Transformative Nanomedicine of an Amphiphilic Camptothecin Prodrug for Long Circulation and High Tumor Uptake in Cancer Therapy

ACS Nano ◽  
2017 ◽  
Vol 11 (9) ◽  
pp. 8838-8848 ◽  
Author(s):  
Fuwu Zhang ◽  
Guizhi Zhu ◽  
Orit Jacobson ◽  
Yi Liu ◽  
Kai Chen ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Tumor Uptake ◽  
High Tumor Uptake

Honokiol Prodrug Nanoparticles Based on In Situ Albumin Binding for Long Circulation and High Tumor Uptake

2021 ◽  
Vol 12 (10) ◽  
pp. 1589-1595
Author(s):  
Lixue Chen ◽  
Shengnan Li ◽  
Yanfang Ding ◽  
Changyuan Wang ◽  
Sitong Zhang ◽  
...  
Keyword(s):  
Albumin Binding ◽  
Tumor Uptake ◽  
High Tumor Uptake

scholarly journals Comparative Radioimmunotherapy of Experimental Melanoma with Novel Humanized Antibody to Melanin Labeled with 213Bismuth and 177Lutetium

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 348 ◽  
Author(s):  
Kevin J. H. Allen ◽  
Rubin Jiao ◽  
Mackenzie E. Malo ◽  
Connor Frank ◽  
Darrell R. Fisher ◽  
...  
Keyword(s):  
Metastatic Melanoma ◽  
Ct Imaging ◽  
Whole Body ◽  
Tumor Uptake ◽  
Slowing Down ◽  
Humanized Antibody ◽  
Alpha Emitter ◽  
Systemic Side Effects ◽  
High Tumor Uptake ◽  
Dosimetry Data

Melanoma is a cancer with increasing incidence and there is a need for alternatives to immunotherapy within effective approaches to treatment of metastatic melanoma. We performed comparative radioimmunotherapy (RIT) of experimental B16-F10 melanoma with novel humanized IgG to melanin h8C3 labeled with a beta emitter, 177Lu, and an alpha-emitter, 213Bi, as well as biodistribution, microSPECT/CT imaging, and mouse and human dosimetry calculations. microSPECT/CT imaging showed that a humanized antibody that targets “free” melanin in the tumor microenvironment had high tumor uptake in B16F10 murine melanoma in C57Bl/6 mice, with little to no uptake in naturally melanized tissues. Extrapolation of the mouse dosimetry data to an adult human demonstrated that doses delivered to major organs and the whole body by 177Lu-h8C3 would be approximately two times higher than those delivered by 213Bi-h8C3, while the doses to the tumor would be almost similar. RIT results indicated that 213Bi-h8C3 was more effective in slowing down the tumor growth than 177Lu-h8C3, while both radiolabeled antibodies did not produce significant hematologic or systemic side effects. We concluded that h8C3 antibody labeled with 213Bi is a promising reagent for translation into a clinical trial in patients with metastatic melanoma.

scholarly journals Noninvasive brain cancer imaging with a bispecific antibody fragment, generated via click chemistry

2015 ◽  
Vol 112 (41) ◽  
pp. 12806-12811 ◽  
Author(s):  
Haiming Luo ◽  
Reinier Hernandez ◽  
Hao Hong ◽  
Stephen A. Graves ◽  
Yunan Yang ◽  
...  
Keyword(s):  
Early Detection ◽  
Near Infrared ◽  
Bispecific Antibody ◽  
Growth Factor Receptor ◽  
Antibody Fragment ◽  
Tumor Uptake ◽  
High Tumor Uptake ◽  
Epidermal Growth ◽  
Detection And Diagnosis ◽  
Near Infrared Fluorescence Imaging

Early diagnosis remains a task of upmost importance for reducing cancer morbidity and mortality. Successful development of highly specific companion diagnostics targeting aberrant molecular pathways of cancer is needed for sensitive detection, accurate diagnosis, and opportune therapeutic intervention. Herein, we generated a bispecific immunoconjugate [denoted as Bs-F(ab)2] by linking two antibody Fab fragments, an anti-epidermal growth factor receptor (EGFR) Fab and an anti-CD105 Fab, via bioorthogonal “click” ligation of trans-cyclooctene and tetrazine. PET imaging of mice bearing U87MG (EGFR/CD105+/+) tumors with 64Cu-labeled Bs-F(ab)2 revealed a significantly enhanced tumor uptake [42.9 ± 9.5 percentage injected dose per gram (%ID/g); n = 4] and tumor-to-background ratio (tumor/muscle ratio of 120.2 ± 44.4 at 36 h postinjection; n = 4) compared with each monospecific Fab tracer. Thus, we demonstrated that dual targeting of EGFR and CD105 provides a synergistic improvement on both affinity and specificity of 64Cu-NOTA-Bs-F(ab)2. 64Cu-NOTA-Bs-F(ab)2 was able to visualize small U87MG tumor nodules (<5 mm in diameter), owing to high tumor uptake (31.4 ± 10.8%ID/g at 36 h postinjection) and a tumor/muscle ratio of 76.4 ± 52.3, which provided excellent sensitivity for early detection. Finally, we successfully confirmed the feasibility of a ZW800-1–labeled Bs-F(ab)2 for near-infrared fluorescence imaging and image-guided surgical resection of U87MG tumors. More importantly, our rationale can be used in the construction of other disease-targeting bispecific antibody fragments for early detection and diagnosis of small malignant lesions.

