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Relevant bibliographies by topics / Preclinical pharmacokinetics / Dissertations / Theses

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Dissertations / Theses on the topic 'Preclinical pharmacokinetics'

Author: Grafiati

Published: 4 June 2021

Last updated: 3 February 2022

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1

Kearbey, Jeffrey Dale. "Preclinical pharmacokinetics and skeletal pharmacology of a selective androgen receptor modulator." Connect to this title online, 2004. http://rave.ohiolink.edu/etdc/view?acc%5Fnum=osu1085168433.

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Thesis (Ph. D.)--Ohio State University, 2004.<br>Document formatted into pages; contains xvii, 162 p. Includes bibliographical references. Abstract available online via OhioLINK's ETD Center; full text release delayed at author's request until 2005 May 24.

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Kearbey, Jeffrey D. "Preclinical pharmacokinetics and skeletal pharmacology of a selective androgen receptor modulator." The Ohio State University, 2004. http://rave.ohiolink.edu/etdc/view?acc_num=osu1085168433.

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3

Dave, Nimita D. "Brain/Brain Tumor Pharmacokinetics and Pharmacodynamics of Letrozole." University of Cincinnati / OhioLINK, 2013. http://rave.ohiolink.edu/etdc/view?acc_num=ucin1368013158.

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4

Tsakalozou, Eleftheria. "PRECLINICAL AND CLINICAL DEVELOPMENT OF THE LIPOPHILIC CAMPTOTHECIN ANALOGUE AR-67." UKnowledge, 2013. http://uknowledge.uky.edu/pharmacy_etds/18.

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AR-67 is a lipophilic third generation camptothecin analogue, currently under early stage clinical trials. It acts by targeting Topoisomerase 1 (Top1), a nuclear enzyme essential for DNA replication and transcription and is present in two forms, the pharmacologically active lipophilic lactone and the charged carboxylate. In oncology patients participating in a phase I clinical trial, AR-67 lactone was the predominant species in plasma. Similarly to other camptothecins, the identified dose-limiting toxicities for AR-67 were neutropenia, thrombocytopenia and fatigue. In addition, in vitro metabo

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Aimiuwu, Josephine Eki. "Modulation of Pharmacologic Effects of 5-Azacytidine by Ribonucleotide Reductase Antisense GTI-2040." The Ohio State University, 2011. http://rave.ohiolink.edu/etdc/view?acc_num=osu1292851882.

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6

Hing, Jeremy P. "The application of non-linear mixed effects modelling to toxicokinetic data : population pharmacokinetics in preclinical studies." Thesis, University of Newcastle Upon Tyne, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.394740.

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7

Burger, A. M., Paul M. Loadman, D. E. Thurston, R. Schultz, H. H. Fiebig, and Michael C. Bibby. "Preclinical pharmacology of the pyrrolobenzodiazepine (PBD) monomer DRH-417 (NSC 709119)." Italian Society of Chemotherapy and the Italian Federation of Human and Animal Mycopathology, 2007. http://hdl.handle.net/10454/4571.

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no<br>The pyrrolobenzodiazepine monomer DRH-417 is a member of the anthramycin group of anti-tumor antibiotics that bind covalently to the N2 of guanine within the minor groove of DNA. DRH-417 emerged from the EORTC-Drug Discovery Committee and NCI 60 cell line in vitro screening programs as a potent antiproliferative agent with differential sensitivity towards certain cancer types such as melanoma, breast and renal cell carcinoma (mean IC(50) = 3 nM). DRH-417 was therefore tested for in vivo activity. The maximum tolerated dose (MTD) was established as 0.5 mg/kg given i.p. Marked anti-tumor a

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8

Ur-Rehman, Tofeeq. "Controlled release gel formulations and preclinical screening of drug candidates." Doctoral thesis, Umeå universitet, Kemiska institutionen, 2011. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-40489.

