||||| NTSR1 targeted radiopharmaceutical therapeutic - Full / Life Technologies Limited
Development of 177Lu-FL-091 for the treatment of NTSR1-positive cancers (717AB (Convention Center); In-Person) - May 8, 2024 - Abstract #SNMMI2024SNMMI_1231; FL-091 displayed enhanced binding affinity to NTST1 and antagonist activity compared to 3BP-227. In addition, 177Lu-FL-091 demonstrated improved in vivo biodistribution profile vs.
- |||||||||| AAA614 / 3B Pharma, Novartis
Enrollment closed, Trial completion date, Trial primary completion date: LuMIERE: A Study of 177Lu-FAP-2286 in Advanced Solid Tumors (clinicaltrials.gov) - Feb 6, 2024 P1/2, N=222, Active, not recruiting, Moreover, the patient did not report any adverse effects. Recruiting --> Active, not recruiting | Trial completion date: Jun 2026 --> Jun 2028 | Trial primary completion date: Jul 2024 --> Jun 2026
- |||||||||| actinium-225 zalsenertant tetraxetan (225Ac-FPI-2059) / Fusion Pharma, 3B Pharma
NTSR1-targeted alpha therapeutic [Ac-225]-FPI-2059 induces growth inhibition in a preclinical colorectal tumor model (Section 19; Poster Board #12) - Mar 14, 2023 - Abstract #AACR2023AACR_7275; Radiolabeling DPI-4452 with gallium-68 ([68Ga]Ga-DPI-4452) or lutetium-177 ([177Lu]Lu-DPI-4452) is an innovative theranostic approach for identifying and treating patients (pts) with CA IX-expressing tumors...Eur J Nucl Med Mol Imaging 2022;49(Suppl 1):S1 These results demonstrate that targeted delivery of [225Ac]-FPI-2059 to NTSR1 expressing tumors results in significant growth inhibition and enhanced survival, thereby providing promising preclinical evidence to support the clinical development of [225Ac]-FPI-2059.
- |||||||||| IPN1087 / Fusion Pharma
Journal: Examination of Charge Modifications of an Endolysosomal Trapping Inhibitor in an Antagonistic NTSR1-Targeted Construct for Colon Cancer. (Pubmed Central) - Jul 23, 2022 These four Lu-labeled, ET-enhanced, NTSR1-targeted agents (Lu-NA-ET1-4), along with the structurally analogous Lu-3BP-227, currently in clinical trials, underwent a battery of in vitro assays using HT-29 xenograft colon cancer cells to examine their NTSR1 binding, internalization and efflux, inhibition, and adduct formation properties...This study demonstrates that the ETs can be successfully incorporated into antagonistic NTSR1-targeted constructs without compromising their adduct formation capabilities. Based on these results, further exploration of the endolysosomal trapping approach is warranted in NTSR1- and other receptor-targeted antagonistic constructs.
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