Types and cooperation of patent assignees (A) Changes in assignee types. (B) Collaboration patterns. The number represents cooperation frequency of different types of assignees (C, private companies; U, universities; R, research institutions; I, individuals).

Types and cooperation of patent assignees (A) Changes in assignee types. (B) Collaboration patterns. The number represents cooperation frequency of different types of assignees (C, private companies; U, universities; R, research institutions; I, individuals).

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Implementing small interfering RNA (siRNA) is a promising therapy because it silences disease-related genes theoretically. However, the efficient delivery of siRNA is challenging, which limits its therapeutic applications. Various pharmaceutical delivery systems containing key technologies have been developed and patented, which are of great concer...

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... the past 20 years, 10 countries and regions have been responsible for 95% of patents published: the United States (51%), Japan (9%), mainland China (7%), Canada (6%), Korea, Germany, and Switzerland (5% each), the United Kingdom (3%), and France and Israel (2% each) (see Figure 4A). Figure 4B displays the technological origins and market destinations. ...
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... the past 20 years, 10 countries and regions have been responsible for 95% of patents published: the United States (51%), Japan (9%), mainland China (7%), Canada (6%), Korea, Germany, and Switzerland (5% each), the United Kingdom (3%), and France and Israel (2% each) (see Figure 4A). Figure 4B displays the technological origins and market destinations. More than 90% of the patents filed originated in the 10 patent offices and organizations listed. ...

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... The development of N-acetylgalactosamine (GalNAc) conjugates, which bind to the asialoglycoprotein receptor (ASGR) abundantly expressed on the surface of hepatocytes, has become a breakthrough approach for targeted delivery of siRNA to hepatocytes [6]. So far, GalNAc based therapies have held a prominent position in the drug development pipeline of several pharmaceutical companies [6], five GalNAc-based siRNA drugs have been approved by FDA, in which siRNAs are all conjugated to a GalNAc ligand and enable ASGPRmediated targeted delivery to hepatocytes [7][8][9]. GalNAc is relatively simple to synthesize and can be administrated subcutaneously, and has shown favorable biocompatibility/toxicity profiles, as well as very high efficacy, so it is currently the most popular platform for siRNA delivery [10]. At present, most siRNA drugs in clinical trials are based on GalNAc conjugation [10,11]. ...
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Small interference RNA (siRNA) is a class of short double-stranded RNA molecules that cause mRNA degradation through an RNA interference mechanism and is a promising therapeutic modality. RBD1016 is a siRNA drug in clinical development for the treatment of chronic Hepatitis B Virus (HBV) infection, which contains a conjugated with N-acetylglucosamine moiety that can facilitate its hepatic delivery. We aimed to construct a semi-mechanistic model of RBD1016 in pre-clinical animals, to elucidate the pharmacokinetic/pharmacodynamic (PK/PD) profiles in mice and PK profiles in monkeys, which can lay the foundation for potential future translation of RBD1016 PK and PD from the pre-clinical stage to the clinic stage. The proposed semi-mechanistic PK/PD model fitted PK and PD data in HBV transgenic mice well and described plasma and liver concentrations in the monkeys well. The simulation results showed that our model has a reasonable predictive ability for Hepatitis B surface antigen (HBsAg) levels after multiple dosing in mice. Further PK and PD data for RBD1016, including clinical data, will assist in refining the model presented here. Our current effort focused on model building for RBD1016, we anticipate that the model could apply to other GalNAc-siRNA drugs.
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