Trop2 exhibits significantly elevated expression in numerous solid malignancies, playing a crucial role in tumor advancement, whereas its presence in healthy tissues is minimal. In this study, we investigated Trop2 expression in bladder cancer models using [Cu]Cu-NOTA-Trodelvy for immunoPET imaging. In HT-1376 models, [Cu]Cu-NOTA-Trodelvy effectively visualized tumor as early as 12 h p.i. (10.30 ± 1.45% ID/g), with tumor uptake increasing and peaking at 48 h p.i. (13.73 ± 1.16% ID/g), highlighting its potential for tumor imaging. Control groups also demonstrated low tumor uptake (5.27 ± 1.14% ID/g at 48 h in the blocking group; 6.33 ± 0.74% ID/g at 48 h in UM-UC-3; 4.50 ± 0.30% ID/g at 48 h in the [Cu]Cu-NOTA-IgG group). Long-term fluorescence imaging further confirmed the tumor uptake rate in the IRDye 800CW-Trodelvy group was significantly higher than in the IRDye 800CW-Trodelvy blockade group ( < 0.001). Our findings demonstrated that [Cu]Cu-NOTA-Trodelvy enables specific and prolonged tumor accumulation in bladder cancer models, providing precise and noninvasive monitoring of Trop2 expression.
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http://dx.doi.org/10.1021/acs.molpharmaceut.5c00069 | DOI Listing |
Clin Lung Cancer
February 2025
The Helmsley Cancer Center, The Hebrew University of Jerusalem Shaare Zedek Medical Center Shmuel Beit 12, Jerusalem, Israel. Electronic address:
Introduction: Despite recent advances in immunotherapy combinations for extensive-stage small cell lung cancer (ES-SCLC), rapid disease progression following chemotherapy discontinuation remains a significant challenge. While the addition of pembrolizumab to platinum-etoposide has demonstrated a modest improvement in progression-free survival (PFS), there is an urgent need for more effective maintenance strategies. Sacituzumab govitecan (SG), an antibody-drug conjugate targeting Trop-2, has shown promising activity in pretreated ES-SCLC.
View Article and Find Full Text PDFCancer Med
March 2025
Translational Research Unit, Montpellier Cancer Institute Val d'Aurelle, Montpellier, France.
Introduction: Triple-Negative Breast Cancer (TNBC) is an aggressive breast cancer subtype, in which targeting the Trophoblast cell-surface antigen-2 (Trop-2), using antibody-drug conjugates (ADC), results in significant clinical improvement. However, clinicopathological correlations with Trop-2 protein expression levels remain limited in TNBC patients.
Methods: Here we assessed by immunohistochemistry (IHC) using the mouse monoclonal anti-Trop-2 antibody (Enzo, Cat.
Mol Pharm
March 2025
Departments of Radiology and Medical Physics, University of Wisconsin - Madison, Madison, Wisconsin 53705, United States.
Trop2 exhibits significantly elevated expression in numerous solid malignancies, playing a crucial role in tumor advancement, whereas its presence in healthy tissues is minimal. In this study, we investigated Trop2 expression in bladder cancer models using [Cu]Cu-NOTA-Trodelvy for immunoPET imaging. In HT-1376 models, [Cu]Cu-NOTA-Trodelvy effectively visualized tumor as early as 12 h p.
View Article and Find Full Text PDFMol Cancer Ther
March 2025
The University of Texas Health Science Center at Houston, Houston, TX, United States.
To explore the potential of site-selectively radiolabeled antibody-drug conjugates (ADCs) against solid tumors, we constructed and evaluated radiolabeled ADCs equipped with lutetium-177 (177Lu) and a membrane permeable antimitotic agent. Site-selective 177Lu-labeled ADCs (anti-TROP2 177Lu-DTPA ADCs or anti-HER2 177Lu-DO3A ADCs), a 177Lu-labeled homogenous radioimmunoconjugate (homogeneous RIC), and 177Lu-labeled conventional RIC (heterogeneous RIC) were constructed. We confirmed that 177Lu-labeled ADCs and the homogeneous RIC were obtained with high homogeneity and defined chelator/payload-to-antibody ratios.
View Article and Find Full Text PDFJ Nanobiotechnology
March 2025
Institute of Molecular Medicine (IMM), Shanghai Key Laboratory for Nucleic Acid Chemistry and Nanomedicine, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, 200240, China.
Recent advancements in antibody-drug conjugates (ADCs) targeting trophoblast surface cell antigen 2 (Trop-2) have brought important progress in the field of targeted therapy. This progress also holds promise for the treatment of small cell lung cancer (SCLC) as anti-Trop-2 therapy appears to have a safe and effective clinical activity in metastatic SCLC patients. However, effective treatments of anti-Trop-2 ADCs rely on the comprehensive assessment of Trop-2 expression at the tumor sites, SCLC exhibits intratumoral heterogeneity, making the accurate acquisition of histological biopsies a challenge.
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