^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG:

Debio 0228

i
Other names: Debio 0228, [177Lu]Lu-DPI-4452, 3B-301
Associations
Company:
3B Pharma, Debiopharm
Drug class:
Ionizing radiation emitter, Carbonic anhydrase IX inhibitor
Related drugs:
Associations
2ms
Preclinical Characterization of DPI-4452: A 68Ga/177Lu Theranostic Ligand for Carbonic Anhydrase IX. (PubMed, J Nucl Med)
[177Lu]Lu-DPI-4452 demonstrated strong tumor growth inhibition in 2 xenograft mouse models. Thus, the 2 agents potentially provide a theranostic approach for selecting and treating patients with CAIX-expressing tumors such as ccRCC, CRC, and pancreatic ductal adenocarcinoma.
Preclinical • Journal
|
VHL (von Hippel-Lindau tumor suppressor) • CA9 (Carbonic anhydrase 9)
|
VHL mutation • CA9 overexpression • CA9 expression
|
Debio 0228
2ms
First-in-Human Safety, Imaging, and Dosimetry of a Carbonic Anhydrase IX-Targeting Peptide, [68Ga]Ga-DPI-4452, in Patients with Clear Cell Renal Cell Carcinoma. (PubMed, J Nucl Med)
[68Ga]Ga-DPI-4452, a first-in-class carbonic anhydrase IX-binding radiolabeled peptide, is the imaging agent of a theranostic pair with [177Lu]Lu-DPI-4452, developed for selecting and treating patients with carbonic anhydrase IX-expressing tumors...No clinically significant toxicity was observed. [68Ga]Ga-DPI-4452 showed exceptional tumor uptake in patients with clear cell renal cell carcinoma, with very high tumor-to-background ratios and no significant adverse events, suggesting potential diagnostic and patient selection applications.
P1 data • Journal
|
CA9 (Carbonic anhydrase 9)
|
Debio 0228
5ms
First-in-human safety, imaging and dosimetry of [68Ga]Ga-DPI-4452, a novel CA IX-targeting peptide, in patients with clear cell renal cell carcinoma. (ASCO-GU 2024)
[68Ga]Ga-DPI-4452 provides exceptional images in patients with ccRCC without clinically significant toxicity. Very high SUVs and tumor-to-background ratios suggest potential for use in both diagnostics and patient selection for therapy. The tumor retention and rapid elimination support potential of [177Lu]Lu-DPI-4452 radioligand therapy.
Clinical • P1 data
|
CA9 (Carbonic anhydrase 9)
|
CA9 overexpression • CA9 expression
|
Debio 0228