A novel solid-phase synthesis of 5'-radiolabeled oligonucleotides is described. The labeling reaction is carried out by the phosphoramidite method with the aid of [4,6-di-14C]-5'-dimethoxytritylthymidine building block 1. The feasibility of the method is demonstrated by preparation of 3'-phosphorylated dodecathymidylate phosphorothioate containing radiolabeled nucleoside at the 5'-terminus.
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http://dx.doi.org/10.1016/s0960-894x(98)00028-6 | DOI Listing |
Cancer Chemother Pharmacol
December 2024
Department of Pharmacy, The First Affiliated Hospital of Soochow University, Suzhou, 215031, China.
Purpose: The study aims to investigate the absorption, metabolism, and excretion of donafenib, a deuterated derivative of sorafenib, in healthy Chinese male volunteers.
Methods: Six healthy Chinese male volunteers were administered a single oral dose of 300 mg donafenib containing 120 µCi of [14 C]-donafenib. The study involved collecting and analyzing plasma, urine, and feces samples to determine the recovery and distribution of total radioactivity, identify metabolites, and assess the metabolic pathways of donafenib.
Eur J Pharm Sci
November 2024
Eli Lilly and Company, Indianapolis, USA.
Tirzepatide is a once-weekly GIP/GLP-1 receptor agonist used for treatment of type 2 diabetes (T2D) in adults and was recently approved for treatment of obesity. To determine the absorption, distribution, metabolism, and excretion (ADME) of tirzepatide, [C]-radiolabeled tirzepatide was investigated in both humans and preclinical species. [C]-Tirzepatide was prepared by incorporating four C's in the linker region between the amino acid backbone and the di-acid moiety.
View Article and Find Full Text PDFDrug Metab Dispos
August 2024
Clinical Pharmacology and Quantitative Pharmacology, BioPharmaceuticals R&D (C.M.), Drug Metabolism and Pharmacokinetics, Oncology R&D (M.W.), Global Medicines Development, Oncology R&D (R.S., D.S.), Integrated Bioanalysis, BioPharmaceuticals R&D (C.B.), and Pharmaceutical Sciences, R&D (R.A.B., M.G.), AstraZeneca, Cambridge, United Kingdom; Drug Metabolism and Pharmacokinetics, Oncology R&D (Z.Z.) and Clinical Pharmacology and Quantitative Pharmacology, BioPharmaceuticals R&D (J.D.), AstraZeneca, Waltham, Massachusetts; Quotient Sciences Ltd, Ruddington, Nottingham, United Kingdom (S.S.); and Clinical Pharmacology and Quantitative Pharmacology, BioPharmaceuticals R&D, AstraZeneca, Gothenburg, Sweden (M.C.)
Antimicrob Agents Chemother
August 2024
Pfizer Inc., New York, New York, USA.
Nucleic Acid Ther
August 2024
Department of Pharmacy and Biotechnologies, University of Bologna, Bologna, Italy.
Although has been considered an undruggable target, alterations confer poor prognosis in many pediatric and adult cancers. The novel -specific inhibitor BGA002 is an antigene peptide nucleic acid oligonucleotide covalently bound to a nuclear localization signal peptide. In the present study, we characterized the pharmacokinetics (PK) of BGA002 after single and repeated administration to mice using a novel specific enzyme-linked immunosorbent assay.
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