Development and Preclinical Evaluation of Dual-Target 68Ga/177Lu-Labeled FAP-Bisphosphonate Radioligands with Enhanced Osteoma Retention [0.03%]
具有增强的骨瘤滞留性的双重靶向68Ga / 177Lu标记的FAP-双膦酸盐放射配体的开发和临床前评估
Ruiyue Zhao,Yuling Deng,Wenbin Jin et al.
Ruiyue Zhao et al.
Bone metastases and associated skeletal-related events (SREs) severely compromise the survival and quality of life of patients with advanced cancer. Although bisphosphonates enable efficient bone targeting, their radiolabeled analogues exhi...
Novel Covalent FAP-Targeted [68Ga]Ga-DOTA-mFS-KERERG-FAP-2286 for Improved Pharmacokinetics and Enhanced Tumor Uptake [0.03%]
新型共价FAP靶向[68Ga]Ga-DOTA-mFS-KERERG-FAP-2286，可改善药代动力学并增强肿瘤摄取
Zhongcai Jin,Tongtong Wu,Shijie Tang et al.
Zhongcai Jin et al.
Preclinical and clinical investigations have revealed the promising potential of various fibroblast-activating protein inhibitor (FAPI) radiopharmaceuticals. One strategy of particular interest involves the covalent targeting of these FAPI-...
Precipitation Inhibition by Small-Molecule Analogues To Sustain Drug Supersaturation [0.03%]
小分子类似物抑制沉淀以维持药物过饱和状态
Parag Roy,Oisín N Kavanagh
Parag Roy
Maintaining supersaturation during gastric-to-intestinal pH transitions can be essential to maximize the oral exposure of pH-sensitive drugs. This study demonstrates a mechanistically guided strategy to stabilize ciprofloxacin supersaturati...
Design and In Vitro Application of Bioactive Cell-Penetrating Peptides as Effective Therapeutic Agents for Corneal Wound Healing [0.03%]
一种用于角膜伤口愈合的生物活性细胞穿透肽的设计及体外应用研究
Mayank Sinha,Archana Chugh
Mayank Sinha
The management of corneal injuries remains a formidable global health challenge, yet current therapeutic strategies remain supportive rather than actively regenerative, primarily because current clinical standards fail to address the delica...
GE11/RGD Dual-Ligand Copper Nanoassemblies Synchronize Cuproptosis and Photothermal Therapy for Targeted Cervical Cancer Ablation [0.03%]
基于GE11/RGD双配体的铜纳米组装体系用于同步诱导宫颈癌铜死亡和光热治疗
Nan Yang,Lu Liu,Lu Ding et al.
Nan Yang et al.
Cervical cancer remains a major global health burden. Conventional surgery, radiotherapy, and chemotherapy are limited by insufficient tumor targeting, severe systemic toxicity, and drug resistance, highlighting an urgent need for safe, pre...
Unveiling Solvent-Mediated Mechanochemical Cocrystallization Pathways by In Situ CLASSIC NMR Spectroscopy [0.03%]
利用原位CLASSIC核磁共振光谱揭示溶剂介导的机械化学共结晶路径
Anna M Gołkowska,Maciej Nowak,László Fábián et al.
Anna M Gołkowska et al.
Although mechanochemical synthesis offers a sustainable way to produce solid forms of pharmaceutical compounds, the molecular-level mechanisms that govern solvent-mediated transformations remain largely unexplored. In this study, we present...
Synthesis and Preclinical Evaluation of [18F]AlF-NOTA-A2P-GPC3P for Imaging of GPC3 [0.03%]
[18F]AlF-NOTA-A2P-GPC3P的合成及其GPC3显像的药代动力学评价与成像性能研究
Zhisheng Jie,Kadeer Tudi,Zihao Chen et al.
Zhisheng Jie et al.
To develop an effective GPC3-targeted PET probe for tumor imaging, [18F]AlF-NOTA-A2P-GPC3P was synthesized by introducing the hydrophilic linker A2P into the L5 peptide scaffold. The probe was efficiently radiolabeled using the [18F]AlF met...
Application of Allometric Scaling and Translational Modeling to Predict Human Pharmacokinetics of mRNA-Encoded Antibodies [0.03%]
比例尺标度和翻译模型在预测mRNA编码抗体人体药代动力学中的应用
Tam N T Nguyen,Philip K-Y Chang,Paul Panorchan et al.
Tam N T Nguyen et al.
Messenger RNA (mRNA)-lipid nanoparticle (mRNA-LNP) platforms enable the in vivo expression of almost any therapeutic protein, offering unprecedented flexibility for clinical translation. However, for these rapidly deployable therapies, pred...
Proteomics-Informed Physiologically Based Pharmacokinetic Modeling for Aldehyde Oxidase Substrates in Colorectal Cancer Liver Metastasis [0.03%]
用于结直肠癌肝转移甲醛脱氢酶底物的蛋白质组学指导的生理药动学模型
Nihan Izat,Areti-Maria Vasilogianni,Zubida M Al-Majdoub et al.
Nihan Izat et al.
Aldehyde oxidase (AO) metabolizes a broad range of compounds, including the oxidation of anticancer kinase inhibitors. Quantitative proteomics data reported in the literature for liver microsomes from colorectal liver metastases (CRLM) indi...
Predicting Agitation Stability of Monoclonal Antibodies during Developability Assessment [0.03%]
在药物研发过程中评估单克隆抗体 agitation 稳定性预测的方法和应用研究
Michaela Cohrs,Nevena Pagureva,Utku Ozbulak et al.
Michaela Cohrs et al.
Developability assessment facilitates the selection of antibody drug candidates with desirable pharmaceutical properties. However, it remains uncertain whether agitation-induced aggregation can be predicted from standard developability para...