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Simple gel formulations may be applied to enhance the systemic and local exposure of potential compounds. The aim of this thesis is the development and characterization of controlled release formulations based on thermo-reversible poloxamer gels, which are suitable for novel drug delivery applications. In particular co-solvents (DMSO, ethanol), mucoadhesive polymers (chitosan, alginate) and salts (sodium tripolyphosphate, CaCl2) have been used to enhance the applications of poloxamer 407 (P407) formulations in preclinical animal studies. The impact of these additives on the micellization and

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Chen, Chunli. "Pharmacokinetic-Pharmacodynamic Evaluations and Experimental Design Recommendations for Preclinical Studies of Anti-tuberculosis Drugs." Doctoral thesis, Uppsala universitet, Institutionen för farmaceutisk biovetenskap, 2017. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-318845.

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Tuberculosis is an ancient infectious disease and a leading cause of death globally. Preclinical research is important for defining drugs and regimens which should be carried forward to human studies. This thesis aims to characterize the population pharmacokinetics and exposure-response relationships of anti-tubercular drugs alone and in combinations, and to suggest experimental designs for preclinical settings. The population pharmacokinetics of rifampicin, isoniazid, ethambutol and pyrazinamide were described for the first time in two mouse models. This allowed for linking the population pha

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10

Jiang, Nan Verfasser], and Dieter [Akademischer Betreuer] [Willbold. "Preclinical pharmacokinetics and cerebral distribution of D-enantiomeric peptides for the treatment of Alzheimer’s disease / Nan Jiang ; Betreuer: Dieter Willbold." Düsseldorf : Universitäts- und Landesbibliothek der Heinrich-Heine-Universität Düsseldorf, 2018. http://d-nb.info/1150918845/34.

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Jiang, Nan [Verfasser], and Dieter [Akademischer Betreuer] Willbold. "Preclinical pharmacokinetics and cerebral distribution of D-enantiomeric peptides for the treatment of Alzheimer’s disease / Nan Jiang ; Betreuer: Dieter Willbold." Düsseldorf : Universitäts- und Landesbibliothek der Heinrich-Heine-Universität Düsseldorf, 2018. http://d-nb.info/1150918845/34.

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12

Marckel, Jordan A. "The in-vivo Preclinical Development of a Humanized Anti-cocaine Monoclonal Antibody and its Fab Fragment for the Treatment of Cocaine Abuse." University of Cincinnati / OhioLINK, 2020. http://rave.ohiolink.edu/etdc/view?acc_num=ucin1613745458699203.

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13

Ananthula, Hari Krishna. "Pharmacokinetic Evaluation and Modeling of Tyrosine Kinase Inhibitors Nilotinib and Imatinib in Preclinical Species to Aid their Repurposing As Anti-Viral Agents." University of Cincinnati / OhioLINK, 2017. http://rave.ohiolink.edu/etdc/view?acc_num=ucin1504802233495176.

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14

de, Souza Paul Linus Clinical School St George Hospital Faculty of Medicine UNSW. "Preclinical and phase I studies of phenoxodiol: a translational approach for the development of a novel isoflavone for the treatment of prostate cancer." Awarded By:University of New South Wales. Clinical School - St George Hospital, 2009. http://handle.unsw.edu.au/1959.4/44510.

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This work presents an investigation of the potential development of phenoxodiol, a novel isoflavone, for the treatment of prostate cancer. The literature concerning isoflavone epidemiology, pharmacology, clinical use and their effect on prostate cancer is reviewed. Isoflavone impact on signal transduction pathways is also reviewed with a particular focus on the Akt / mTOR signal transduction pathway, a key signaling pathway in prostate cancer cells. In vitro experiments and xenograft nude mice studies show that phenoxodiol inhibits the growth of DU145 and PC3 prostate cancer cells, when used a

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Zoghaib, Iury Valentim Jorge. "Avaliação pré-clínica do perfil farmacocinético do protótipo antitumoral lLQFM030 em ratos por LC-MS/MS." Universidade Federal de Goiás, 2013. http://repositorio.bc.ufg.br/tede/handle/tede/3469.

