nastorazepide (Z 360) / Zeria Pharma - LARVOL DELTA

Novel nastorazepide-based radioligands demonstrate effective cholecystokinin-2 receptor targeting with potential for theranostic applications. (PubMed, Theranostics) - "Although no significant therapeutic efficacy was observed in the tested xenograft model, the results support [177Lu]Lu-DOTAGA-NPP as a promising lead for optimization. Overall, these findings highlight the potential of Z-360-based CCK2R antagonists as scaffolds for next-generation theranostic radioligands and support their development as alternatives to minigastrin-based tracers."

Journal • Lung Cancer • Oncology • Solid Tumor • Thyroid Gland Carcinoma • Thyroid Gland Medullary Carcinoma • CCKBR • GAST

Evaluation of two Nastorazepide derived 68 Ga-labelled radiotracers for imaging of CCK2R expressing tumors. (EANM 2025) - "In vitro studies confirmed good targeting properties. The biodistribution profile and tumor uptake will be assessed in the A431-CCK2R/A431-mock xenograft model"

Gastrointestinal Cancer • Gastrointestinal Stromal Tumor • Oncology • Sarcoma • CCKBR

Potential clinical indications for a CCK2 receptor antagonist. (PubMed) - Curr Opin Pharmacol - "Netazepide and Z-360 are currently undergoing clinical development, for treatment of gastric neuroendocrine tumours and pancreatic cancer, respectively. There are several other potential indications for a CCK2RA and an unmet need."

Journal • Review • Biosimilar • Gastrointestinal Cancer • Oncology • Pancreatic Cancer

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Stereoselective pharmacokinetics of (R)-(+)- and (S)-(-)-rabeprazole in human using chiral LC-MS/MS after administration of rabeprazole sodium enteric-coated tablet. (PubMed, Chirality) - "...An API 4000 mass spectrometer was used as detector for the analysis, and the multiple reactions monitoring transitions of m/z 360.1 → 242.2 and 346.1 → 198.1 were opted for quantifying rabeprazole enantiomers and internal standard. Matrix effects were not apparent for each enantiomer and internal standard (esomeprazole), the calibration curves were linear over the concentration of 0.500 to 400 ng·mL , the intra-run precisions were below 5.4%, the inter-run precisions were below 9.9%, and the accuracy was between -9.2% and 9.3%. There was no chiral inversion observed during sample storage, preparation procedure, and analysis, demonstrating that analytes were stable in this study. This method was applied to the stereoselective pharmacokinetic study of (R)-(+)- and (S)-(-)-rabeprazole after oral administration of 10-mg rabeprazole sodium enteric-coated tablet in healthy Chinese subjects."

Journal • PK/PD data