Considerations and recommendations for assessment of plasma protein binding and drug–drug interactions for siRNA therapeutics

Impact of Serum Proteins on the Uptake and RNA Interference Activity of N-Acetylgalactosamine-Conjugated Small Interfering RNAs

(2021) Saket Agarwal et al.   Nucleic Acid Therapeutics

Pharmacokinetics and Pharmacodynamics of the Small Interfering Ribonucleic Acid (siRNA), Givosiran, in Patients with Acute Hepatic Porphyria

(2020) Sagar Agarwal et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Efficient Delivery of Antisense Oligonucleotides Using Bioreducible Lipid Nanoparticles In Vitro and In Vivo

(2020) Liu Yang et al.   Molecular Therapy-Nucleic Acids

Rheumatoid arthritis downregulates the drug transporter OATP1B1: Fluvastatin as a probe

(2020) Juciene Aparecida Caris et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Emerging siRNA Design Principles and Consequences for Biotransformation and Disposition in Drug Development

(2020) Sara C. Humphreys et al.   JOURNAL OF MEDICINAL CHEMISTRY

POE Immunoassay: Plate-based oligonucleotide electro-chemiluminescent immunoassay for the quantification of nucleic acids in biological matrices

(2020) Mai B. Thayer et al.   Scientific Reports

Investigating the pharmacodynamic durability of GalNAc–siRNA conjugates

(2020) Christopher R Brown et al.   NUCLEIC ACIDS RESEARCH

Introducing an In Vitro Liver Stability Assay Capable of Predicting the In Vivo Pharmacodynamic Efficacy of siRNAs for IVIVC

(2020) Babak Basiri et al.   Molecular Therapy-Nucleic Acids

High penetrance of acute intermittent porphyria in a Spanish founder mutation population and CYP2D6 genotype as a susceptibility factor

(2019) María Barreda-Sánchez et al.   Orphanet Journal of Rare Diseases

Safety evaluation of 2′-deoxy-2′-fluoro nucleotides in GalNAc-siRNA conjugates

(2019) Maja M Janas et al.   NUCLEIC ACIDS RESEARCH

RNA-Targeted Therapeutics

(2019) Stanley T. Crooke et al.   Cell Metabolism

Plasma and liver protein binding of GalNAc conjugated siRNA

(2019) Sara C Humphreys et al.   DRUG METABOLISM AND DISPOSITION

Current Development of siRNA Bioconjugates: From Research to the Clinic

(2019) Ivan V. Chernikov et al.   Frontiers in Pharmacology

In Vitro Drug-Drug Interaction Evaluation of GalNAc conjugated siRNAs Against CYP450 Enzymes and Transporters

(2019) Diane Ramsden et al.   DRUG METABOLISM AND DISPOSITION

Pharmacokinetics and Clinical Pharmacology Considerations of GalNAc3-Conjugated Antisense Oligonucleotides

(2019) Yanfeng Wang et al.   Expert Opinion on Drug Metabolism & Toxicology

Update on Therapeutic Protein–Drug Interaction: Information in Labeling

(2019) Xing Jing et al.   CLINICAL PHARMACOKINETICS

PBPK models for evaluating membrane transporter mediated DDIs: Current capabilities, case studies, future opportunities and recommendations

(2019) Kunal Taskar et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Effects of Renal Impairment on the Pharmacokinetics, Efficacy, and Safety of Inclisiran: An Analysis of the ORION-7 and ORION-1 Studies

(2019) R. Scott Wright et al.   MAYO CLINIC PROCEEDINGS

Evaluation of electrophoretic mobility shift assay as a method to determine plasma protein binding of siRNA

(2019) Carrie Rocca et al.   Bioanalysis

Development of a new Japanese guideline on drug interaction for drug development and appropriate provision of information

(2019) Akihiro Ishiguro et al.   Drug Metabolism and Pharmacokinetics

Evaluation of GalNAc-siRNA Conjugate Activity in Pre-clinical Animal Models with Reduced Asialoglycoprotein Receptor Expression

(2018) Jennifer L.S. Willoughby et al.   MOLECULAR THERAPY

Advanced siRNA Designs Further Improve In Vivo Performance of GalNAc-siRNA Conjugates

(2018) Donald J. Foster et al.   MOLECULAR THERAPY

Patisiran, an RNAi Therapeutic, for Hereditary Transthyretin Amyloidosis

(2018) David Adams et al.   NEW ENGLAND JOURNAL OF MEDICINE

Improving siRNA Delivery In Vivo Through Lipid Conjugation

(2018) Maire F. Osborn et al.   Nucleic Acid Therapeutics

The Oligonucleotide Safety Working Group (OSWG)