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Submitted by Luciana Ferreira (lucgeral@gmail.com) on 2014-10-29T14:34:23Z No. of bitstreams: 2 Dissertação - Iury Valentim Jorge Zoghaib - 2013.pdf: 1607539 bytes, checksum: d92b3313edee2773935cb667be5b908d (MD5) license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b86306 (MD5)<br>Approved for entry into archive by Luciana Ferreira (lucgeral@gmail.com) on 2014-10-30T10:48:45Z (GMT) No. of bitstreams: 2 Dissertação - Iury Valentim Jorge Zoghaib - 2013.pdf: 1607539 bytes, checksum: d92b3313edee2773935cb667be5b908d (MD5) license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b863

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Nadkarni, Priya. "PULMONARY DELIVERY OF ANORECTIC GUT SECRETED PEPTIDES FOR APPETITE SUPPRESSION IN RATS." VCU Scholars Compass, 2009. http://scholarscompass.vcu.edu/etd/1941.

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This dissertation project aimed to demonstrate that pulmonary delivery of two anorectic gut secreted peptides, peptide YY (PYY) and oxyntomodulin (OXM) enabled food intake suppression and reduced body weight gain in rats via their systemic absorption from the lung and interaction with the brain. After PYY and OXM were administered to the lungs at varying doses, food intake and body weight gain were monitored in freely feeding rats. Significant 30-35 % food intake suppression was achieved for 4-6 h following pulmonary administration of endogenously active PYY3-36 and OXM1-37 at 0.80 and 0.50 mg

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Zoghaib, Alarisse Arçari Fachetti. "Avaliação pré-clínica do perfil farmacocinético do complexo de rutênio II/ triptofano em ratos por espectrofotometria UV-Vis." Universidade Federal de Goiás, 2015. http://repositorio.bc.ufg.br/tede/handle/tede/5879.

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Submitted by Luciana Ferreira (lucgeral@gmail.com) on 2016-08-09T14:22:46Z No. of bitstreams: 2 Dissertação - Alarisse Arçari Fachetti Zoghaib - 2015.pdf: 1188040 bytes, checksum: 9ab52dc612351ab19ab98e90e7ce6ec9 (MD5) license_rdf: 0 bytes, checksum: d41d8cd98f00b204e9800998ecf8427e (MD5)<br>Approved for entry into archive by Luciana Ferreira (lucgeral@gmail.com) on 2016-08-09T14:24:14Z (GMT) No. of bitstreams: 2 Dissertação - Alarisse Arçari Fachetti Zoghaib - 2015.pdf: 1188040 bytes, checksum: 9ab52dc612351ab19ab98e90e7ce6ec9 (MD5) license_rdf: 0 bytes, checksum: d41d8cd98f00b204e9800998ecf8

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Strydom, Natasha. "Preclinical pharmacokinetic evaluation of novel antimalarial and antituberculosis drug leads." Doctoral thesis, University of Cape Town, 2018. http://hdl.handle.net/11427/29467.

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Preclinical pharmacokinetics relies on efficient and accurate screening to select clinical candidates from early leads. Poor pharmacokinetic interpretation can disadvantage drug discovery by promoting inadequate compounds and expelling potential drug candidates. Objectives of this project included pharmacokinetic evaluation of antimalarial and anti-tuberculosis lead compounds with techniques aimed at improving preclinical pharmacokinetic outcomes. This included mechanistic pharmacokinetic approaches such as non-linear mixed effects (NLME) modelling in comparison with traditional non-compartmen

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19

Georgiou, Leonidas. "DCE-MRI assessment of hepatic uptake and efflux of the contrast agent, gadoxetate, to monitor transporter-mediated processes and drug-drug interactions : in vitro and in vivo studies." Thesis, University of Manchester, 2015. https://www.research.manchester.ac.uk/portal/en/theses/dcemri-assessment-of-hepatic-uptake-and-efflux-of-the-contrast-agent-gadoxetate-to-monitor-transportermediated-processes-and-drugdrug-interactions-in-vitro-and-in-vivo-studies(d4b3bc62-8636-470b-90ae-38e25e7ee7be).html.

