GCN-BBB: Deep Learning Blood-Brain Barrier (BBB) Permeability PharmacoAnalytics with Graph Convolutional Neural (GCN) Network [0.03%]
基于图卷积神经网络的血脑屏障渗透性评价模型
Yankang Jing,Guangyi Zhao,Yuanyuan Xu et al.
Yankang Jing et al.
The Blood-Brain Barrier (BBB) is a selective barrier between the Central Nervous System (CNS) and the peripheral system, regulating the distribution of molecules. BBB permeability has been crucial in CNS-targeting drug development, such as ...
Virtual Bioequivalence Assessment of Tofacitinib Once Daily Modified Release Dosage Form in Pediatric Subjects [0.03%]
托法替尼儿科受试者一日一次缓释制剂的生物等效性评估
Kazuko Sagawa,Vivek Purohit,Vu Le et al.
Kazuko Sagawa et al.
Tofacitinib is a potent, selective inhibitor of the Janus kinase (JAK) family of kinases with a high degree of selectivity within the human genome's set of protein kinases. Currently approved formulations for tofacitinib citrate are immedia...
Hsien Wei Huang,Shengjia Wu,Shufang Liu et al.
Hsien Wei Huang et al.
This study investigates the role of FcRn in brain disposition of monoclonal antibodies. Human FcRn (hFcRn) expressing mice and different FcRn binding variants of a non-target binding antibody trastuzumab (WT) were used for the investigation...
Nomlabofusp, a Fusion Protein of Human Frataxin and a Cell Penetrant Peptide, Delivers Mature and Functional Frataxin into Mitochondria [0.03%]
Nomlabofusp，一个由人乳酸血症蛋白和细胞穿透肽融合的蛋白质，能够将成熟的有功能的乳酸血症蛋白传递进线粒体
Matthew G Baile,John Jones,Natasha Sahr et al.
Matthew G Baile et al.
Friedreich's ataxia is a rare, progressive, genetic disorder, the root cause of which is a significant deficiency in the mitochondrial protein frataxin. Frataxin is ubiquitously expressed, but its deficiency results in a variety of debilita...
Leveraging Buprenorphine and Halofantrine as Tool Molecules to Develop a Novel Semi-Physiologically based Pharmacokinetic Model Accounting for Gastro-Intestinal Lymphatic Absorption and Enabling Cross-Species Translation [0.03%]
利用丁丙诺啡和卤风扇特作为工具分子，开发一个新的半生理药代动力学模型，该模型考虑了胃肠淋巴吸收并实现跨物种转换
Xun Tao,Shraddha Sadekar,Douglas Leipold et al.
Xun Tao et al.
Intestinal lymphatic absorption is a crucial alternative to portal uptake for highly lipophilic drugs (log P > 5), bypassing first-pass metabolism. Unlike the portal-hepatic pathway, lymphatic uptake is rarely considered in physiologically ...
Establishing a Platform Method for Physical Appearance Assessment of New Parenteral Pharmaceuticals [0.03%]
新注射用药外观质量检测平台法的建立
Ying Wan,Walter Wasylaschuk,Joseph Straub et al.
Ying Wan et al.
Physical appearance (PA) is an attribute indicating the quality of parenteral pharmaceuticals. It is routinely evaluated during release and stability testing and included in regulatory filings. PA assessment of liquids involves three tests:...
The Drug Titration Paradox in the Presence of Intra-Individual Variation: Can we Estimate the True Concentration-Effect Relationship? [0.03%]
个体内部变异存在时的药物滴定悖论：我们能估计真正的浓度-效应关系吗？
Sebastiaan C Goulooze,Elke H J Krekels,Catherijne A J Knibbe et al.
Sebastiaan C Goulooze et al.
The drug titration paradox arises when higher drug concentrations are paradoxically associated with poorer efficacy outcomes, due to the titration of an individual's drug dose to achieve a desired effect. In cases with substantial intraindi...
Yasir Alshehry,Xiang Liu,Wenhua Li et al.
Yasir Alshehry et al.
Cancer immunotherapy is poised to be one of the major modalities for cancer treatment. Messenger RNA (mRNA) has emerged as a versatile and promising platform for the development of effective cancer immunotherapy. Delivery systems for mRNA t...
A Facile Way to Enhance the Therapeutic Efficacy of Hydrophobic Drugs via Amorphous Solid Dispersions [0.03%]
通过无定形固体分散体提升疏水药物的治疗效果的便捷方法
Ning Tao,Zihui Yan,Xin Wang et al.
Ning Tao et al.
Approximately 40% of marketed drugs and 75% of invested drugs in the pharmaceutical field are poorly soluble hydrophobic drugs with minimal solubility in water which make them difficult to be absorbed by the body and significantly limiting ...
Therapeutic Drug Monitoring of Biologics: Current Practice, Challenges and Opportunities - a Workshop Report [0.03%]
生物制剂的治疗药物监测：现状、挑战和机遇 – 一个研讨会报告
Sophie Shubow,Michele Gunsior,Amy Rosenberg et al.
Sophie Shubow et al.
Therapeutic drug monitoring (TDM) for dose modification of biologics has the potential to improve patient outcomes. The US Food and Drug Administration (FDA) and the American Association of Pharmaceutical Scientists (AAPS) hosted the first ...