(2018) Dave Schubert et al.   Nucleic Acid Therapeutics

Hydrophobicity drives the systemic distribution of lipid-conjugated siRNAs via lipid transport pathways

(2018) Maire F Osborn et al.   NUCLEIC ACIDS RESEARCH

Diverse lipid conjugates for functional extra-hepatic siRNA delivery in vivo

(2018) Annabelle Biscans et al.   NUCLEIC ACIDS RESEARCH

Industry Perspective on Contemporary Protein-Binding Methodologies: Considerations for Regulatory Drug-Drug Interaction and Related Guidelines on Highly Bound Drugs

(2017) Li Di et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Impact of enhanced metabolic stability on pharmacokinetics and pharmacodynamics of GalNAc–siRNA conjugates

(2017) Jayaprakash K. Nair et al.   NUCLEIC ACIDS RESEARCH

Safety Evaluation of Lipid Nanoparticle–Formulated Modified mRNA in the Sprague-Dawley Rat and Cynomolgus Monkey

(2017) Maja Sedic et al.   VETERINARY PATHOLOGY

Recommendations of the Oligonucleotide Safety Working Group's Formulated Oligonucleotide Subcommittee for the Safety Assessment of Formulated Oligonucleotide-Based Therapeutics

(2017) Jennifer L. Marlowe et al.   Nucleic Acid Therapeutics

Systemic inflammation in acute intermittent porphyria: a case-control study

(2016) E. Storjord et al.   CLINICAL AND EXPERIMENTAL IMMUNOLOGY

Integrated Safety Assessment of 2′-O-Methoxyethyl Chimeric Antisense Oligonucleotides in NonHuman Primates and Healthy Human Volunteers

(2016) Stanley T Crooke et al.   MOLECULAR THERAPY

OSWG Recommendations for Genotoxicity Testing of Novel Oligonucleotide-Based Therapeutics

(2016) Cindy L. Berman et al.   Nucleic Acid Therapeutics

Considerations for the Characterization and Interpretation of Results Related to Alternative Complement Activation in Monkeys Associated with Oligonucleotide-Based Therapeutics

(2016) Scott P. Henry et al.   Nucleic Acid Therapeutics

Oligo Safety Working Group Exaggerated Pharmacology Subcommittee Consensus Document

(2015) Doug Kornbrust et al.   Nucleic Acid Therapeutics

Multivalent N-Acetylgalactosamine-Conjugated siRNA Localizes in Hepatocytes and Elicits Robust RNAi-Mediated Gene Silencing

(2014) Jayaprakash K. Nair et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Bioanalysis for plasma protein binding studies in drug discovery and drug development: views and recommendations of the European Bioanalysis Forum

(2014) Brigitte Buscher et al.   Bioanalysis

Considerations for Assessment of Reproductive and Developmental Toxicity of Oligonucleotide-Based Therapeutics

(2014) Joy Cavagnaro et al.   Nucleic Acid Therapeutics

Shielding of Lipid Nanoparticles for siRNA Delivery: Impact on Physicochemical Properties, Cytokine Induction, and Efficacy

(2014) Varun Kumar et al.   Molecular Therapy-Nucleic Acids

Plasma protein binding: From discovery to development

(2013) Tonika Bohnert et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Drug−disease interaction: Crohn's disease elevates verapamil plasma concentrations but reduces response to the drug proportional to disease activity

(2011) Forough Sanaee et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Disease–Drug–Drug Interaction Involving Tocilizumab and Simvastatin in Patients With Rheumatoid Arthritis

(2011) C Schmitt et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Inflammation-mediated changes in drug transporter expression/activity: implications for therapeutic drug response

(2011) Alexander M Cressman et al.   Expert Review of Clinical Pharmacology

Variability in drug metabolizing enzyme activity in HIV-infected patients

(2010) Amanda E. Jones et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

Elimination Pathways of Systemically Delivered siRNA

(2010) Yuanyu Huang et al.   MOLECULAR THERAPY

The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery

(2010) Dennis A. Smith et al.   NATURE REVIEWS DRUG DISCOVERY

A preliminary study of atorvastatin plasma concentrations in critically ill patients with sepsis

(2008) Peter S. Kruger et al.   INTENSIVE CARE MEDICINE

Sequence- and target-independent angiogenesis suppression by siRNA via TLR3

(2008) Mark E. Kleinman et al.   NATURE

Metabolite identification of small interfering RNA duplex by high-resolution accurate mass spectrometry

(2008) Yan Zou et al.   RAPID COMMUNICATIONS IN MASS SPECTROMETRY

Decreased dromotropic response to verapamil despite pronounced increased drug concentration in rheumatoid arthritis

(2003) Patrick R. Mayo et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY