Metabolism and disposition of imatinib mesylate in healthy volunteers

HP Gschwind, U Pfaar, F Waldmeier, M Zollinger… - Drug metabolism and …, 2005 - ASPET
… Radiolabeled components detected in urine and feces are indicated as U and F. Amounts
of imatinib and its metabolites in urine (0-72 h) and feces (0-168 h) are given in percentage of …

Biodistribution and plasma protein binding of zoledronic acid

HM Weiss, U Pfaar, A Schweitzer, H Wiegand… - Drug Metabolism and …, 2008 - ASPET
… of unbound drug (C u )] and in the sample introduced into the reservoir before ultrafiltration
[concentration in plasma (C p )]. The unbound fraction in plasma was calculated as C u /C p . …

Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800

…, J Brueggen, P Chène, MJ Drysdale, U Pfaar… - Molecular cancer …, 2010 - AACR
Heat shock protein 90 (Hsp90) is a ubiquitously expressed molecular chaperone with ATPase
activity involved in the conformational maturation and stability of key signaling molecules …

Absorption, distribution, metabolism, and excretion of capmatinib (INC280) in healthy male volunteers and in vitro aldehyde oxidase phenotyping of the major …

…, R Hansen, K Schroer, G Rahmanzadeh, U Pfaar… - Drug Metabolism and …, 2020 - ASPET
Capmatinib (INC280), a highly selective and potent inhibitor of the MET receptor tyrosine
kinase, has demonstrated clinically meaningful efficacy and a manageable safety profile in …

Phenotypic and metabolic investigation of a CSF-1R kinase receptor inhibitor (BLZ945) and its pharmacologically active metabolite

JA Krauser, Y Jin, M Walles, U Pfaar, J Sutton… - Xenobiotica, 2015 - Taylor & Francis
… The heated capillary temperature was set to 300 C, sheath gas flow was 40 U, auxiliary
gas flow was 10 U, spray voltage was 4 kV and capillary voltage 19 kV. The instrument was …

Development and validation of a highly sensitive RIA for zoledronic acid, a new potent heterocyclic bisphosphonate, in human serum, plasma and urine

F Legay, S Gauron, F Deckert, G Gosset, U Pfaar… - … of pharmaceutical and …, 2002 - Elsevier
Zoledronic acid is a new, highly potent bisphosphonate drug under clinical evaluation. A
radioimmunoassay has been developed to determine zoledronic acid concentration in human …

Characterization of a novel diclofenac metabolite in human urine by capillary gas chromatography-negative chemical ionization mass spectrometry

W Blum, JW Faigle, U Pfaar, A Sallmann - Journal of Chromatography B …, 1996 - Elsevier
A sensitive analytical method was developed to characterize diclofenac metabolites in small
amounts of body fluids. Desalted and lyophilized urine samples were extracted with …

Enzymatic synthesis of β-D-glucuronides with in situ regeneration of uridine 5′-diphosphoglucuronic acid

D Gygax, P Spies, T Winkler, U Pfaar - Tetrahedron, 1991 - Elsevier
β-D-glucuronides of 1 and 2 have been synthesized by a multi-enzyme system with in situ
regeneration of uridine 5′-diphosphoglucuronic acid. Crude liver homogenate containing all …

A microplate solid scintillation counter as a radioactivity detector for high performance liquid chromatography in drug metabolism: validation and applications

GJ Bruin, F Waldmeier, KO Boernsen, U Pfaar… - … of Chromatography A, 2006 - Elsevier
Sensitive radioactivity detection following high performance liquid chromatography (HPLC)
separation remains a challenge in many drug metabolism studies with radiolabeled …

MIK665/S64315, a novel Mcl-1 inhibitor, in combination with Bcl-2 inhibitors exhibits strong synergistic antitumor activity in a range of hematologic malignancies

…, S Sanghavi, Y Chen, G Lysiak, AL Maragno, U Pfaar… - Cancer Research, 2019 - AACR
One of the hallmarks of cancer is evasion of apoptosis. The B-cell lymphoma-2 (Bcl-2) family
of proteins represents a crucial point of control of apoptosis. The Bcl-2 family comprises …