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Integrative preclinical strategy for pharmacokinetic profiling and candidate selection of 3-hydroxypropanamidines: a promising antimalarial class. [PDF]
Moritz A +7 more
europepmc +1 more source
PET-MRI biomarkers reveal efficacy of a novel NLRP3 inhibitor in Parkinson's disease models. [PDF]
Albornoz EA +17 more
europepmc +1 more source
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Preclinical pharmacokinetics of statins
Methods and Findings in Experimental and Clinical Pharmacology, 2002This review summarizes the pharmacokinetic properties of HMG-CoA reductase inhibitors (or statins) reported in animals. Lovastatin and simvastatin are administered as lactone prodrugs in contrast to other statins, which are generally formulated in the pharmacological active hydroxy acid form.
R F, Reinoso +3 more
openaire +2 more sources
Clinical and Preclinical Pharmacokinetics of Raltitrexed
Clinical Pharmacokinetics, 2000Raltitrexed is a specific, folate-based inhibitor of thymidylate synthase with activity in advanced colorectal cancer comparable with that of fluorouracil (5-fluorouracil) plus folinic acid. Its activity is enhanced by rapid cellular entry and polyglutamation, with the polyglutamated derivatives having approximately 100-fold greater inhibitory potency ...
S J, Clarke, P J, Beale, L P, Rivory
openaire +2 more sources
Preclinical pharmacokinetics of paclitaxel and docetaxel
Anti-Cancer Drugs, 1998The taxanes paclitaxel and docetaxel represent a novel class of antineoplastic agents. A major problem of both drugs is their low aqueous solubility and the design of suitable formulations has been a difficult step in the process of therapeutic development.
Sparreboom, A. +3 more
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Preclinical pharmacokinetics of radiolabelled hyaluronan
Pharmacological Reports, 2012Hyaluronan (HYA) is a high molecular weight glucosaminoglycan with a great perspective for medical applications. Because HYA is widespread in the body, it is difficult to determine the fate of exogenously administered HYA.In this study, HYAof different molecular weights (0.1-1 MDa) was labelled with (99m)Tc, and the distribution profiles were ...
Milan, Laznicek +3 more
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Preclinical pharmacokinetics and antitumor activity of imexon
Investigational New Drugs, 1995Imexon is an aziridine compound originally studied for immune-enhancing effects on lymphocytes. The drug was well-tolerated in humans and was shown to be active in a variety of animal tumor models. Recently, imexon has demonstrated antitumor activity in human multiple myeloma cell lines in vitro.
R T, Dorr +3 more
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Preclinical Pharmacokinetics of Triptolide: A Potential Antitumor Drug
Current Drug Metabolism, 2019Background:Triptolide, a bioactive component in Tripterygium wilfordii extracts, possess strong antiproliferative activity on all 60-National Cancer Institute (NCI) cancer cell lines. However, the widespread use of triptolide in the clinical practice is greatly limited for its multi-organ toxicity and narrow therapeutic window.
Wei Song, Yong Chen, Zhihong Peng
exaly +3 more sources
Pharmacokinetics, Metabolites, and Preclinical Safety of Vinflunine
Seminars in Oncology, 2008The novel microtubule inhibitor, vinflunine, has a unique mechanism of action that differs from other members of the vinca alkaloid class in terms of tubulin-binding affinity, microtubule dynamics, spiral formation, and intracellular accumulation. Vinflunine has shown significant activity in vivo, which involves its antimitotic, antiangiogenic, and ...
Sharon, Lobert, Christian, Puozzo
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