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http://dx.doi.org/10.1245/s10434-022-11766-z | DOI Listing |
Chem Sci
September 2025
Molecular AI, Discovery Sciences, BioPharmaceuticals R&D, AstraZeneca Gothenburg Sweden
Incorporating non-natural amino acids (NNAAs) into peptides enhances therapeutic properties, including binding affinity, metabolic stability, and half-life time. The pursuit of novel NNAAs for improved peptide designs faces the challenge of effective synthesis of these building blocks as well as the entire peptide itself. Solid-Phase Peptide Synthesis (SPPS) is an essential technology for the automated assembly of peptides with NNAAs, necessitating careful protection for effective coupling of amino acids in the peptide chain.
View Article and Find Full Text PDFBackgroundRAY1216 is an alpha-ketoamide-based peptide inhibitor of severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2) major protease (M). This study evaluated the absorption, distribution, metabolism and excretion of [C]-labelled RAY1216 by oral administration.Research design and methodsThis phase Ι study was designed to assess the pharmacokinetics, mass balance and metabolic pathways in 6 healthy Chinese adult men after a single fasting oral administration of 240 mL (containing 400 mg/100 μCi) [C] RAY1216.
View Article and Find Full Text PDFProstate
September 2025
Department of Urology, University of Rochester Medical Center, Rochester, New York, USA.
Background: Prostate cancer (PCa) is the only cancer in men to exhibit androgen sensitivity at diagnosis, which has allowed for the development of androgen deprivation therapy (ADT). However, outcomes in high-risk PCa (HRPCa) remain significantly worse than low risk disease and the use of ADT varies among treatment algorithms and medical specialties. In men treated with radiation, testosterone recovery after completing ADT has been associated with oncologic outcomes.
View Article and Find Full Text PDFDiabetes Obes Metab
September 2025
Department of Endocrinology, Peking University People's Hospital, Beijing, People's Republic of China.
Aim: To evaluate the long-term efficacy and safety data at 104 weeks in tirzepatide-treated participants with type 2 diabetes who had inadequate glycaemic control on metformin and/or sulfonylurea.
Materials And Methods: This post-hoc analysis was based on the SURPASS-4 data (NCT03730662), a multicenter, Phase III trial. Participants were randomised to receive tirzepatide (5, 10, or 15 mg) or insulin glargine.
Eur J Pharm Biopharm
September 2025
RaDes GmbH, Schnackenburgallee 114, 22525 Hamburg, Germany. Electronic address:
Polysorbate 20 (PS20) is one of the most commonly used non-ionic surfactants in cosmetics, pharmaceuticals and food products. Considered as biocompatible and non-irritating, it is further valued for its solubilising and protein stabilising properties. PS20 is manufactured through a multi-stage reaction of sorbitol with various fatty acids and ethylene oxide, resulting in a complex mixture of components with different molecular weights and polarity.
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