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- || Lu 177 zalsenertant tetraxetan (177Lu-IPN01087) / AstraZeneca
PK/PD data, Journal: Chelator boosted tumor-retention and pharmacokinetic properties: development of 64Cu labeled radiopharmaceuticals targeting neurotensin receptor. (Pubmed Central) - Sep 2, 2024
Through the side-by-side comparison, [64Cu]Cu-4b was identified as the lead agent for further evaluation based on its high and sustained tumor uptake and moderate liver uptake. 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.
- Lu 177 zalsenertant tetraxetan (177Lu-IPN01087) / AstraZeneca
Elucidation of the Impact of Linker Modifications on the Biological Efficacy of Antagonistic NTSR1-Targeted Radionuclide Therapeutics for Colorectal Cancer (Exhibit Hall D - Science Pavilion (Convention Center); Screen 3; In-Person Only) - May 8, 2024 - Abstract #SNMMI2024SNMMI_1581;
Substitution of aminoalkoxy-containing linkers resulted in prominent increases in renal uptake and retention. Further investigation into the impact of linker modifications in NTSR1- and other receptor-targeted antagonistic TRTs can improve the biological efficacy of agents.
- 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.
- Lu 177 zalsenertant tetraxetan (177Lu-IPN01087) / AstraZeneca
Phase classification: Study to Evaluate the Safety and Activity (Including Distribution) of 177Lu-3BP-227 in Subjects With Solid Tumours Expressing Neurotensin Receptor Type 1. (clinicaltrials.gov) - Dec 12, 2023
P1, N=14, Terminated, Sponsor: Ipsen
In addition, 177Lu-FL-091 demonstrated improved in vivo biodistribution profile vs. Phase classification: P1/2 --> P1
- | 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.
- | IPN1087 / Fusion Pharma
Journal: Positron Emission Tomography Imaging of Neurotensin Receptor-Positive Tumors with Ga-Labeled Antagonists: The Chelate Makes the Difference Again. (Pubmed Central) - Aug 27, 2021
A small molecule NTS antagonist, named [Lu]Lu-IPN01087, is currently evaluated in phase I/II clinical trials for the targeted therapy of neurotensin receptor-positive cancers...Its rapid clearance from healthy tissues led to high tumor-to-organ ratios, resulting in highly contrasted PET images. These results were confirmed on subcutaneous xenografts of AsPC-1 tumor cells, a model of NTS-positive human pancreatic adenocarcinoma.
- | Lu 177 zalsenertant tetraxetan (177Lu-IPN01087) / AstraZeneca
Enrollment change, Trial completion date, Trial termination: Study to Evaluate the Safety and Activity (Including Distribution) of 177Lu-3BP-227 in Subjects With Solid Tumours Expressing Neurotensin Receptor Type 1. (clinicaltrials.gov) - Jun 7, 2021
P1/2, N=14, Terminated, Sponsor: Ipsen
These results were confirmed on subcutaneous xenografts of AsPC-1 tumor cells, a model of NTS-positive human pancreatic adenocarcinoma. N=320 --> 14 | Trial completion date: Aug 2022 --> Apr 2021 | Recruiting --> Terminated; Due to agreement to transfer rights for IPN01087 to an external partner, not due to safety concerns
- || Lu 177 zalsenertant tetraxetan (177Lu-IPN01087) / AstraZeneca
Trial completion date: Study to Evaluate the Safety and Activity (Including Distribution) of 177Lu-3BP-227 in Subjects With Solid Tumours Expressing Neurotensin Receptor Type 1. (clinicaltrials.gov) - Feb 25, 2021
P1/2, N=320, Recruiting, Sponsor: Ipsen
N=320 --> 14 | Trial completion date: Aug 2022 --> Apr 2021 | Recruiting --> Terminated; Due to agreement to transfer rights for IPN01087 to an external partner, not due to safety concerns Trial completion date: Aug 2026 --> Aug 2022
- || Lu 177 zalsenertant tetraxetan (177Lu-IPN01087) / AstraZeneca
Trial completion date, Trial primary completion date: Study to Evaluate the Safety and Activity (Including Distribution) of 177Lu-3BP-227 in Subjects With Solid Tumours Expressing Neurotensin Receptor Type 1. (clinicaltrials.gov) - Nov 27, 2020
P1/2, N=320, Recruiting, Sponsor: Ipsen
Trial completion date: Aug 2026 --> Aug 2022 Trial completion date: Apr 2023 --> Aug 2026 | Trial primary completion date: Apr 2021 --> Aug 2021
- || Lu 177 zalsenertant tetraxetan (177Lu-IPN01087) / AstraZeneca
Trial completion date, Trial primary completion date: Study to Evaluate the Safety and Activity (Including Distribution) of 177Lu-3BP-227 in Subjects With Solid Tumours Expressing Neurotensin Receptor Type 1. (clinicaltrials.gov) - May 31, 2020
P1/2, N=320, Recruiting, Sponsor: Ipsen
Trial completion date: Apr 2023 --> Aug 2026 | Trial primary completion date: Apr 2021 --> Aug 2021 Trial completion date: Mar 2022 --> Apr 2023 | Trial primary completion date: Apr 2020 --> Apr 2021
- | 3BP-227 / Ipsen
Clinical, Journal: (177)Lu-3BP-227 for neurotensin receptor 1-targeted therapy of metastatic pancreatic adenocarcinoma - first clinical results. (Pubmed Central) - May 11, 2019
This patient survived 13 months from diagnosis and 11 months from start of (177)Lu-3BP-227 therapy. This initial report provides first clinical evidence of the feasibility of treatment of ductal pancreatic adenocarcinoma using (177)Lu-3BP-227.
- | Lu 177 zalsenertant tetraxetan (177Lu-IPN01087) / AstraZeneca
Trial completion date, Trial primary completion date: Study to Evaluate the Safety and Activity (Including Distribution) of 177Lu-3BP-227 in Subjects With Solid Tumours Expressing Neurotensin Receptor Type 1. (clinicaltrials.gov) - Nov 30, 2018
P1/2, N=320, Recruiting, Sponsor: Ipsen
This initial report provides first clinical evidence of the feasibility of treatment of ductal pancreatic adenocarcinoma using (177)Lu-3BP-227. Trial completion date: Nov 2021 --> Mar 2022 | Trial primary completion date: Sep 2021 --> Apr 2020
- |||| Lu 177 zalsenertant tetraxetan (177Lu-IPN01087) / AstraZeneca
Enrollment open: Study to Evaluate the Safety and Activity (Including Distribution) of 177Lu-3BP-227 in Subjects With Solid Tumours Expressing Neurotensin Receptor Type 1. (clinicaltrials.gov) - Jun 11, 2018
P1/2, N=300, Recruiting, Sponsor: Ipsen
Trial completion date: Nov 2021 --> Mar 2022 | Trial primary completion date: Sep 2021 --> Apr 2020 Not yet recruiting --> Recruiting
- ||||| Lu 177 zalsenertant tetraxetan (177Lu-IPN01087) / AstraZeneca
New P1/2 trial: Study to Evaluate the Safety and Activity (Including Distribution) of 177Lu-3BP-227 in Subjects With Solid Tumours Expressing Neurotensin Receptor Type 1. (clinicaltrials.gov) - May 18, 2018
P1/2, N=300, Not yet recruiting, Sponsor: Ipsen