scholarly journals [18F]Fluoroethyltriazolyl Monocyclam Derivatives as Imaging Probes for the Chemokine Receptor CXCR4

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1612 ◽  
Author(s):  
Alejandro Amor-Coarasa ◽  
James M. Kelly ◽  
Pradeep K. Singh ◽  
Shashikanth Ponnala ◽  
Anastasia Nikolopoulou ◽  
...  
Keyword(s):  
Chemokine Receptor ◽  
Cxcr4 Expression ◽  
Tumor Uptake ◽  
Multiple Tumor ◽  
Chemokine Receptor Cxcr4 ◽  
Positron Emission ◽  
Imaging Probes ◽  
High Tumor Uptake ◽  
Tumor Types

Determining chemokine receptor CXCR4 expression is significant in multiple diseases due to its role in promoting inflammation, cell migration and tumorigenesis. [68Ga]Pentixafor is a promising ligand for imaging CXCR4 expression in multiple tumor types, but its utility is limited by the physical properties of 68Ga. We screened a library of >200 fluorine-containing structural derivatives of AMD-3465 to identify promising candidates for in vivo imaging of CXCR4 expression by positron emission tomography (PET). Compounds containing fluoroethyltriazoles consistently achieved higher docking scores. Six of these higher scoring compounds were radiolabeled by click chemistry and evaluated in PC3-CXCR4 cells and BALB/c mice bearing bilateral PC3-WT and PC3-CXCR4 xenograft tumors. The apparent CXCR4 affinity of the ligands was relatively low, but tumor uptake was CXCR4-specific. The tumor uptake of [18F]RPS-534 (7.2 ± 0.3 %ID/g) and [18F]RPS-547 (3.1 ± 0.5 %ID/g) at 1 h p.i. was highest, leading to high tumor-to-blood, tumor-to-muscle, and tumor-to-lung ratios. Total cell-associated activity better predicted in vivo tumor uptake than did the docking score or apparent CXCR4 affinity. By this metric, and on the basis of their high yielding radiosynthesis, high tumor uptake, and good contrast to background, [18F]RPS-547, and especially [18F]RPS-534, are promising 18F-labeled candidates for imaging CXCR4 expression.

scholarly journals A Bivalent Inhibitor of Prostate Specific Membrane Antigen Radiolabeled with Copper‐64 with High Tumor Uptake and Retention

2019 ◽  
Vol 58 (42) ◽  
pp. 14991-14994 ◽  
Author(s):  
Nicholas A. Zia ◽  
Carleen Cullinane ◽  
Jessica K. Van Zuylekom ◽  
Kelly Waldeck ◽  
Lachlan E. McInnes ◽  
...  
Keyword(s):  
Prostate Specific Membrane Antigen ◽  
Tumor Uptake ◽  
High Tumor Uptake ◽  
Specific Membrane

99mTcO(MAG2-3G3-dimer): a new integrin αvβ3-targeted SPECT radiotracer with high tumor uptake and favorable pharmacokinetics

2009 ◽  
Vol 36 (11) ◽  
pp. 1874-1884 ◽  
Author(s):  
Jiyun Shi ◽  
Lijun Wang ◽  
Young-Seung Kim ◽  
Shizhen Zhai ◽  
Bing Jia ◽  
...  
Keyword(s):  
Integrin Αvβ3 ◽  
Tumor Uptake ◽  
High Tumor Uptake

scholarly journals A Bivalent Inhibitor of Prostate Specific Membrane Antigen Radiolabeled with Copper‐64 with High Tumor Uptake and Retention

2019 ◽  
Vol 131 (42) ◽  
pp. 15133-15136
Author(s):  
Nicholas A. Zia ◽  
Carleen Cullinane ◽  
Jessica K. Van Zuylekom ◽  
Kelly Waldeck ◽  
Lachlan E. McInnes ◽  
...  
Keyword(s):  
Prostate Specific Membrane Antigen ◽  
Tumor Uptake ◽  
High Tumor Uptake ◽  
Specific Membrane

scholarly journals Ultrasmall Glutathione-Protected Gold Nanoclusters as Next Generation Radiotherapy Sensitizers with High Tumor Uptake and High Renal Clearance

2015 ◽  
Vol 5 (1) ◽  
Author(s):  
Xiao-Dong Zhang ◽  
Zhentao Luo ◽  
Jie Chen ◽  
Shasha Song ◽  
Xun Yuan ◽  
...  
Keyword(s):  
Renal Clearance ◽  
Gold Nanoclusters ◽  
Tumor Uptake ◽  
Next Generation ◽  
High Tumor Uptake

Synthesis and characterization of 18F-labeled hydrazinocurcumin derivatives for tumor imaging

RSC Advances ◽  
2015 ◽  
Vol 5 (117) ◽  
pp. 96733-96745 ◽  
Author(s):  
Sarah Shin ◽  
Hyun-Jung Koo ◽  
Iljung Lee ◽  
Yearn Seong Choe ◽  
Joon Young Choi ◽  
...  
Keyword(s):  
Tumor Imaging ◽  
C6 Glioma ◽  
Synthesis And Characterization ◽  
Tumor Uptake ◽  
High Tumor Uptake ◽  
Reductive Metabolism

Radiolabeled hydrazinocurcumin derivatives, [18F]1 and [18F]2 were synthesized and both radioligands were resistant to reductive metabolism. MicroPET images of C6 glioma xenografted mice showed high tumor uptake and retention of [18F]2.

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