Search Results - "Fretland, J."
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Camonsertib in DNA damage response-deficient advanced solid tumors: phase 1 trial results
Published in Nature medicine (01-06-2023)“…Predictive biomarkers of response are essential to effectively guide targeted cancer treatment. Ataxia telangiectasia and Rad3-related kinase inhibitors (ATRi)…”
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Utility of Intersystem Extrapolation Factors in Early Reaction Phenotyping and the Quantitative Extrapolation of Human Liver Microsomal Intrinsic Clearance Using Recombinant Cytochromes P450
Published in Drug metabolism and disposition (01-03-2011)“…Reaction phenotyping using recombinant human cytochromes P450 (P450) has great utility in early discovery. However, to fully realize the advantages of using…”
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Determination of time-dependent inactivation of CYP3A4 in cryopreserved human hepatocytes and assessment of human drug-drug interactions
Published in Drug metabolism and disposition (01-11-2011)“…Assessment of time-dependent inhibition (TDI), especially CYP3A4, is an important parameter for preclinical and clinical development. The use of human liver…”
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Mechanistic physiology-based pharmacokinetic modeling to elucidate vincristine-induced peripheral neuropathy following treatment with novel kinase inhibitors
Published in Cancer chemotherapy and pharmacology (01-09-2021)“…Purpose Limited information is available regarding the drug–drug interaction (DDI) potential of molecular targeted agents and rituximab plus cyclophosphamide,…”
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Molecular Genetics and Epidemiology of the NAT1 and NAT2 Acetylation Polymorphisms
Published in Cancer epidemiology, biomarkers & prevention (01-01-2000)“…The focus of this review is the molecular genetics, including consensus NAT1 and NAT2 nomenclature, and cancer epidemiology of the NAT1 and NAT2 acetylation…”
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Epoxide hydrolases: biochemistry and molecular biology
Published in Chemico-biological interactions (01-12-2000)“…Epoxides are organic three-membered oxygen compounds that arise from oxidative metabolism of endogenous, as well as xenobiotic compounds via chemical and…”
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Multiscale Model Identifies Improved Schedule for Treatment of Acute Myeloid Leukemia In Vitro With the Mcl‐1 Inhibitor AZD5991
Published in CPT: pharmacometrics and systems pharmacology (01-10-2020)“…Anticancer efficacy is driven not only by dose but also by frequency and duration of treatment. We describe a multiscale model combining cell cycle, cellular…”
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Effects of single nucleotide polymorphisms in human N‐acetyltransferase 2 on metabolic activation (O‐acetylation) of heterocyclic amine carcinogens
Published in International journal of cancer (01-09-2006)“…N‐Acetyltransferase 2 (NAT2) catalyzes the O‐acetylation of N‐hydroxy heterocyclic amines such as N‐hydroxy‐2‐amino‐3,8‐dimethylimidazo[4,5‐f]quinoxaline…”
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Improving the Accuracy of Predicted Human Pharmacokinetics: Lessons Learned from the AstraZeneca Drug Pipeline Over Two Decades
Published in Trends in pharmacological sciences (Regular ed.) (01-06-2020)“…During drug discovery and prior to the first human dose of a novel candidate drug, the pharmacokinetic (PK) behavior of the drug in humans is predicted from…”
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Sustained release and improved bioavailability in mice after subcutaneous administration of griseofulvin as nano- and microcrystals
Published in International journal of pharmaceutics (20-07-2019)“…[Display omitted] The objective of the study was to evaluate the pharmacokinetic profile after different subcutaneous (s.c.) administrations of nano- and…”
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Tissue distribution of N-acetyltransferase 1 and 2 catalyzing the N-acetylation of 4-aminobiphenyl and O-acetylation of N-hydroxy-4-aminobiphenyl in the congenic rapid and slow acetylator Syrian hamster
Published in Molecular carcinogenesis (01-04-2006)“…N‐acetyltransferase 1 (NAT1) and 2 (NAT2) enzymes catalyzing both deactivation (N‐acetylation) and activation (O‐acetylation) of arylamine carcinogens such as…”
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Identification and Biosynthesis of an N-Glucuronide Metabolite of Camonsertib
Published in Drug metabolism and disposition (01-05-2024)“…Camonsertib is a novel ATR kinase inhibitor in clinical development for advanced cancers targeting sensitizing mutations. This article describes the…”
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Development of a quantification method for adenosine in tumors by LC-MS/MS with dansyl chloride derivatization
Published in Analytical biochemistry (01-03-2019)“…Adenosine is known to be an important signaling molecule in many physiological processes and has recently been shown to be an important molecule in oncology. A…”
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Development of a Practical Nomogram for Personalized Anemia Management in Patients Treated with Ataxia Telangiectasia and Rad3-related Inhibitor Camonsertib
Published in Clinical cancer research (16-02-2024)“…Camonsertib is a highly selective and potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase. Dose-dependent anemia is a class-related…”
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Ataxia telangiectasia and Rad3-related (ATR) inhibitor camonsertib dose optimization in patients with biomarker-selected advanced solid tumors (TRESR study)
Published in JNCI : Journal of the National Cancer Institute (01-09-2024)“…Abstract Background Camonsertib is a selective oral inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase with demonstrated efficacy in tumors with…”
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Dietary Selenium Reduces the Formation of Aberrant Crypts in Rats Administered 3,2′-Dimethyl-4-aminobiphenyl
Published in Toxicology and applied pharmacology (15-05-1999)“…Human epidemiologic studies suggest that low selenium status is associated with increased cancer risk and that selenium supplementation is associated with…”
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Novel Human N-Acetyltransferase 2 Alleles That Differ in Mechanism for Slow Acetylator Phenotype
Published in The Journal of biological chemistry (03-12-1999)“…Three novel human NAT2 alleles ( NAT2*5D , NAT2*6D , and NAT2*14G ) were identified and characterized in a yeast expression system. The common rapid ( NAT2*4 )…”
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Quantitative Evaluation of Dendritic Nanoparticles in Mice: Biodistribution Dynamics and Downstream Tumor Efficacy Outcomes
Published in Molecular pharmaceutics (03-01-2022)“…A physiologically based pharmacokinetic model was developed to describe the tissue distribution kinetics of a dendritic nanoparticle and its conjugated active…”
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Further Considerations Towards an Effective and Efficient Oncology Drug Discovery DMPK Strategy
Published in Current drug metabolism (01-01-2020)“…DMPK data and knowledge are critical in maximising the probability of developing successful drugs via the application of in silico, in vitro and in vivo…”
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