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Dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) techniques offer the opportunity to understand the physiological processes involved in the distribution of the contrast agent in vivo. This work utilises a liver specific contrast agent (gadoxetate) and demonstrates the potential use of these techniques to study transporter-mediated process in vivo. In vitro experiments investigated gadoxetate’s interaction with uptake and efflux transporters at the cellular level, ideally a prerequisite to understand the contribution of transporter proteins in in vivo pharmacokinetics. MRI was use

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20

Nuthalapati, Silpa. "PRECLINICAL PHARMACOKINETIC AND PHARMACODYNAMIC EVALUATION OF NEW ANTICANCER AGENTS FOR BRAIN TUMOR CHEMOTHERAPY." Diss., Temple University Libraries, 2012. http://cdm16002.contentdm.oclc.org/cdm/ref/collection/p245801coll10/id/181390.

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Pharmaceutical Sciences<br>Ph.D.<br>Glioblastoma multiforme (GBM) is the most common malignant primary brain tumor in adults for which overall prognosis remains poor despite recent treatment advances, thus emphasizing the need for developing effective therapeutic agents. Styryl sulfones belong to a class of non-ATP competitive antineoplastic agents in early stage clinical trials. Detailed investigation of the pharmacokinetics (PKs) and pharmacodynamics (PDs) of novel agents in the preclinical stage plays a pivotal role in drug development that could be applied to guide clinical trials. The mai

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21

Tronde, Ann. "Pulmonary Drug Absorption : In vitro and in vivo investigations of drug absorption across the lung barrier and its relation to drug physicochemical properties." Doctoral thesis, Uppsala University, Department of Pharmacy, 2002. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-2557.

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<p>Although, pulmonary drug delivery is a well established means for targeting of drugs to the lungs for the treatment of respiratory diseases as well as for the systemic delivery of volatile anesthetic agents, drug absorption kinetics in the lung have not been subjected to extensive research. The main objective of this thesis was to investigate drug absorption characteristics of the lung barrier, using the isolated and perfused rat lung model and in vivo pharmacokinetic studies in rats. Physicochemically diverse drugs (i.e. atenolol, budesonide, cromolyn, cyanocobalamin, enalapril, enalaprila

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22

Higginbotham, Mary Lynn. "Preclinical pharmacokinetic and tolerance assessment and phase I clinical trial of MU-gold, a novel chemotherapeutic agent /." Free to MU Campus, others may purchase, 2004. http://wwwlib.umi.com/cr/mo/fullcit?p1421141.

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23

Benay, Stephan. "Mise au point des outils analytiques et formels utilisés dans la recherche préclinique en oncologie." Thesis, Aix-Marseille, 2014. http://www.theses.fr/2014AIXM5501.

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Afin d'analyser les données in vitro de l'effet de l'erlotinib sur la croissance des cellules A431 suivie par impédance-métrie, nous avons développé un modèle pharmacocinétique - pharmacodynamique non linéaire décrivant simultanément la diminution de la concentration d'erlotinib et son effet sur la croissance cellulaire au cours du temps. La non-linéarité du modèle imposant le recours à des méthodes itératives pour l'estimation des paramètres, plusieurs étapes de la procédure d'identification du modèle ont été étudiées et des solutions proposées, avec des exemples d'application à des molécules

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24

Percelay, Solenn. "Validation d'un modèle murin de schizophrénie pour améliorer la recherche de nouveaux traitements : approche psychopharmacologique, en imagerie et en électrophysiologie A new 3-hit mouse model of schizophrenia built on genetic, early and late factors Functional dysregulations in CA1 hippocampal networks of a 3-hit mouse model of schizophrenia Olfactory laterality is valence-dependent in mice Assessing olfactory laterality in mice: new tool in preclinical psychiatric study Combination of MAP6 deficit, maternal separation and MK801 in female mice: a 3-hit animal model of neurodevelopmental disorder with cognitive deficits Antipsychotic lurasidone: Behavioural and pharmacokinetic data in C57BL/6 mice." Thesis, Normandie, 2021. http://www.theses.fr/2021NORMC403.

