Preclinical comparison of osimertinib with other EGFR-TKIs in EGFR-mutant NSCLC brain metastases models, and early evidence of clinical brain metastases activity
…, DW Kim, JCH Yang, M Cantarini, K Pickup… - Clinical Cancer …, 2016 - AACR
Purpose: Approximately one-third of patients with non–small cell lung cancer (NSCLC)
harboring tumors with EGFR-tyrosine kinase inhibitor (TKI)-sensitizing mutations (EGFRm) …
harboring tumors with EGFR-tyrosine kinase inhibitor (TKI)-sensitizing mutations (EGFRm) …
Metabolic disposition of osimertinib in rats, dogs, and humans: insights into a drug designed to bind covalently to a cysteine residue of epidermal growth factor …
…, J Collier, P Frewer, S Martin, K Pickup… - Drug Metabolism and …, 2016 - ASPET
Preclinical and clinical studies were conducted to determine the metabolism and pharmacokinetics
of osimertinib and key metabolites AZ5104 and AZ7550. Osimertinib was designed …
of osimertinib and key metabolites AZ5104 and AZ7550. Osimertinib was designed …
Diclofenac metabolism in the mouse: Novel in vivo metabolites identified by high performance liquid chromatography coupled to linear ion trap mass spectrometry
S Sarda, C Page, K Pickup, T Schulz-Utermoehl… - Xenobiotica, 2012 - Taylor & Francis
The metabolism of [ 14 C]-diclofenac in mice was investigated following a single oral dose of
10 mg/kg. The majority of the drug-related material was excreted in the urine within 24 h of …
10 mg/kg. The majority of the drug-related material was excreted in the urine within 24 h of …
Utility of spatially-resolved atmospheric pressure surface sampling and ionization techniques as alternatives to mass spectrometric imaging (MSI) in drug metabolism
EQ Blatherwick, GJ Van Berkel, K Pickup… - Xenobiotica, 2011 - Taylor & Francis
Tissue distribution studies of drug molecules play an essential role in the pharmaceutical
industry and are commonly undertaken using quantitative whole body autoradiography (QWBA…
industry and are commonly undertaken using quantitative whole body autoradiography (QWBA…
Pharmacokinetics and metabolism of midazolam in chimeric mice with humanised livers
K Samuelsson, K Pickup, S Sarda, JG Swales… - Xenobiotica, 2012 - Taylor & Francis
The pharmacokinetics and biotransformation of midazolam were investigated following single
oral doses of 0.1, 1 and 10 mg/kg to chimeric mice with humanised livers (PXB mice) and …
oral doses of 0.1, 1 and 10 mg/kg to chimeric mice with humanised livers (PXB mice) and …
The hepatic reductase null mouse as a model for exploring hepatic conjugation of xenobiotics: application to the metabolism of diclofenac
K Pickup, A Gavin, HB Jones, E Karlsson, C Page… - Xenobiotica, 2012 - Taylor & Francis
The distribution, metabolism, excretion and hepatic effects of diclofenac were investigated
following a single oral dose of 10 mg/kg to wild type and hepatic reductase null (HRN) mice. …
following a single oral dose of 10 mg/kg to wild type and hepatic reductase null (HRN) mice. …
Troglitazone metabolism and transporter effects in chimeric mice: a comparison between chimeric humanized and chimeric murinized FRG mice
K Samuelsson, K Pickup, S Sarda, JR Foster… - Xenobiotica, 2014 - Taylor & Francis
The biotransformation, hepatic transporter and blood chemistry effects of troglitazone were
investigated following 7 days of dosing at 600 mg/kg/day to chimeric murinized or humanized …
investigated following 7 days of dosing at 600 mg/kg/day to chimeric murinized or humanized …
Drug–drug interactions and metabolism in cytochrome P450 2C knockout mice: Application to troleandomycin and midazolam
A Grimsley, R Gallagher, M Hutchison, K Pickup… - Biochemical …, 2013 - Elsevier
Drug–drug interactions (DDIs) may cause serious drug toxicity and delay development of
candidate drugs. Screening using human liver microsomes and hepatocytes can help predict …
candidate drugs. Screening using human liver microsomes and hepatocytes can help predict …
The metabolic fate of [14C]-fenclozic acid in the hepatic reductase null (HRN) mouse
K Pickup, J Wills, A Rodrigues, HB Jones, C Page… - Xenobiotica, 2014 - Taylor & Francis
The distribution, metabolism, excretion and hepatic effects of fenclozic acid were investigated
following a single oral dose of 10 mg/kg to hepatic reductase null (HRN) mice. 2. The …
following a single oral dose of 10 mg/kg to hepatic reductase null (HRN) mice. 2. The …
HPLC–MS Profiling and Structural Identification of [14C]-Diclofenac Metabolites in Mouse Bile
S Sarda, EA Partridge, K Pickup, A McCarthy… - Chromatographia, 2014 - Springer
Biliary metabolites present at 6 h post-dose following a single oral dose of [ 14 C]-diclofenac
(10 mg kg −1 ) to male bile duct-cannulated C57BL/6 J mice were profiled and identified. …
(10 mg kg −1 ) to male bile duct-cannulated C57BL/6 J mice were profiled and identified. …