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Sarah Kempshall

Explore the profile of Sarah Kempshall including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 12
Citations 294
Followers 0
Related Specialties
Pharmacology
Biochemistry
Toxicology
Top 10 Co-Authors
Katherine S Fenner
Yurong Lai
Bo Feng
Matthew D Troutman
Hugh A Barton
Hannah M Jones
Ruth Hyland
Iain Gardner
Mohammed Ullah
Emi Kimoto
Published In
Drug Metab Dispos
Xenobiotica
Br J Clin Pharmacol
J Pharm Sci
Mol Pharm
Affiliations
Soon will be listed here.
Recent Articles
1.
In vitro evaluation of hepatic transporter-mediated clinical drug-drug interactions: hepatocyte model optimization and retrospective investigation
Bi Y, Kimoto E, Sevidal S, Jones H, Barton H, Kempshall S, et al.
Drug Metab Dispos . 2012 Mar; 40(6):1085-92. PMID: 22381335
To assess the feasibility of using sandwich-cultured human hepatocytes (SCHHs) as a model to characterize transport kinetics for in vivo pharmacokinetic prediction, the expression of organic anion-transporting polypeptide (OATP) proteins...
2.
Mechanistic pharmacokinetic modeling for the prediction of transporter-mediated disposition in humans from sandwich culture human hepatocyte data
Jones H, Barton H, Lai Y, Bi Y, Kimoto E, Kempshall S, et al.
Drug Metab Dispos . 2012 Feb; 40(5):1007-17. PMID: 22344703
With efforts to reduce cytochrome P450-mediated clearance (CL) during the early stages of drug discovery, transporter-mediated CL mechanisms are becoming more prevalent. However, the prediction of plasma concentration-time profiles for...
3.
The evolution of the OATP hepatic uptake transport protein family in DMPK sciences: from obscure liver transporters to key determinants of hepatobiliary clearance
Fenner K, Jones H, Ullah M, Kempshall S, Dickins M, Lai Y, et al.
Xenobiotica . 2011 Nov; 42(1):28-45. PMID: 22077101
Over the last two decades the impact on drug pharmacokinetics of the organic anion transporting polypeptides (OATPs: OATP-1B1, 1B3 and 2B1), expressed on the sinusoidal membrane of the hepatocyte, has...
4.
Case studies addressing human pharmacokinetic uncertainty using a combination of pharmacokinetic simulation and alternative first in human paradigms
Harrison A, Gardner I, Hay T, Dickins M, Beaumont K, Phipps A, et al.
Xenobiotica . 2011 Oct; 42(1):57-74. PMID: 21992032
PF-184298 ((S)-2,3-dichloro-N-isobutyl-N-pyrrolidin-3-ylbenzamide) and PF-4776548 ((3-(4-fluoro-2-methoxy-benzyl)-7-hydroxy-8,9-dihydro-3H,7H-pyrrolo[2,3-c][1,7]naphthyridin-6-one)) are novel compounds which were selected to progress to human studies. Discordant human pharmacokinetic predictions arose from pre-clinical in vivo studies in rat and dog,...
5.
Full efficacy with no CNS side-effects: unachievable panacea or reality? DMPK considerations in design of drugs with limited brain penetration
Cole S, Bagal S, El-Kattan A, Fenner K, Hay T, Kempshall S, et al.
Xenobiotica . 2011 Oct; 42(1):11-27. PMID: 21970687
Optimising drug properties can be an important strategy to limit penetration into the CNS and offers advantages in reducing the risk of undesirable neurological effects When considering the design of...
6.
Development of a new permeability assay using low-efflux MDCKII cells
Di L, Whitney-Pickett C, Umland J, Zhang H, Zhang X, Gebhard D, et al.
J Pharm Sci . 2011 Jul; 100(11):4974-85. PMID: 21766308
Permeability is an important property of drug candidates. The Madin-Darby canine kidney cell line (MDCK) permeability assay is widely used and the primary concern of using MDCK cells is the...
7.
A comprehensive non-clinical evaluation of the CNS penetration potential of antimuscarinic agents for the treatment of overactive bladder
Callegari E, Malhotra B, Bungay P, Webster R, Fenner K, Kempshall S, et al.
Br J Clin Pharmacol . 2011 Mar; 72(2):235-46. PMID: 21392072
What Is Already Known About This Subject: This study provides antimuscarinic agents for overactive bladder (OAB) display variable association with side effects mediated by the central nervous system (CNS), which...
8.
Investigation into UDP-glucuronosyltransferase (UGT) enzyme kinetics of imidazole- and triazole-containing antifungal drugs in human liver microsomes and recombinant UGT enzymes
Bourcier K, Hyland R, Kempshall S, Jones R, Maximilien J, Irvine N, et al.
Drug Metab Dispos . 2010 Mar; 38(6):923-9. PMID: 20304965
Imidazoles and triazoles represent major classes of antifungal azole derivatives. With respect to UDP-glucuronosyltransferase (UGT) enzymes, the drug metabolism focus has mainly concentrated on their inhibitory effects with little known...
9.
Excretion and metabolism of lersivirine (5-{[3,5-diethyl-1-(2-hydroxyethyl)(3,5-14C2)-1H-pyrazol-4-yl]oxy}benzene-1,3-dicarbonitrile), a next-generation non-nucleoside reverse transcriptase inhibitor, after administration of [14C]Lersivirine to...
Vourvahis M, Gleave M, Nedderman A, Hyland R, Gardner I, Howard M, et al.
Drug Metab Dispos . 2010 Feb; 38(5):789-800. PMID: 20124396
Lersivirine [UK-453,061, 5-((3,5-diethyl-1-(2-hydroxyethyl)(3,5-14C2)-1H-pyrazol-4-yl)oxy)benzene-1,3-dicarbonitrile] is a next-generation non-nucleoside reverse transcriptase inhibitor, with a unique binding interaction within the reverse transcriptase binding pocket. Lersivirine has shown antiviral activity and is well tolerated...
10.
Refining the in vitro and in vivo critical parameters for P-glycoprotein, [I]/IC50 and [I2]/IC50, that allow for the exclusion of drug candidates from clinical digoxin interaction studies
Cook J, Feng B, Fenner K, Kempshall S, Liu R, Rotter C, et al.
Mol Pharm . 2009 Dec; 7(2):398-411. PMID: 20025245
The objective of this work was to further investigate the reasons for disconcordant clinical digoxin drug interactions (DDIs) particularly for false negative where in vitro data suggests no P-glycoprotein (P-gp)...