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La schizophrénie est une maladie psychiatrique très invalidante qui concerne près de 1% de la population. Bien que son étiologie soit toujours inconnue, elle est certainement multifactorielle et comprend une interaction entre prédisposition génétique et facteurs environnementaux. Il existe des traitements médicamenteux mais ils ne sont pas totalement efficaces, particulièrement pour la prise en charge des symptômes négatifs et des déficits cognitifs. Le développement de nouveaux traitements plus efficaces passe par l’amélioration des modèles animaux prenant en compte le caractère multifactorie

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25

Shen, Liang. "preclinical pharmacokinetics and bioavailability studies of S-carboxymethylcysteine, N-acetylcysteine and (-)-carbodine." 2008. http://purl.galileo.usg.edu/uga%5Fetd/shen%5Fliang%5F200812%5Fphd.

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26

Loadman, Paul M., Michael C. Bibby, Steven D. Shnyder, et al. "Comparative Preclinical Pharmacokinetic and Metabolic Studies of the Combretastatin Prodrugs Combretastatin A4 Phosphate and A1 Phosphate." 2004. http://hdl.handle.net/10454/2953.

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Purpose: Combretastatin A4 phosphate (CA4P) and its structural analog, combretastatin A1 phosphate (CA1P), are soluble prodrugs capable of interacting with tubulin and causing rapid vascular shutdown within tumors. CA4P has completed Phase I clinical trials, but recent preclinical studies have shown that CA1P displays a greater antitumor effect than the combretastatin A4 (CA4) analog at equal doses. The aim of this study, therefore, is to compare pharmacokinetics and metabolism of the two compounds to determine whether pharmacokinetics plays a role in their differential activity. Experimenta

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27

Kirwan, Ian G., Paul M. Loadman, David J. Swaine, et al. "Comparative Preclinical Pharmacokinetic and Metabolic Studies of the Combretastatin Prodrugs Combretastatin A4 Phosphate and A1 Phosphate." 2004. http://hdl.handle.net/10454/13684.

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no<br>Purpose: Combretastatin A4 phosphate (CA4P) and its structural analog, combretastatin A1 phosphate (CA1P), are soluble prodrugs capable of interacting with tubulin and causing rapid vascular shutdown within tumors. CA4P has completed Phase I clinical trials, but recent preclinical studies have shown that CA1P displays a greater antitumor effect than the combretastatin A4 (CA4) analog at equal doses. The aim of this study, therefore, is to compare pharmacokinetics and metabolism of the two compounds to determine whether pharmacokinetics plays a role in their differential activity. Experim

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Kong, Linghui. "Preclinical pharmacokinetic studies of 3'-azido-2',3'-dideoxyuridine and its novel prodrugs." 2001. http://purl.galileo.usg.edu/uga%5Fetd/kong%5Flinghui%5F200108%5Fphd.

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Thesis (Ph. D.)--University of Georgia, 2001.<br>Directed by F.D Boudinot. Includes articles submitted to Antiviral chemistry and chemotherapy, Journal of chromatography B: biomedical applications, and Antimicrobial agents and chemotherapy. Includes bibliographical references.

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29

Höcherl, Peter [Verfasser]. "New tariquidar-like ABCB1 modulators in cancer chemotherapy : preclinical pharmacokinetic, pharmacodynamic investigations and computational studies / vorgelegt von Peter Höcherl." 2010. http://d-nb.info/1004959842/34.

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30

Authier, Simon. "Validation des modèles de pharmacologie de sécurité et évaluation de la valeur thérapeutique de l'oxytocine dans le traitement de l'infarctus du myocarde." Thèse, 2009. http://hdl.handle.net/1866/3247.

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En février, 2009 un rapport de PHRMA (Pharmaceutical Research and Manufacturers of America) confirmait que plus de 300 médicaments pour le traitement des maladies cardiaques étaient en phase d’essais cliniques ou en révision par les agences règlementaires. Malgré cette abondance de nouvelles thérapies cardiovasculaires, le nombre de nouveaux médicaments approuvés chaque année (toutes indications confondues) est en déclin avec seulement 17 et 24 nouveaux médicaments approuvés en 2007 et 2008, respectivement. Seulement 1 médicament sur 5000 sera approuvé après 10 à 15 ans de développement au coû

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